Literature for peptidase A01.004: BACE1 g.p. (Homo sapiens)

Summary Gene structure Alignment Tree Sequences Sequence features Distribution Structure Literature Substrates Pharma

(Topics flags: A Assay, S Structure, T Target, P Specificity, K Knockout, E Expression, V Review, M Mutation, R Splicing, I Inhibitor, L Localization. To select only the references relevant to a single topic, click the link above. See explanation.)

    2024
  1. Banoo,R., Nuthakki,V.K., Wadje,B.N., Sharma,A. and Bharate,S.B.
    Design, synthesis, and pharmacological evaluation of indole-piperidine amides as Blood-brain barrier permeable dual cholinesterase and beta-secretase inhibitors
    Eur J Med Chem266, 116131-116131. PubMed  Europe PubMed DOI  I
  2. Coimbra,J.R.M., Resende,R., Custodio,J.B.A., Salvador,J.A.R. and Santos,A.E.
    BACE1 Inhibitors for Alzheimer's Disease: Current Challenges and Future Perspectives
    J Alzheimers Dis101, S53-S78. PubMed  Europe PubMed DOI  V
  3. Gao,F., Zhang,M., Wang,Q., Ni,M., Liu,C., Deng,K., Xie,Q., Wang,S., Shi,J. and Shen,Y.
    Associations of CSF BACE1 with amyloid pathology, neurodegeneration, and cognition in Alzheimer's disease
    Acta Neuropathol147, 97-97. PubMed  Europe PubMed DOI
  4. Jia,T., Wang,H., Chi,W., Zhou,W., Guo,L., Dai,Y., Bian,K., Sun,Z., Ding,X. and Yu,Y.
    Knockdown of BACE1 by a multistage brain-targeting polyion complex improved memory and learning behaviors in APP/PS1 transgenic mouse model
    Int J Pharm650, 123727-123727. PubMed  Europe PubMed DOI
  5. Li,Y., Li,H., Liang,W., Li,Y. and Wang,Z.
    The Large Ectodomain of APP Prevents APP from being Directly Cleaved by gamma-Secretase
    Front Biosci (Landmark Ed)29, 78-78. PubMed  Europe PubMed DOI
  6. Nakamoto,K., Kikuhara,S., Fujimori,H., Saraswat,B., Gao,Z., Vadi Velu,A., Zhang,Z., Tong,Y., Imamichi,S., Nozaki,T., Murakami,Y. and Masutani,M.
    Effect of Functional Inhibition of BACE1 on Sensitization to gamma-Irradiation in Cancer Cells
    Curr Issues Mol Biol46, 450-460. PubMed  Europe PubMed DOI  K
  7. Quang De,T., Nguyen,C.Q., Le Dang,Q., Nguyen Thi,N.Y., Trong Tuan,N., Hoon Suh,D., Chu,J., Bepary,S., Lee,G.H., Kang,N.S., Cho,H., Park,W.K. and Lim,H.J.
    Rational design of novel diaryl ether-linked benzimidazole derivatives as potent and selective BACE1 inhibitors
    Biochem Biophys Res Commun698, 149538-149538. PubMed  Europe PubMed DOI  I
  8. Schmidt,A., Hrupka,B., van Bebber,F., Sunil Kumar,S., Feng,X., Tschirner,S.K., Assfalg,M., Muller,S.A., Hilger,L.S., Hofmann,L.I., Pigoni,M., Jocher,G., Voytyuk,I., Self,E.L., Ito,M., Hyakkoku,K., Yoshimura,A., Horiguchi,N., Feederle,R., De Strooper,B., Schulte-Merker,S., Lammert,E., Moechars,D., Schmid,B. and Lichtenthaler,S.F.
    The Alzheimer's disease-linked protease BACE2 cleaves VEGFR3 and modulates its signaling
    J Clin Invest134, e170550-e170550. PubMed  Europe PubMed DOI
  9. Tutus,B., Kaya,A.Z., Baz,Y., Evren,A.E., Saglik Ozkan,B.N. and Yurttas,L.
    Synthesis of new N-(5,6-methylenedioxybenzothiazole-2-yl)-2-[(substituted)thio/piperazine]acetamide/propanamide derivatives and evaluation of their AChE, BChE, and BACE-1 inhibitory activities
    Drug Dev Res85, e22214-e22214. PubMed  Europe PubMed DOI  I
  10. Wang,Y.R., Zeng,X.Q., Wang,J., Fowler,C.J., Li,Q.X., Bu,X.L., Doecke,J., Maruff,P., Martins,R.N., Rowe,C.C., Masters,C.L., Wang,Y.J. and Liu,Y.H.
    Autoantibodies to BACE1 promote Abeta accumulation and neurodegeneration in Alzheimer's disease
    Acta Neuropathol148, 57-57. PubMed  Europe PubMed DOI
  11. Wang,Z., Zhou,J., Zhang,B., Xu,Z., Wang,H., Sun,Q. and Wang,N.
    Inhibitory effects of beta-asarone on lncRNA BACE1-mediated induction of autophagy in a model of Alzheimer's disease
    Behav Brain Res463, 114896-114896. PubMed  Europe PubMed DOI
  12. Wei,X., Fan,J., Hao,Y., Dong,H., Zhang,Y., Zhou,Y. and Xu,M.
    Electrochemiluminescence and electrochemical dual-mode detection of BACE1 activity based on the assembly of peptide and luminol co-functionalized silver nanoparticles induced by cucurbit[8]uril
    Talanta266, 124904-124904. PubMed  Europe PubMed DOI
  13. Zimmer,V.C., Lauer,A.A., Haupenthal,V., Stahlmann,C.P., Mett,J., Grosgen,S., Hundsdorfer,B., Rothhaar,T., Endres,K., Eckhardt,M., Hartmann,T., Grimm,H.S. and Grimm,M.O.W.
    A bidirectional link between sulfatide and Alzheimer's disease
    Cell Chem Biol31, 265-283. PubMed  Europe PubMed DOI
  14. 2023
  15. Abraham,C.B., Xu,L., Pantelopulos,G.A. and Straub,J.E.
    Characterizing the transmembrane domains of ADAM10 and BACE1 and the impact of membrane composition
    Biophys J122, 3999-4010. PubMed  Europe PubMed DOI
  16. Bao,H. and Shen,Y.
    Unmasking BACE1 in aging and age-related diseases
    Trends Mol Med29, 99-111. PubMed  Europe PubMed DOI  V
  17. Benoit,M.R., Darboe,M., Das,B., Ge,Y., Zhou,J., Yao,A., He,W., Yan,R. and Hu,X.
    Postnatal neuronal Bace1 deletion impairs neuroblast and oligodendrocyte maturation
    Hum Mol Genet32, 1193-1207. PubMed  Europe PubMed DOI
  18. Bhatia,S., Singh,M., Sharma,P., Mujwar,S., Singh,V., Mishra,K.K., Singh,T.G., Singh,T. and Ahmad,S.F.
    Scaffold Morphing and In Silico Design of Potential BACE-1 (beta-Secretase) Inhibitors: A Hope for a Newer Dawn in Anti-Alzheimer Therapeutics
    Molecules28, PubMed  Europe PubMed DOI  I
  19. Drozdowska,D., Maliszewski,D., Wrobel,A., Ratkiewicz,A. and Sienkiewicz,M.
    New Benzamides as Multi-Targeted Compounds: A Study on Synthesis, AChE and BACE1 Inhibitory Activity and Molecular Docking
    Int J Mol Sci24, PubMed  Europe PubMed DOI  I
  20. Monteiro,K.L.C., Dos Santos Alcantara,M.G., Freire,N.M.L., Brandao,E.M., do Nascimento,V.L., Dos Santos Viana,L.M., de Aquino,T.M. and da Silva-Junior,E.F.
    BACE-1 Inhibitors Targeting Alzheimer's Disease
    Curr Alzheimer Res20, 131-148. PubMed  Europe PubMed DOI  V  I
  21. Munj,S.M. and Patil,P.B.
    Drug Discovery to Drug Development of BACE1 Inhibitor as Antialzheimer's: A Review
    Curr Top Med Chem23, 77-97. PubMed  Europe PubMed DOI  V
  22. Nangare,S. and Patil,P.
    Platinum-alginate-chitosan nanobioconjugate decorated carbon backbone layered biosensor for highly sensitive and selective detection of BACE-1
    Int J Biol Macromol250, 126224-126224. PubMed  Europe PubMed DOI
  23. Pratsch,K., Unemura,C., Ito,M., Lichtenthaler,S.F., Horiguchi,N. and Herms,J.
    New Highly Selective BACE1 Inhibitors and Their Effects on Dendritic Spine Density In Vivo
    Int J Mol Sci24, PubMed  Europe PubMed DOI  I
  24. Rather,H.A., Almousa,S., Kumar,A., Sharma,M., Pennington,I., Kim,S., Su,Y., He,Y., Ghara,A.R., Sai,K.K.S., Navone,N.M., Vander Griend,D.J. and Deep,G.
    The beta-Secretase 1 Enzyme as a Novel Therapeutic Target for Prostate Cancer
    Cancers (Basel)16, PubMed  Europe PubMed DOI
  25. 2022
  26. Bhakat,S. and Soderhjelm,P.
    Flap Dynamics in Pepsin-Like Aspartic Proteases: A Computational Perspective Using Plasmepsin-II and BACE-1 as Model Systems
    J Chem Inf Model62, 914-926. PubMed  Europe PubMed DOI
  27. Choi,J.Y., Park,J.H., Jo,C., Kim,K.C. and Koh,Y.H.
    SARS-CoV-2 spike S1 subunit protein-mediated increase of beta-secretase 1 (BACE1) impairs human brain vessel cells
    Biochem Biophys Res Commun626, 66-71. PubMed  Europe PubMed DOI
  28. Diaz,A., Martin-Jimenez,C., Woo,Y., Merino,P., Torre,E. and Yepes,M.
    Urokinase-Type Plasminogen Activator Triggers Wingless/Int1-Independent Phosphorylation of the Low-Density Lipoprotein Receptor-Related Protein-6 in Cerebral Cortical Neurons
    J Alzheimers Dis89, 877-891. PubMed  Europe PubMed DOI
  29. Ihara,M.
    Endothelial BACE1: Bridging the Gap Between Hypertension and Alzheimer's Disease
    Circ Res130, 1342-1344. PubMed  Europe PubMed DOI
  30. Sayad,A., Najafi,S., Hussen,B.M., Abdullah,S.T., Movahedpour,A., Taheri,M. and Hajiesmaeili,M.
    The Emerging Roles of the beta-Secretase BACE1 and the Long Non-coding RNA BACE1-AS in Human Diseases: A Focus on Neurodegenerative Diseases and Cancer
    Front Aging Neurosci14, 853180-853180. PubMed  Europe PubMed DOI
  31. Singh,N., Benoit,M.R., Zhou,J., Das,B., Davila-Velderrain,J., Kellis,M., Tsai,L.H., Hu,X. and Yan,R.
    BACE-1 inhibition facilitates the transition from homeostatic microglia to DAM-1
    Sci Adv8, eabo1286-eabo1286. PubMed  Europe PubMed DOI
  32. Taoka,B.M., Wu,W.L., Hao,J., Dolmaski,M., Wang,H., Levorse,D., Orth,P., Hyde,L.A., Smith,B., Michener,M.S., Kennedy,M.E., Parker,E.M. and Cumming,J.N.
    Design and discovery of C2-fluoroalkyl iminothiazine dioxides as BACE inhibitors
    Bioorg Med Chem Lett56, 128463-128463. PubMed  Europe PubMed DOI  I
  33. Taylor,H.A., Przemylska,L., Clavane,E.M. and Meakin,P.J.
    BACE1: More than just a beta-secretase
    Obes Reve13430-e13430. PubMed  Europe PubMed DOI  V
  34. Ugbaja,S.C., Lawal,I.A., Abubakar,B.H., Mushebenge,A.G., Lawal,M.M. and Kumalo,H.M.
    Allostery Inhibition of BACE1 by Psychotic and Meroterpenoid Drugs in Alzheimer's Disease Therapy
    Molecules27, PubMed  Europe PubMed DOI
  35. Yeap,Y.J., Kandiah,N., Nizetic,D. and Lim,K.L.
    BACE2: A Promising Neuroprotective Candidate for Alzheimer's Disease
    J Alzheimers Dis PubMed  Europe PubMed DOI  V
  36. 2021
  37. Armbrust,F., Bickenbach,K., Marengo,L., Pietrzik,C. and Becker-Pauly,C.
    The Swedish dilemma - the almost exclusive use of APPswe-based mouse models impedes adequate evaluation of alternative beta-secretases
    Biochim Biophys Acta Mol Cell Res119164-119164. PubMed  Europe PubMed DOI
  38. Bhakat,S.
    Pepsin-like aspartic proteases (PAPs) as model systems for combining biomolecular simulation with biophysical experiments
    RSC Adv11, 11026-11047. PubMed  Europe PubMed DOI
  39. Bouza,A.A., Edokobi,N., Hodges,S.L., Pinsky,A.M., Offord,J., Piao,L., Zhao,Y.T., Lopatin,A.N., Lopez-Santiago,L.F. and Isom,L.L.
    Sodium channel beta1 subunits participate in regulated intramembrane proteolysis-excitation coupling
    JCI Insight PubMed  Europe PubMed DOI
  40. Checler,F., Afram,E., Pardossi-Piquard,R. and Lauritzen,I.
    Is gamma-secretase a beneficial inactivating enzyme of the toxic APP C-terminal fragment C99?
    J Biol Chem100489-100489. PubMed  Europe PubMed DOI  V
  41. Fissel,J.A. and Farah,M.H.
    The influence of BACE1 on macrophage recruitment and activity in the injured peripheral nerve
    J Neuroinflammation18, 71-71. PubMed  Europe PubMed DOI  V
  42. Fujimoto,K., Yoshida,S., Tadano,G., Asada,N., Fuchino,K., Suzuki,S., Matsuoka,E., Yamamoto,T., Yamamoto,S., Ando,S., Kanegawa,N., Tonomura,Y., Ito,H., Moechars,D., Rombouts,F.J.R., Gijsen,H.J.M. and Kusakabe,K.I.
    Structure-Based Approaches to Improving Selectivity through Utilizing Explicit Water Molecules: Discovery of Selective beta-Secretase (BACE1) Inhibitors over BACE2
    J Med Chem64, 3075-3085. PubMed  Europe PubMed DOI  I
  43. Gaborit,B., Govers,R., Altie,A., Brunel,J.M., Morange,P. and Peiretti,F.
    The aminosterol Claramine inhibits beta-secretase 1-mediated insulin receptor cleavage
    J Biol Chem100818-100818. PubMed  Europe PubMed DOI
  44. Ma,F., Wang,Q., Xu,Q. and Zhang,C.Y.
    Self-Assembly of Superquenched Gold Nanoparticle Nanosensors for Lighting up BACE-1 in Live Cells
    Anal Chem93, 15124-15132. PubMed  Europe PubMed DOI
  45. McKinzie,D.L., Winneroski,L.L., Green,S.J., Hembre,E.J., Erickson,J.A., Willis,B.A., Monk,S.A., Aluise,C.D., Baker,T.K., Lopez,J.E., Hendle,J., Beck,J.P., Brier,R.A., Boggs,L.N., Borders,A.R., Cocke,P.J., Garcia-Losada,P., Lowe,S.L., Mathes,B.M., May,P.C., Porter,W.J., Stout,S.L., Timm,D.E., Watson,B.M., Yang,Z. and Mergott,D.J.
    Discovery and Early Clinical Development of LY3202626, a Low-Dose, CNS-Penetrant BACE Inhibitor
    J Med Chem64, 8076-8100. PubMed  Europe PubMed DOI  I
  46. Miranda,A., Montiel,E., Ulrich,H. and Paz,C.
    Selective Secretase Targeting for Alzheimer's Disease Therapy
    J Alzheimers Dis PubMed  Europe PubMed DOI  I
  47. Mycroft-West,C.J., Devlin,A.J., Cooper,L.C., Guimond,S.E., Procter,P., Guerrini,M., Miller,G.J., Fernig,D.G., Yates,E.A., Lima,M.A. and Skidmore,M.A.
    Glycosaminoglycans from Litopenaeus vannamei Inhibit the Alzheimer's Disease beta Secretase, BACE1
    Mar Drugs19, PubMed  Europe PubMed DOI  I
  48. Pont,C., Ginex,T., Grinan-Ferre,C., Scheiner,M., Mattellone,A., Martinez,N., Arce,E.M., Soriano-Fernandez,Y., Naldi,M., De Simone,A., Barenys,M., Gomez-Catalan,J., Perez,B., Sabate,R., Andrisano,V., Loza,M.I., Brea,J., Bartolini,M., Bolognesi,M.L., Decker,M., Pallas,M., Luque,F.J. and Munoz-Torrero,D.
    From virtual screening hits targeting a cryptic pocket in BACE-1 to a nontoxic brain permeable multitarget anti-Alzheimer lead with disease-modifying and cognition-enhancing effects
    Eur J Med Chem225, 113779-113779. PubMed  Europe PubMed DOI
  49. Ugbaja,S., Lawal,I., Kumalo,H. and Lawal,M.
    Alzheimer's Disease and beta-Secretase Inhibition: An Update With a Focus on Computer-Aided Inhibitor Design
    Curr Drug Targets PubMed  Europe PubMed DOI  V
  50. Vishal,P.K., Oh,J.M., Khames,A., Abdelgawad,M.A., Nair,A.S., Nath,L.R., Gambacorta,N., Ciriaco,F., Nicolotti,O., Kim,H. and Mathew,B.
    Trimethoxylated Halogenated Chalcones as Dual Inhibitors of MAO-B and BACE-1 for the Treatment of Neurodegenerative Disorders
    Pharmaceutics13, PubMed  Europe PubMed DOI  I
  51. Xia,Y., Wang,Z.H., Zhang,Z., Liu,X., Yu,S.P., Wang,J.Z., Wang,X.C. and Ye,K.
    Delta- and beta- secretases crosstalk amplifies the amyloidogenic pathway in Alzheimer's disease
    Prog Neurobiol102113-102113. PubMed  Europe PubMed DOI
  52. 2020

  53. Correction for Bao et al., BACE1 SUMOylation increases its stability and escalates the protease activity in Alzheimer's disease
    Proc Natl Acad Sci U S A117, 28528-28530. PubMed  Europe PubMed DOI
  54. Ali,S., Asad,M.H.H.B., Khan,F., Murtaza,G., Rizvanov,A.A., Iqbal,J., Babak,B. and Hussain,I.
    Biological evaluation of newly synthesized biaryl guanidine derivatives to arrest beta-secretase enzymatic activity involved in Alzheimer's disease
    Biomed Res Int2020, 8934289-8934289. PubMed  Europe PubMed DOI  I
  55. Arakawa,R., Takano,A., Stenkrona,P., Stepanov,V., Nag,S., Jahan,M., Gryback,P., Bolin,M., Chen,L., Zhang,L., He,P., Villalobos,A., McCarthy,T.J., Halldin,C. and Varrone,A.
    PET imaging of beta-secretase 1 in the human brain: radiation dosimetry, quantification, and test-retest examination of [(18)F]PF-06684511
    Eur J Nucl Med Mol Imaging47, 2429-2439. PubMed  Europe PubMed DOI  L
  56. Durrant,C.S., Ruscher,K., Sheppard,O., Coleman,M.P. and Ozen,I.
    Beta secretase 1-dependent amyloid precursor protein processing promotes excessive vascular sprouting through NOTCH3 signalling
    Cell Death Dis11, 98-98. PubMed  Europe PubMed DOI  I
  57. Escamilla-Ayala,A.A., Sannerud,R., Mondin,M., Poersch,K., Vermeire,W., Paparelli,L., Berlage,C., Koenig,M., Chavez-Gutierrez,L., Ulbrich,M.H., Munck,S., Mizuno,H. and Annaert,W.
    Super-resolution microscopy reveals majorly mono- and dimeric presenilin1/gamma-secretase at the cell surface
    elife9, PubMed  Europe PubMed DOI
  58. Hampel,H., Vassar,R., De Strooper,B., Hardy,J., Willem,M., Singh,N., Zhou,J., Yan,R., Vanmechelen,E., de Vos,A., Nistico,R., Corbo,M., Imbimbo,B.P., Streffer,J., Voytyuk,I., Timmers,M., Tahami Monfared,A.A., Irizarry,M., Albala,B., Koyama,A., Watanabe,N., Kimura,T., Yarenis,L., Lista,S., Kramer,L. and Vergallo,A.
    The beta-secretase BACE1 in Alzheimer's disease
    Biol Psychiatry PubMed  Europe PubMed DOI
  59. Jagtap,A.D., Kondekar,N.B., Hung,P.Y., Hsieh,C.E., Yang,C.R., Chen,G.S. and Chern,J.W.
    4-Substituted 2-amino-3,4-dihydroquinazolines with a 3-hairpin turn side chain as novel inhibitors of BACE-1
    Bioorg Chem95, 103135-103135. PubMed  Europe PubMed DOI  I
  60. Jain,P., Wadhwa,P.K. and Jadhav,H.R.
    Design, Synthesis and Evaluation of 2,4,6-substituted Pyrimidine Derivatives as BACE-1 inhibitor: Plausible lead for Alzheimer's Disease
    Med Chem PubMed  Europe PubMed DOI  I
  61. Jepsen,W.M., De Both,M., Siniard,A.L., Ramsey,K., Piras,I.S., Naymik,M., Henderson,A. and Huentelman,M.J.
    Adenosine triphosphate Binding Cassette subfamily C member 1 (ABCC1) overexpression reduces APP processing and increases alpha- versus beta-secretase activity, in vitro
    Biol Open PubMed  Europe PubMed DOI
  62. Kumar,V., Ojha,P.K., Saha,A. and Roy,K.
    Exploring 2D-QSAR for prediction of beta-secretase 1 (BACE1) inhibitory activity against Alzheimer's disease
    SAR QSAR Environ Res31, 87-133. PubMed  Europe PubMed DOI  I
  63. Mori,T., Koyama,N., Yokoo,T., Segawa,T., Maeda,M., Sawmiller,D., Tan,J. and Town,T.
    Gallic Acid is a Dual alpha/beta-Secretase Modulator that Reverses Cognitive Impairment and Remediates Pathology in Alzheimer Mice
    J Biol Chem PubMed  Europe PubMed DOI
  64. Mouchlis,V.D., Melagraki,G., Zacharia,L.C. and Afantitis,A.
    Computer-aided drug design of beta-secretase, gamma-secretase and anti-tau inhibitors for the discovery of novel Alzheimer's therapeutics
    Int J Mol Sci21, PubMed  Europe PubMed DOI  I
  65. Mycroft-West,C.J., Devlin,A.J., Cooper,L.C., Procter,P., Miller,G.J., Fernig,D.G., Guerrini,M., Guimond,S.E., Lima,M.A., Yates,E.A. and Skidmore,M.A.
    Inhibition of BACE1, the beta-secretase implicated in Alzheimer's disease, by a chondroitin sulfate extract from Sardina pilchardus
    Neural Regen Res15, 1546-1553. PubMed  Europe PubMed DOI  I
  66. Ovsepian,S.V., Horacek,J., O'Leary,V.B. and Hoschl,C.
    The Ups and Downs of BACE1: Walking a Fine Line between Neurocognitive and Other Psychiatric Symptoms of Alzheimer's Disease
    Neuroscientist1073858420940943-1073858420940943. PubMed  Europe PubMed DOI
  67. Perrin,F., Papadopoulos,N., Suelves,N., Opsomer,R., Vadukul,D.M., Vrancx,C., Smith,S.O., Vertommen,D., Kienlen-Campard,P. and Constantinescu,S.N.
    Dimeric Transmembrane Orientations of APP/C99 Regulate gamma-Secretase Processing Line Impacting Signaling and Oligomerization
    iScience23, 101887-101887. PubMed  Europe PubMed DOI
  68. Peschiulli,A., Oehlrich,D., Rombouts,F., Vos,A. and Gijsen,H.J.
    3,3-Difluoro-3,4,5,6-tetrahydropyridin-2-amines: potent and permeable BACE-1 inhibitors
    Bioorg Med Chem Lett126999-126999. PubMed  Europe PubMed DOI  I
  69. Promyo,K., Iqbal,F., Chaidee,N. and Chetsawang,B.
    Aluminum chloride-induced amyloid beta accumulation and endoplasmic reticulum stress in rat brain are averted by melatonin
    Food Chem Toxicol146, 111829-111829. PubMed  Europe PubMed DOI  I
  70. Rahman,S.O., Kaundal,M., Salman,M., Shrivastava,A., Parvez,S., Panda,B.P., Akhter,M., Akhtar,M. and Najmi,A.K.
    Alogliptin reversed hippocampal insulin resistance in an amyloid-beta fibrils induced animal model of Alzheimer's disease
    Eur J Pharmacol173522-173522. PubMed  Europe PubMed DOI  I
  71. Resuello,D.L., Lirio,S.B., Porto,A.E., Macabeo,A.P.G., Huang,H.Y., Corpuz,M.J.T. and Villaflores,O.B.
    beta-Secretase 1 inhibitory activity and AMP-activated protein kinase activation of Callyspongia samarensis extracts
    Nat Prod Res34, 525-529. PubMed  Europe PubMed DOI  I
  72. Rudan Njavro,J., Klotz,J., Dislich,B., Wanngren,J., Shmueli,M.D., Herber,J., Kuhn,P.H., Kumar,R., Koeglsperger,T., Conrad,M., Wurst,W., Feederle,R., Vlachos,A., Michalakis,S., Jedlicka,P., Muller,S.A. and Lichtenthaler,S.F.
    Mouse brain proteomics establishes MDGA1 and CACHD1 as in vivo substrates of the Alzheimer protease BACE1
    FASEB J34, 2465-2482. PubMed  Europe PubMed DOI  P
  73. Sekine,Y., Lindborg,J.A. and Strittmatter,S.M.
    A proteolytic C-terminal fragment of Nogo-A (reticulon-4A) is released in exosomes and potently inhibits axon regeneration
    J Biol Chem295, 2175-2183. PubMed  Europe PubMed DOI
  74. Shah,H., Patel,A., Parikh,V., Nagani,A., Bhimani,B., Shah,U. and Bambharoliya,T.
    The beta-secretase enzyme BACE1: a biochemical enigma for Alzheimer's disease
    CNS Neurol Disord Drug Targets19, 184-194. PubMed  Europe PubMed DOI
  75. Sho,M., Ichiyanagi,N., Imaizumi,K., Ishikawa,M., Morimoto,S., Watanabe,H. and Okano,H.
    A combinational treatment of carotenoids decreases Abeta secretion in human neurons via beta-secretase inhibition
    Neurosci Res158, 47-55. PubMed  Europe PubMed DOI  I
  76. Tam,J.M., Josephson,L., Pilozzi,A.R. and Huang,X.
    A novel dual fluorochrome near-infrared imaging probe for potential Alzheimer's enzyme biomarkers-BACE1 and cathepsin D
    Molecules25, PubMed  Europe PubMed DOI  L
  77. Wang,B. and Ng,H.L.
    Deep neural network affinity model for BACE inhibitors in D3R Grand Challenge 4
    J Comput Aided Mol Des34, 201-217. PubMed  Europe PubMed DOI  I
  78. Wang,Y., Yang,J.Q., Hong,T.T., Sun,Y.H., Huang,H.L., Chen,F., Chen,X.J., Chen,H.Y., Dong,S.S., Cui,L.L. and Yang,T.L.
    RTN4B-mediated suppression of Sirtuin 2 activity ameliorates beta-amyloid pathology and cognitive impairment in Alzheimer's disease mouse model
    Aging Celle13194-e13194. PubMed  Europe PubMed DOI
  79. 2019
  80. Aathi,M. and Piramanayagam,S.
    From EST to structure models for functional inference of APP, BACE1, PSEN1, PSEN2 genes
    Bioinformation15, 760-771. PubMed  Europe PubMed DOI  I
  81. Anan,K., Iso,Y., Oguma,T., Nakahara,K., Suzuki,S., Yamamoto,T., Matsuoka,E., Ito,H., Sakaguchi,G., Ando,S., Morimoto,K., Kanegawa,N., Kido,Y., Kawachi,T., Fukushima,T., Teisman,A., Urmaliya,V., Dhuyvetter,D., Borghys,H., Austin,N., Van Den Bergh,A., Verboven,P., Bischoff,F., Gijsen,H.J.M., Yamano,Y. and Kusakabe,K.
    Trifluoromethyl dihydrothiazine-based beta-secretase (BACE1) inhibitors with robust central beta-amyloid reduction and minimal covalent binding burden
    ChemMedChem14, 1894-1910. PubMed  Europe PubMed DOI  I
  82. Bhaskar,V., Chowdary,R., Dixit,S.R. and Joshi,S.D.
    Synthesis, molecular modeling and BACE-1 inhibitory study of tetrahydrobenzo[b] pyran derivatives
    Bioorg Chem84, 202-210. PubMed  Europe PubMed DOI  I
  83. Blass,B.E.
    Tricyclic inhibitors of beta-secretase and their methods of use for the treatment of Alzheimer's disease
    ACS Med Chem Lett10, 8-9. PubMed  Europe PubMed DOI  I
  84. Das,B. and Yan,R.
    A close look at BACE1 inhibitors for Alzheimer's disease treatment
    CNS Drugs33, 251-263. PubMed  Europe PubMed DOI  I
  85. Das,S., Chakraborty,S. and Basu,S.
    Hybrid approach to sieve out natural compounds against dual targets in Alzheimer's disease
    Sci Rep9, 3714-3714. PubMed  Europe PubMed DOI  I
  86. Dierich,M., Hartmann,S., Dietrich,N., Moeser,P., Brede,F., Johnson Chacko,L., Tziridis,K., Schilling,A., Krauss,P., Hessler,S., Karch,S., Schrott-Fischer,A., Blumer,M., Birchmeier,C., Oliver,D., Moser,T., Schulze,H., Alzheimer,C., Leitner,M.G. and Huth,T.
    beta-secretase BACE1 is required for normal cochlear function
    J Neurosci39, 9013-9027. PubMed  Europe PubMed DOI  K  I
  87. Fan,T.Y., Wu,W.Y., Yu,S.P., Zhong,Y., Zhao,C., Chen,M., Li,H.M., Li,N.G., Chen,Z., Chen,S., Sun,Z.H., Duan,J.A. and Shi,Z.H.
    Design, synthesis and evaluation of 2-amino-imidazol-4-one derivatives as potent beta-site amyloid precursor protein cleaving enzyme 1 (BACE-1) inhibitors
    Bioorg Med Chem Lett29, 126772-126772. PubMed  Europe PubMed DOI  I
  88. Fang,W.S., Sun,D.Y., Yang,S., Cheng,C., Moschke,K., Li,T., Sun,S., Lichtenthaler,S.F., Huang,J. and Wang,Y.
    Discovery of a series of selective and cell permeable beta-secretase (BACE1) inhibitors by fragment linking with the assistance of STD-NMR
    Bioorg Chem92, 103253-103253. PubMed  Europe PubMed DOI  I
  89. Feng,F., Li,Y., Huang,N. and Luo,Y.
    Icaritin, an inhibitor of beta-site amyloid cleaving enzyme-1, inhibits secretion of amyloid precursor protein in APP-PS1-HEK293 cells by impeding the amyloidogenic pathway
    PeerJ7, e8219-e8219. PubMed  Europe PubMed DOI  I
  90. Ghosh,A.K., Brindisi,M., Yen,Y.C., Lendy,E.K., Kovela,S., Cardenas,E.L., Reddy,B.S., Rao,K.V., Downs,D., Huang,X., Tang,J. and Mesecar,A.D.
    Highly selective and potent human beta-secretase 2 (BACE2) inhibitors against type 2 diabetes: design, synthesis, X-ray structure and structure-activity relationship studies
    ChemMedChem14, 545-560. PubMed  Europe PubMed DOI  S  I
  91. Ion,G.N.D., Mihai,D.P., Lupascu,G. and Nitulescu,G.M.
    Application of molecular framework-based data-mining method in the search for beta-secretase 1 inhibitors through drug repurposing
    J Biomol Struct Dyn37, 3674-3685. PubMed  Europe PubMed DOI  I
  92. Islam,M.A. and Pillay,T.S.
    beta-Secretase inhibitors for Alzheimer's disease: identification using pharmacoinformatics
    J Biomol Struct Dyn37, 503-522. PubMed  Europe PubMed DOI  I
  93. Joseph,O.A., Babatomiwa,K., Niyi,A., Olaposi,O. and Olumide,I.
    Molecular docking and 3D QSAR studies of C000000956 as a potent inhibitor of BACE-1
    Drug Res (Stuttg)69, 451-457. PubMed  Europe PubMed DOI  I
  94. Lazic,D., Sagare,A.P., Nikolakopoulou,A.M., Griffin,J.H., Vassar,R. and Zlokovic,B.V.
    3K3A-Activated protein C blocks amyloidogenic BACE1 pathway and improves functional outcome in mice
    J Exp Med216, 279-293. PubMed  Europe PubMed DOI
  95. Li,J., Li,J., Sun,T., Cai,C., Shao,M. and Yu,G.
    Concise chemoenzymatic synthesis of heparan sulfate analogues as potent BACE-1 inhibitors
    Carbohydr Polym217, 232-239. PubMed  Europe PubMed DOI  I
  96. Liu,L., Ding,L., Rovere,M., Wolfe,M.S. and Selkoe,D.J.
    A cellular complex of BACE1 and gamma-secretase sequentially generates Abeta from its full-length precursor
    J Cell Biol218, 644-663. PubMed  Europe PubMed DOI
  97. Liu,L., Lauro,B.M., Ding,L., Rovere,M., Wolfe,M.S. and Selkoe,D.J.
    Multiple BACE1 inhibitors abnormally increase the BACE1 protein level in neurons by prolonging its half-life
    Alzheimers Dement15, 1183-1194. PubMed  Europe PubMed DOI  I
  98. Maia,M.A. and Sousa,E.
    BACE-1 and gamma-secretase as therapeutic targets for Alzheimer's disease
    Pharmaceuticals (Basel)12, PubMed  Europe PubMed DOI  I
  99. Mycroft-West,C.J., Cooper,L.C., Devlin,A.J., Procter,P., Guimond,S.E., Guerrini,M., Fernig,D.G., Lima,M.A., Yates,E.A. and Skidmore,M.A.
    A glycosaminoglycan extract from Portunus pelagicus inhibits BACE1, the beta secretase implicated in Alzheimer's disease
    Mar Drugs17, PubMed  Europe PubMed DOI
  100. Narang,S.S., Goyal,D. and Goyal,B.
    Molecular insights into the inhibitory mechanism of bi-functional bis-tryptoline triazole against beta-secretase (BACE1) enzyme
    Amino Acids51, 1593-1607. PubMed  Europe PubMed DOI  I
  101. Oehlrich,D., Peschiulli,A., Tresadern,G., Van Gool,M., Vega,J.A., De Lucas,A.I., Alonso De Diego,S.A., Prokopcova,H., Austin,N., Van Brandt,S., Surkyn,M., De Cleyn,M., Vos,A., Rombouts,F.J.R., Macdonald,G., Moechars,D., Gijsen,H.J.M. and Trabanco,A.A.
    Evaluation of a series of beta-secretase 1 inhibitors containing novel heteroaryl-fused-piperazine amidine warheads
    ACS Med Chem Lett10, 1159-1165. PubMed  Europe PubMed DOI  I
  102. Oguma,T., Anan,K., Suzuki,S., Hisakawa,S., Takada,A., Ogawa,M. and Kusakabe,K.I.
    Synthesis of a 6-CF3-substituted 2-amino-dihydro-1,3-thiazine beta-secretase inhibitor by N, N-diethylaminosulfur trifluoride-mediated chemoselective cyclization
    J Org Chem84, 4893-4897. PubMed  Europe PubMed DOI  I
  103. Panza,F., Lozupone,M., Watling,M. and Imbimbo,B.P.
    Do BACE inhibitor failures in Alzheimer patients challenge the amyloid hypothesis of the disease?
    Expert Rev Neurother19, 599-602. PubMed  Europe PubMed DOI  I
  104. Ponzoni,I., Sebastian-Perez,V., Martinez,M.J., Roca,C., De la Cruz Perez,C., Cravero,F., Vazquez,G.E., Paez,J.A., Diaz,M.F. and Campillo,N.E.
    QSAR Classification models for predicting the activity of inhibitors of beta-secretase (BACE1) associated with Alzheimer's disease
    Sci Rep9, 9102-9102. PubMed  Europe PubMed DOI  I
  105. Ribaudo,G., Coghi,P., Zanforlin,E., Law,B.Y.K., Wu,Y.Y.J., Han,Y., Qiu,A.C., Qu,Y.Q., Zagotto,G. and Wong,V.K.W.
    Semi-synthetic isoflavones as BACE-1 inhibitors against Alzheimer's disease
    Bioorg Chem87, 474-483. PubMed  Europe PubMed DOI  I
  106. Selkoe,D.
    beta-Secretase inhibitors for Alzheimer's disease: heading in the wrong direction?
    Lancet Neurol18, 624-626. PubMed  Europe PubMed DOI  I
  107. Tadano,G., Komano,K., Yoshida,S., Suzuki,S., Nakahara,K., Fuchino,K., Fujimoto,K., Matsuoka,E., Yamamoto,T., Asada,N., Ito,H., Sakaguchi,G., Kanegawa,N., Kido,Y., Ando,S., Fukushima,T., Teisman,A., Urmaliya,V., Dhuyvetter,D., Borghys,H., Van Den Bergh,A., Austin,N., Gijsen,H.J.M., Yamano,Y., Iso,Y. and Kusakabe,K.I.
    Discovery of an extremely potent thiazine-based beta-secretase inhibitor with reduced cardiovascular and liver toxicity at a low projected human dose
    J Med Chem62, 9331-9337. PubMed  Europe PubMed DOI  I
  108. Takano,A., Chen,L., Nag,S., Brodney,M.A., Arakawa,R., Chang,C., Amini,N., Doran,S.D., Dutra,J.K., McCarthy,T.J., Nolan,C.E., O'Neill,B.T., Villalobos,A., Zhang,L. and Halldin,C.
    Quantitative analysis of (18)F-PF-06684511, a novel PET radioligand for selective beta-secretase 1 imaging, in non-human primate brain
    J Nucl Med60, 992-997. PubMed  Europe PubMed DOI  L
  109. Yang,E.J., Lee,T. and Song,K.S.
    beta-Secretase inhibition by C-methylisoflavones from Abronia nana
    Nat Prod Res33, 1705-1712. PubMed  Europe PubMed DOI  I
  110. Zhu,B.L., Long,Y., Luo,W., Yan,Z., Lai,Y.J., Zhao,L.G., Zhou,W.H., Wang,Y.J., Shen,L.L., Liu,L., Deng,X.J., Wang,X.F., Sun,F. and Chen,G.J.
    MMP13 inhibition rescues cognitive decline in Alzheimer transgenic mice via BACE1 regulation
    Brain142, 176-192. PubMed  Europe PubMed DOI  I
  111. 2018
  112. Bao,J., Qin,M., Mahaman,Y.A.R., Zhang,B., Huang,F., Zeng,K., Xia,Y., Ke,D., Wang,Q., Liu,R., Wang,J.Z., Ye,K. and Wang,X.
    BACE1 SUMOylation increases its stability and escalates the protease activity in Alzheimer's disease
    Proc Natl Acad Sci U S A115, 3954-3959. PubMed  Europe PubMed DOI
  113. Bittner,H.J., Guixa-Gonzalez,R. and Hildebrand,P.W.
    Structural basis for the interaction of the beta-secretase with copper
    Biochim Biophys Acta1860, 1105-1113. PubMed  Europe PubMed DOI
  114. Campagna,J., Vadivel,K., Jagodzinska,B., Jun,M., Bilousova,T., Spilman,P. and John,V.
    Evaluation of an allosteric BACE inhibitor peptide to identify mimetics that can interact with the loop F region of the enzyme and prevent APP cleavage
    J Mol Biol430, 1566-1576. PubMed  Europe PubMed DOI  I
  115. Fuchino,K., Mitsuoka,Y., Masui,M., Kurose,N., Yoshida,S., Komano,K., Yamamoto,T., Ogawa,M., Unemura,C., Hosono,M., Ito,H., Sakaguchi,G., Ando,S., Ohnishi,S., Kido,Y., Fukushima,T., Miyajima,H., Hiroyama,S., Koyabu,K., Dhuyvetter,D., Borghys,H., Gijsen,H.J.M., Yamano,Y., Iso,Y. and Kusakabe,K.I.
    Rational design of novel 1,3-oxazine based beta-secretase (BACE1) inhibitors: incorporation of a double bond to reduce P-gp efflux leading to robust Abeta reduction in the brain
    J Med Chem61, 5122-5137. PubMed  Europe PubMed DOI  I
  116. Gabr,M.T. and Abdel-Raziq,M.S.
    Design and synthesis of donepezil analogues as dual AChE and BACE-1 inhibitors
    Bioorg Chem80, 245-252. PubMed  Europe PubMed DOI  I
  117. Gabr,M.T. and Abdel-Raziq,M.S.
    Structure-based design, synthesis, and evaluation of structurally rigid donepezil analogues as dual AChE and BACE-1 inhibitors
    Bioorg Med Chem Lett28, 2910-2913. PubMed  Europe PubMed DOI  I
  118. Gasse,C., Zaarour,M., Noppen,S., Abramov,M., Marliere,P., Liekens,S., De Strooper,B. and Herdewijn,P.
    Modulation of BACE1 activity by chemically modified aptamers
    Chembiochem19, 754-763. PubMed  Europe PubMed DOI  I
  119. Ghosh,A.K., Ghosh,K., Brindisi,M., Lendy,E.K., Yen,Y.C., Kumaragurubaran,N., Huang,X., Tang,J. and Mesecar,A.D.
    Design, synthesis, X-ray studies, and biological evaluation of novel BACE1 inhibitors with bicyclic isoxazoline carboxamides as the P3 ligand
    Bioorg Med Chem Lett28, 2605-2610. PubMed  Europe PubMed DOI  S  I
  120. Gijsen,H.J.M., Alonso De Diego,S.A., De Cleyn,M., Garcia-Molina,A., Macdonald,G.J., Martinez-Lamenca,C., Oehlrich,D., Prokopcova,H., Rombouts,F.J.R., Surkyn,M., Trabanco,A.A., Van Brandt,S., Van den Bossche,D., Van Gool,M., Austin,N., Borghys,H., Dhuyvetter,D. and Moechars,D.
    Optimization of 1,4-oxazine beta-secretase 1 (BACE1) inhibitors toward a clinical candidate
    J Med Chem61, 5292-5303. PubMed  Europe PubMed DOI  I
  121. Gueto-Tettay,C., Martinez-Consuegra,A., Pelaez-Bedoya,L. and Drosos-Ramirez,J.C.
    G-score: A function to solve the puzzle of modeling the protonation states of beta-secretase binding pocket
    J Mol Graph Model85, 1-12. PubMed  Europe PubMed DOI  I
  122. Gueto-Tettay,C., Pelaez-Bedoya,L. and Drosos-Ramirez,J.C.
    Population density analysis for determining the protonation state of the catalytic dyad in BACE1-tertiary carbinamine-based inhibitor complex
    J Biomol Struct Dyn36, 3557-3574. PubMed  Europe PubMed DOI  I
  123. Hosen,S.M.Z., Rubayed,M., Dash,R., Junaid,M., Mitra,S., Alam,M.S. and Dey,R.
    Prospecting and structural insight into the binding of novel plant-derived molecules of Leea indica as inhibitors of BACE1
    Curr Pharm Des24, 3972-3979. PubMed  Europe PubMed DOI  I
  124. Johansson,P., Kaspersson,K., Gurrell,I.K., Back,E., Eketjall,S., Scott,C.W., Cebers,G., Thorne,P., McKenzie,M.J., Beaton,H., Davey,P., Kolmodin,K., Holenz,J., Duggan,M.E., Budd Haeberlein,S. and Burli,R.W.
    Toward beta-secretase-1 inhibitors with improved isoform selectivity
    J Med Chem61, 3491-3502. PubMed  Europe PubMed DOI  I
  125. Karch,S., Broichhagen,J., Schneider,J., Boning,D., Hartmann,S., Schmid,B., Tripal,P., Palmisano,R., Alzheimer,C., Johnsson,K. and Huth,T.
    A new fluorogenic small-molecule labeling tool for surface diffusion analysis and advanced fluorescence imaging of beta-site amyloid precursor protein (APP)-cleaving enzyme 1 based on silicone rhodamine: SiR-BACE1
    J Med Chem61, 6121-6139. PubMed  Europe PubMed DOI  L
  126. Lee,J., Samson,A.A.S. and Song,J.M.
    Inkjet printing-based beta-secretase fluorescence resonance energy transfer (FRET) assay for screening of potential beta-secretase inhibitors of Alzheimer's disease
    Anal Chim Acta1022, 89-95. PubMed  Europe PubMed DOI  A
  127. Low,J.D., Bartberger,M.D., Cheng,Y., Whittington,D., Xue,Q., Wood,S., Allen,J.R. and Minatti,A.E.
    Diastereoselective synthesis of fused cyclopropyl-3-amino-2,4-oxazine beta-amyloid cleaving enzyme (BACE) inhibitors and their biological evaluation
    Bioorg Med Chem Lett28, 1111-1115. PubMed  Europe PubMed DOI  I
  128. Luque Ruiz,I. and Gomez-Nieto,M.A.
    QSAR classification and regression models for beta-secretase inhibitors using relative distance matrices
    SAR QSAR Environ Res29, 355-383. PubMed  Europe PubMed DOI  I
  129. Machalkova,M., Schejbal,J., Glatz,Z. and Preisler,J.
    A label-free MALDI TOF MS-based method for studying the kinetics and inhibitor screening of the Alzheimer's disease drug target beta-secretase
    Anal Bioanal Chem410, 7441-7448. PubMed  Europe PubMed DOI  A
  130. Mermelstein,D.J., McCammon,J.A. and Walker,R.C.
    pH-Dependent conformational dynamics of beta-secretase 1: a molecular dynamics study
    J Mol Recognite2765-e2765. PubMed  Europe PubMed DOI
  131. Mondragon-Rodriguez,S., Gu,N., Manseau,F. and Williams,S.
    Alzheimer's transgenic model is characterized by very early brain network alterations and beta-CTF fragment accumulation: reversal by beta-secretase inhibition
    Front Cell Neurosci12, 121-121. PubMed  Europe PubMed DOI  I
  132. Nakahara,K., Fuchino,K., Komano,K., Asada,N., Tadano,G., Hasegawa,T., Yamamoto,T., Sako,Y., Ogawa,M., Unemura,C., Hosono,M., Ito,H., Sakaguchi,G., Ando,S., Ohnishi,S., Kido,Y., Fukushima,T., Dhuyvetter,D., Borghys,H., Gijsen,H.J.M., Yamano,Y., Iso,Y. and Kusakabe,K.I.
    Discovery of potent and centrally active 6-substituted 5-fluoro-1,3-dihydro-oxazine beta-secretase (BACE1) inhibitors via active conformation stabilization
    J Med Chem61, 5525-5546. PubMed  Europe PubMed DOI  I
  133. Neumann,U., Ufer,M., Jacobson,L.H., Rouzade-Dominguez,M.L., Huledal,G., Kolly,C., Luond,R.M., Machauer,R., Veenstra,S.J., Hurth,K., Rueeger,H., Tintelnot-Blomley,M., Staufenbiel,M., Shimshek,D.R., Perrot,L., Frieauff,W., Dubost,V., Schiller,H., Vogg,B., Beltz,K., Avrameas,A., Kretz,S., Pezous,N., Rondeau,J.M., Beckmann,N., Hartmann,A., Vormfelde,S., David,O.J., Galli,B., Ramos,R., Graf,A. and Lopez Lopez,C.
    The BACE-1 inhibitor CNP520 for prevention trials in Alzheimer's disease
    EMBO Mol Med10, e9316-e9316. PubMed  Europe PubMed DOI  I
  134. Panza,F., Lozupone,M., Solfrizzi,V., Sardone,R., Piccininni,C., Dibello,V., Stallone,R., Giannelli,G., Bellomo,A., Greco,A., Daniele,A., Seripa,D., Logroscino,G. and Imbimbo,B.P.
    BACE inhibitors in clinical development for the treatment of Alzheimer's disease
    Expert Rev Neurother18, 847-857. PubMed  Europe PubMed DOI  I
  135. Prati,F., Bottegoni,G., Bolognesi,M.L. and Cavalli,A.
    BACE-1 inhibitors: from recent single-target molecules to multitarget compounds for Alzheimer's disease
    J Med Chem61, 619-637. PubMed  Europe PubMed DOI  I
  136. Razzaghi-Asl,N., Karimi,A. and Ebadi,A.
    The potential of natural product vs neurodegenerative disorders: In silico study of artoflavanocoumarin as BACE-1 inhibitor
    Comput Biol Chem77, 307-317. PubMed  Europe PubMed DOI  I
  137. Sagar,S.R., Singh,D.P., Panchal,N.B., Das,R.D., Pandya,D.H., Sudarsanam,V., Nivsarkar,M. and Vasu,K.K.
    Thiazolyl-thiadiazines as beta site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitors and anti-inflammatory agents: multitarget-directed ligands for the efficient management of Alzheimer's disease
    ACS Chem Neurosci9, 1663-1679. PubMed  Europe PubMed DOI  I
  138. Shen,Y., Wang,H., Sun,Q., Yao,H., Keegan,A.P., Mullan,M., Wilson,J., Lista,S., Leyhe,T., Laske,C., Rujescu,D., Levey,A., Wallin,A., Blennow,K., Li,R. and Hampel,H.
    Increased plasma beta-secretase 1 may predict conversion to Alzheimer's disease dementia in individuals with mild cognitive impairment
    Biol Psychiatry83, 447-455. PubMed  Europe PubMed DOI
  139. Veenstra,S.J., Rueeger,H., Voegtle,M., Lueoend,R., Holzer,P., Hurth,K., Tintelnot-Blomley,M., Frederiksen,M., Rondeau,J.M., Jacobson,L., Staufenbiel,M., Neumann,U. and Machauer,R.
    Discovery of amino-1,4-oxazines as potent BACE-1 inhibitors
    Bioorg Med Chem Lett28, 2195-2200. PubMed  Europe PubMed DOI  I
  140. Volloch,V. and Rits,S.
    Results of beta secretase-inhibitor clinical trials support amyloid precursor protein-independent generation of beta amyloid in sporadic Alzheimer's disease
    Med Sci (Basel)6, PubMed  Europe PubMed DOI  I
  141. Zhang,L., Chen,L., Dutra,J.K., Beck,E.M., Nag,S., Takano,A., Amini,N., Arakawa,R., Brodney,M.A., Buzon,L.M., Doran,S.D., Lanyon,L.F., McCarthy,T.J., Bales,K.R., Nolan,C.E., O'Neill,B.T., Schildknegt,K., Halldin,C. and Villalobos,A.
    Identification of a novel positron emission tomography (PET) ligand for imaging beta-site amyloid precursor protein cleaving enzyme 1 (BACE-1) in brain
    J Med Chem61, 3296-3308. PubMed  Europe PubMed DOI  L
  142. Zhang,Z., Li,X.G., Wang,Z.H., Song,M., Yu,S.P., Kang,S.S., Liu,X., Zhang,Z., Xie,M., Liu,G.P., Wang,J.Z. and Ye,K.
    delta-Secretase-cleaved Tau stimulates Abeta production via upregulating STAT1-BACE1 signaling in Alzheimer's disease
    Mol Psychiatry26, 586-603. PubMed  Europe PubMed DOI
  143. Zhu,K., Peters,F., Filser,S. and Herms,J.
    Consequences of pharmacological BACE inhibition on synaptic structure and function
    Biol Psychiatry84, 478-487. PubMed  Europe PubMed DOI  I
  144. Zuo,X., Dai,H., Zhang,H., Liu,J., Ma,S. and Chen,X.
    A peptide-WS2 nanosheet based biosensing platform for determination of beta-secretase and screening of its inhibitors
    Analyst143, 4585-4591. PubMed  Europe PubMed DOI  A
  145. 2017
  146. Andrew,R.J., Fernandez,C.G., Stanley,M., Jiang,H., Nguyen,P., Rice,R.C., Buggia-Prevot,V., De Rossi,P., Vetrivel,K.S., Lamb,R., Argemi,A., Allaert,E.S., Rathbun,E.M., Krause,S.V., Wagner,S.L., Parent,A.T., Holtzman,D.M. and Thinakaran,G.
    Lack of BACE1 S-palmitoylation reduces amyloid burden and mitigates memory deficits in transgenic mouse models of Alzheimer's disease
    Proc Natl Acad Sci U S A114, E9665-E9665. PubMed  Europe PubMed DOI
  147. Blass,B.
    C5-C6 Carbocyclic-fused iminothiadiazine dioxides as BACE inhibitors, their compositions, and their use
    ACS Med Chem Lett8, 786-788. PubMed  Europe PubMed DOI  I
  148. Bueno,A.B., Agejas,J., Broughton,H., Dally,R., Durham,T.B., Espinosa,J.F., Gonzalez,R., Hahn,P.J., Marcos,A., Rodriguez,R., Sanz,G., Soriano,J.F., Timm,D., Vidal,P., Yang,H.C. and McCarthy,J.R.
    Optimization of hydroxyethylamine transition state isosteres as aspartic protease inhibitors by exploiting conformational preferences
    J Med Chem60, 9807-9820. PubMed  Europe PubMed DOI  I
  149. Butler,C.R., Ogilvie,K., Martinez-Alsina,L., Barreiro,G., Beck,E.M., Nolan,C.E., Atchison,K., Benvenuti,E., Buzon,L., Doran,S., Gonzales,C., Helal,C.J., Hou,X., Hsu,M.H., Johnson,E.F., Lapham,K., Lanyon,L., Parris,K., O'Neill,B.T., Riddell,D., Robshaw,A., Vajdos,F. and Brodney,M.A.
    Aminomethyl-derived beta secretase (BACE1) inhibitors: engaging Gly230 without an anilide functionality
    J Med Chem60, 386-402. PubMed  Europe PubMed DOI  I
  150. Cheron,N. and Shakhnovich,E.I.
    Effect of sampling on BACE-1 ligands binding free energy predictions via MM-PBSA calculations
    J Comput Chem38, 1941-1951. PubMed  Europe PubMed DOI
  151. Di Pietro,O., Juarez-Jimenez,J., Munoz-Torrero,D., Laughton,C.A. and Luque,F.J.
    Unveiling a novel transient druggable pocket in BACE-1 through molecular simulations: conformational analysis and binding mode of multisite inhibitors
    PLoS ONE12, e0177683-e0177683. PubMed  Europe PubMed DOI  I
  152. Ellis,C.R., Tsai,C.C., Lin,F.Y. and Shen,J.
    Conformational dynamics of cathepsin D and binding to a small-molecule BACE1 inhibitor
    J Comput Chem38, 1260-1269. PubMed  Europe PubMed DOI  I
  153. Ghosh,A.K., Brindisi,M., Yen,Y.C., Cardenas,E.L., Ella-Menye,J.R., Kumaragurubaran,N., Huang,X., Tang,J. and Mesecar,A.D.
    Design, synthesis, and X-ray structural studies of BACE-1 inhibitors containing substituted 2-oxopiperazines as P1'-P2' ligands
    Bioorg Med Chem Lett27, 2432-2438. PubMed  Europe PubMed DOI  S  I
  154. Gueto-Tettay,C., Martinez-Consuegra,A., Zuchniarz,J., Gueto-Tettay,L.R. and Drosos-Ramirez,J.C.
    A PM7 dynamic residue-ligand interactions energy landscape of the BACE1 inhibitory pathway by hydroxyethylamine compounds. Part I: The flap closure process
    J Mol Graph Model76, 274-288. PubMed  Europe PubMed DOI  I
  155. Harris,R.C., Tsai,C.C., Ellis,C.R. and Shen,J.
    Proton-coupled conformational allostery modulates the inhibitor selectivity for beta-secretase
    J Phys Chem Lett4832-4837. PubMed  Europe PubMed DOI  I
  156. Innocenti,R., Lenci,E., Menchi,G., Pupi,A. and Trabocchi,A.
    Design and synthesis of bicyclic acetals as beta secretase (BACE1) inhibitors
    Bioorg Med Chem25, 5077-5083. PubMed  Europe PubMed DOI  I
  157. Keranen,H., Perez-Benito,L., Ciordia,M., Delgado,F., Steinbrecher,T.B., Oehlrich,D., van Vlijmen,H.W., Trabanco,A.A. and Tresadern,G.
    Acylguanidine beta secretase 1 inhibitors: a combined experimental and free energy perturbation study
    J Chem Theory Comput13, 1439-1453. PubMed  Europe PubMed DOI  I
  158. Kumar,A., Srivastava,G. and Sharma,A.
    A physicochemical descriptor based method for effective and rapid screening of dual inhibitors against BACE-1 and GSK-3beta as targets for Alzheimer's disease
    Comput Biol Chem71, 1-9. PubMed  Europe PubMed DOI  I
  159. Kumar,A., Srivastava,G., Srivastava,S., Verma,S., Negi,A.S. and Sharma,A.
    Investigation of naphthofuran moiety as potential dual inhibitor against BACE-1 and GSK-3beta: molecular dynamics simulations, binding energy, and network analysis to identify first-in-class dual inhibitors against Alzheimer's disease
    J Mol Model23, 239-239. PubMed  Europe PubMed DOI  I
  160. Liebsch,F., Aurousseau,M.R.P., Bethge,T., McGuire,H., Scolari,S., Herrmann,A., Blunck,R., Bowie,D. and Multhaup,G.
    Full-length cellular beta-secretase has a trimeric subunit stoichiometry, and its sulfur-rich transmembrane interaction site modulates cytosolic copper compartmentalization
    J Biol Chem292, 13258-13270. PubMed  Europe PubMed DOI
  161. Liu,R., Liu,Y.C., Meng,J., Zhu,H. and Zhang,X.
    A microfluidics-based mobility shift assay to identify new inhibitors of beta-secretase for Alzheimer's disease
    Anal Bioanal Chem409, 6635-6642. PubMed  Europe PubMed DOI  A  I
  162. Low,J.D., Bartberger,M.D., Chen,K., Cheng,Y., Fielden,M.R., Gore,V., Hickman,D., Liu,Q., Allen Sickmier,E., Vargas,H.M., Werner,J., White,R.D., Whittington,D.A., Wood,S. and Minatti,A.E.
    Development of 2-aminooxazoline 3-azaxanthene beta-amyloid cleaving enzyme (BACE) inhibitors with improved selectivity against cathepsin D
    MedChemComm8, 1196-1206. PubMed  Europe PubMed DOI  I
  163. Marumoto,S., Okuno,Y. and Miyazawa,M.
    Inhibition of beta-secretase activity by monoterpenes, sesquiterpenes, and C13 norisoprenoids
    J Oleo Sci66, 851-855. PubMed  Europe PubMed DOI  I
  164. Palakurti,R. and Vadrevu,R.
    Pharmacophore based 3D-QSAR modeling, virtual screening and docking for identification of potential inhibitors of beta-secretase
    Comput Biol Chem68, 107-117. PubMed  Europe PubMed DOI  I
  165. Parenti,N., Del Grosso,A., Antoni,C., Cecchini,M., Corradetti,R., Pavone,F.S. and Calamai,M.
    Direct imaging of APP proteolysis in living cells
    PeerJ5, e3086-e3086. PubMed  Europe PubMed DOI  A  L
  166. Reminek,R., Slezackova,L., Schejbal,J. and Glatz,Z.
    Development and comprehensive comparison of two on-line capillary electrophoretic methods for beta-secretase inhibitor screening
    J Chromatogr A1518, 89-96. PubMed  Europe PubMed DOI  A  I
  167. Rombouts,F.J.R., Alexander,R., Cleiren,E., de Groot,A., Carpentier,M., Dijkmans,J., Fierens,K., Masure,S., Moechars,D., Palomino-Schatzlein,M., Pineda-Lucena,A., Trabanco,A.A., Van Glabbeek,D., Vos,A. and Tresadern,G.
    Fragment binding to beta-secretase 1 without catalytic aspartate interactions identified via orthogonal screening approaches
    ACS Omega2, 685-697. PubMed  Europe PubMed DOI  I
  168. Ruderisch,N., Schlatter,D., Kuglstatter,A., Guba,W., Huber,S., Cusulin,C., Benz,J., Rufer,A.C., Hoernschemeyer,J., Schweitzer,C., Bulau,T., Gartner,A., Hoffmann,E., Niewoehner,J., Patsch,C., Baumann,K., Loetscher,H., Kitas,E. and Freskgard,P.O.
    Potent and selective BACE-1 peptide inhibitors lower brain abeta levels mediated by brain shuttle transport
    EBioMedicine24, 76-92. PubMed  Europe PubMed DOI  I
  169. Sakamoto,K., Matsuki,S., Matsuguma,K., Yoshihara,T., Uchida,N., Azuma,F., Russell,M., Hughes,G., Haeberlein,S.B., Alexander,R.C., Eketjall,S. and Kugler,A.R.
    BACE1 Inhibitor Lanabecestat (AZD3293) in a phase 1 study of healthy Japanese subjects: pharmacokinetics and effects on plasma and cerebrospinal fluid Abeta peptides
    J Clin Pharmacol57, 1460-1471. PubMed  Europe PubMed DOI  I
  170. Schejbal,J., Slezackova,L., Reminek,R. and Glatz,Z.
    A capillary electrophoresis-mass spectrometry based method for the screening of beta-secretase inhibitors as potential Alzheimer's disease therapeutics
    J Chromatogr A1487, 235-241. PubMed  Europe PubMed DOI  A
  171. Yan,R.
    Physiological functions of the beta-site amyloid precursor protein cleaving enzyme 1 and 2
    Front Mol Neurosci10, 97-97. PubMed  Europe PubMed DOI
  172. Zhang,S., Lin,Z., Pu,Y., Zhang,Y., Zhang,L. and Zuo,Z.
    Comparative QSAR studies using HQSAR, CoMFA, and CoMSIA methods on cyclic sulfone hydroxyethylamines as BACE1 inhibitors
    Comput Biol Chem67, 38-47. PubMed  Europe PubMed DOI  I
  173. 2016
  174. Araki,W.
    Post-translational regulation of the beta-secretase BACE1
    Brain Res Bull126, 170-177. PubMed  Europe PubMed DOI  V
  175. Barao,S., Moechars,D., Lichtenthaler,S.F. and De Strooper,B.
    BACE1 physiological functions may limit its use as therapeutic target for Alzheimer's disease
    Trends Neurosci39, 158-169. PubMed  Europe PubMed DOI  V
  176. Ben Halima,S., Mishra,S., Raja,K.M., Willem,M., Baici,A., Simons,K., Brustle,O., Koch,P., Haass,C., Caflisch,A. and Rajendran,L.
    Specific inhibition of beta-secretase processing of the Alzheimer disease amyloid precursor protein
    Cell Rep14, 2127-2141. PubMed  Europe PubMed DOI  P  I
  177. Chon,S.H., Yang,E.J., Lee,T. and Song,K.S.
    beta-Secretase (BACE1) inhibitory and neuroprotective effects of p-terphenyls from Polyozellus multiplex
    Food Funct7, 3834-3842. PubMed  Europe PubMed DOI  I
  178. Fleck,D., Voss,M., Brankatschk,B., Giudici,C., Hampel,H., Schwenk,B., Edbauer,D., Fukumori,A., Steiner,H., Kremmer,E., Haug-Kroper,M., Rossner,M.J., Fluhrer,R., Willem,M. and Haass,C.
    Proteolytic processing of neuregulin 1 type III by three intramembrane-cleaving proteases
    J Biol Chem291, 318-333. PubMed  Europe PubMed DOI  P
  179. Gueto-Tettay,C., Zuchniarz,J., Fortich-Seca,Y., Gueto-Tettay,L.R. and Drosos-Ramirez,J.C.
    A molecular dynamics study of the BACE1 conformational change from apo to closed form induced by hydroxyethylamine derived compounds
    J Mol Graph Model70, 181-195. PubMed  Europe PubMed DOI
  180. Gueto-Tettay,C., Pestana-Nobles,R. and Drosos-Ramirez,J.C.
    Determination of the protonation state for the catalytic dyad in beta-secretase when bound to hydroxyethylamine transition state analogue inhibitors: a molecular dynamics simulation study
    J Mol Graph Model66, 155-167. PubMed  Europe PubMed DOI  I
  181. Huang,J., Zhu,Y., Sun,B., Yao,Y. and Liu,J.
    Determination of the protonation state of the Asp dyad: conventional molecular dynamics versus thermodynamic integration
    J Mol Model22, 58-58. PubMed  Europe PubMed DOI
  182. Jain,P., Wadhwa,P.K., Rohilla,S. and Jadhav,H.R.
    Rational design, synthesis and in vitro evaluation of allylidene hydrazinecarboximidamide derivatives as BACE-1 inhibitors
    Bioorg Med Chem Lett26, 33-37. PubMed  Europe PubMed DOI  I
  183. Jain,P., Wadhwa,P.K., Gunapati,S. and Jadhav,H.R.
    Design, synthesis and in vitro evaluation studies of sulfonyl-amino-acetamides as small molecule BACE-1 inhibitors
    Bioorg Med Chem24, 2567-2575. PubMed  Europe PubMed DOI  I
  184. Jordan,J.B., Whittington,D.A., Bartberger,M.D., Sickmier,E.A., Chen,K., Cheng,Y. and Judd,T.
    Fragment-linking approach using (19)F NMR spectroscopy to obtain highly potent and selective inhibitors of beta-secretase
    J Med Chem59, 3732-3749. PubMed  Europe PubMed DOI  I
  185. Ju,Y., Li,Z., Deng,Y., Tong,A., Zhou,L. and Luo,Y.
    Identification of novel BACE1 inhibitors by combination of pharmacophore modeling, structure-based design and in vitro assay
    Curr Comput Aided Drug Des12, 73-82. PubMed  Europe PubMed  I
  186. Kennedy,M.E., Stamford,A.W., Chen,X., Cox,K., Cumming,J.N., Dockendorf,M.F., Egan,M., Ereshefsky,L., Hodgson,R.A., Hyde,L.A., Jhee,S., Kleijn,H.J., Kuvelkar,R., Li,W., Mattson,B.A., Mei,H., Palcza,J., Scott,J.D., Tanen,M., Troyer,M.D., Tseng,J.L., Stone,J.A., Parker,E.M. and Forman,M.S.
    The BACE1 inhibitor verubecestat (MK-8931) reduces CNS beta-amyloid in animal models and in Alzheimer's disease patients
    Sci Transl Med8, 363ra150-363ra. PubMed  Europe PubMed DOI  I
  187. Kumalo,H.M., Bhakat,S. and Soliman,M.E.
    Investigation of flap flexibility of beta-secretase using molecular dynamic simulations
    J Biomol Struct Dyn34, 1008-1019. PubMed  Europe PubMed DOI
  188. Kumalo,H.M. and Soliman,M.E.
    A comparative molecular dynamics study on BACE1 and BACE2 flap flexibility
    J Recept Signal Transduct Res36, 505-514. PubMed  Europe PubMed DOI
  189. Lehnert,S., Hartmann,S., Hessler,S., Adelsberger,H., Huth,T. and Alzheimer,C.
    Ion channel regulation by beta-secretase BACE1 - enzymatic and non-enzymatic effects beyond Alzheimer's disease
    Channels (Austin)10, 365-378. PubMed  Europe PubMed DOI  V
  190. Li,H., Wang,M., Gong,Y.N. and Yan,A.
    Discrimination of active and weakly active human BACE1 inhibitors using self-organizing map and support vector machine
    Comb Chem High Throughput Screen19, 470-480. PubMed  Europe PubMed  I
  191. Mandal,M., Wu,Y., Misiaszek,J., Li,G., Buevich,A., Caldwell,J.P., Liu,X., Mazzola,R.D., Orth,P., Strickland,C., Voigt,J., Wang,H., Zhu,Z., Chen,X., Grzelak,M., Hyde,L.A., Kuvelkar,R., Leach,P.T., Terracina,G., Zhang,L., Zhang,Q., Michener,M.S., Smith,B., Cox,K., Grotz,D., Favreau,L., Mitra,K., Kazakevich,I., McKittrick,B.A., Greenlee,W., Kennedy,M.E., Parker,E.M., Cumming,J.N. and Stamford,A.W.
    Structure-based design of an iminoheterocyclic beta-site amyloid precursor protein cleaving enzyme (BACE) inhibitor that lowers central abeta in nonhuman primates
    J Med Chem59, 3231-3248. PubMed  Europe PubMed DOI  I
  192. Munro,K.M., Nash,A., Pigoni,M., Lichtenthaler,S.F. and Gunnersen,J.M.
    Functions of the Alzheimer's disease protease BACE1 at the synapse in the central nervous system
    J Mol Neurosci60, 305-315. PubMed  Europe PubMed DOI  I
  193. Nisha,C.M., Kumar,A., Nair,P., Gupta,N., Silakari,C., Tripathi,T. and Kumar,A.
    Molecular docking and in silico ADMET study reveals acylguanidine 7a as a potential inhibitor of beta-secretase
    Adv Bioinformatics2016, 9258578-9258578. PubMed  Europe PubMed DOI  I
  194. Paul,T.J., Barman,A., Ozbil,M., Bora,R.P., Zhang,T., Sharma,G., Hoffmann,Z. and Prabhakar,R.
    Mechanisms of peptide hydrolysis by aspartyl and metalloproteases
    Phys Chem Chem Phys18, 24790-24801. PubMed  Europe PubMed DOI
  195. Pigoni,M., Wanngren,J., Kuhn,P.H., Munro,K.M., Gunnersen,J.M., Takeshima,H., Feederle,R., Voytyuk,I., De Strooper,B., Levasseur,M.D., Hrupka,B.J., Muller,S.A. and Lichtenthaler,S.F.
    Seizure protein 6 and its homolog seizure 6-like protein are physiological substrates of BACE1 in neurons
    Mol Neurodegener11, 67-67. PubMed  Europe PubMed DOI
  196. Qu,F., Yang,M. and Rasooly,A.
    Dual signal amplification electrochemical biosensor for monitoring the activity and inhibition of the Alzheimer's related protease beta-secretase
    Anal Chem88, 10559-10565. PubMed  Europe PubMed DOI  A
  197. Sabbah,D.A. and Zhong,H.A.
    Modeling the protonation states of beta-secretase binding pocket by molecular dynamics simulations and docking studies
    J Mol Graph Model68, 206-215. PubMed  Europe PubMed DOI
  198. Scott,J.D., Li,S.W., Brunskill,A.P., Chen,X., Cox,K., Cumming,J.N., Forman,M., Gilbert,E.J., Hodgson,R.A., Hyde,L.A., Jiang,Q., Iserloh,U., Kazakevich,I., Kuvelkar,R., Mei,H., Meredith,J., Misiaszek,J., Orth,P., Rossiter,L.M., Slater,M., Stone,J., Strickland,C.O., Voigt,J.H., Wang,G., Wang,H., Wu,Y., Greenlee,W.J., Parker,E.M., Kennedy,M.E. and Stamford,A.W.
    Discovery of the 3-imino-1,2,4-thiadiazinane 1,1-dioxide derivative verubecestat (MK-8931)-a beta-site amyloid precursor protein cleaving enzyme 1 inhibitor for the treatment of Alzheimer's disease
    J Med Chem59, 10435-10450. PubMed  Europe PubMed DOI  I
  199. Shimshek,D.R., Jacobson,L.H., Kolly,C., Zamurovic,N., Balavenkatraman,K.K., Morawiec,L., Kreutzer,R., Schelle,J., Jucker,M., Bertschi,B., Theil,D., Heier,A., Bigot,K., Beltz,K., Machauer,R., Brzak,I., Perrot,L. and Neumann,U.
    Pharmacological BACE1 and BACE2 inhibition induces hair depigmentation by inhibiting PMEL17 processing in mice
    Sci Rep6, 21917-21917. PubMed  Europe PubMed DOI  I
  200. Shin,K.Y., Noh,S.-J., Park,C.H., Jeong,Y.H., Chang,K.-A., Yoo,J., Kim,H.J., Ha,S., Kim,H.-S., Park,H.-J., Lee,J.-H., Moon,C. and Suh,Y.-H.
    Dehydroevodiamine.HCl protects against memory impairment and cerebral amyloid-beta production in Tg2576 mice by acting as a beta-secretase inhibitor
    CNS Neurol Disord Drug Targets15, 935-944. PubMed  Europe PubMed DOI  I
  201. Wu,Y.J., Guernon,J., Rajamani,R., Toyn,J.H., Ahlijanian,M.K., Albright,C.F., Muckelbauer,J., Chang,C., Camac,D., Macor,J.E. and Thompson,L.A.
    Discovery of furo[2,3-d][1,3]thiazinamines as beta amyloid cleaving enzyme-1 (BACE1) inhibitors
    Bioorg Med Chem Lett26, 5729-5731. PubMed  Europe PubMed DOI  I
  202. Wu,Y.J., Guernon,J., Shi,J., Marcin,L., Higgins,M., Rajamani,R., Muckelbauer,J., Lewis,H., Chang,C., Camac,D., Toyn,J.H., Ahlijanian,M.K., Albright,C.F., Macor,J.E. and Thompson,L.A.
    Discovery of S3-truncated, C-6 heteroaryl substituted aminothiazine beta-site APP cleaving enzyme-1 (BACE1) inhibitors
    J Med Chem59, 8593-8600. PubMed  Europe PubMed DOI  I
  203. Wu,Y.J., Guernon,J., Yang,F., Snyder,L., Shi,J., Mcclure,A., Rajamani,R., Park,H., Ng,A., Lewis,H., Chang,C., Camac,D., Toyn,J.H., Ahlijanian,M.K., Albright,C.F., Macor,J.E. and Thompson,L.A.
    Targeting the BACE1 active site flap leads to a potent inhibitor that elicits robust brain Abeta reduction in rodents
    ACS Med Chem Lett7, 271-276. PubMed  Europe PubMed DOI  I
  204. Zuhl,A.M., Nolan,C.E., Brodney,M.A., Niessen,S., Atchison,K., Houle,C., Karanian,D.A., Ambroise,C., Brulet,J.W., Beck,E.M., Doran,S.D., O'Neill,B.T., Am Ende,C.W., Chang,C., Geoghegan,K.F., West,G.M., Judkins,J.C., Hou,X., Riddell,D.R. and Johnson,D.S.
    Chemoproteomic profiling reveals that cathepsin D off-target activity drives ocular toxicity of beta-secretase inhibitors
    Nat Commun7, 13042-13042. PubMed  Europe PubMed DOI  I
  205. 2015
  206. Al-Nadaf,A.H., Taha,M.O. and Aldal'in,H.K.
    Haloperidol inhibits memapsin 2: innovation by docking simulation and in vitro assay
    Pak J Pharm Sci28, 139-146. PubMed  Europe PubMed  I
  207. Barao,S., Gartner,A., Leyva-Diaz,E., Demyanenko,G., Munck,S., Vanhoutvin,T., Zhou,L., Schachner,M., Lopez-Bendito,G., Maness,P.F. and De Strooper,B.
    Antagonistic effects of BACE1 and APH1B-gamma-secretase control axonal guidance by regulating growth cone collapse
    Cell Rep12, 1367-1376. PubMed  Europe PubMed DOI
  208. Boy,K.M., Guernon,J.M., Wu,Y.J., Zhang,Y., Shi,J., Zhai,W., Zhu,S., Gerritz,S.W., Toyn,J.H., Meredith,J.E., Barten,D.M., Burton,C.R., Albright,C.F., Good,A.C., Grace,J.E., Lentz,K.A., Olson,R.E., Macor,J.E. and Thompson LA 3rd
    Macrocyclic prolinyl acyl guanidines as inhibitors of beta-secretase (BACE)
    Bioorg Med Chem Lett25, 5040-5047. PubMed  Europe PubMed DOI  I
  209. Butler,C.R., Brodney,M.A., Beck,E.M., Barreiro,G., Nolan,C.E., Pan,F., Vajdos,F., Parris,K., Varghese,A.H., Helal,C.J., Lira,R., Doran,S.D., Riddell,D.R., Buzon,L.M., Dutra,J.K., Martinez-Alsina,L.A., Ogilvie,K., Murray,J.C., Young,J.M., Atchison,K., Robshaw,A., Gonzales,C., Wang,J., Zhang,Y. and O'Neill,B.T.
    Discovery of a series of efficient, centrally efficacious BACE1 inhibitors through structure-based drug design
    J Med Chem58, 2678-2702. PubMed  Europe PubMed DOI  I
  210. Chakraborty,S. and Basu,S.
    Structural insight into the mechanism of amyloid precursor protein recognition by beta-secretase 1: A molecular dynamics study
    Biophys Chem202, 1-12. PubMed  Europe PubMed DOI
  211. Chen,J.J., Liu,Q., Yuan,C., Gore,V., Lopez,P., Ma,V., Amegadzie,A., Qian,W., Judd,T.C., Minatti,A.E., Brown,J., Cheng,Y., Xue,M., Zhong,W., Dineen,T.A., Epstein,O., Human,J., Kreiman,C., Marx,I., Weiss,M.M., Hitchcock,S.A., Powers,T.S., Chen,K., Wen,P.H., Whittington,D.A., Cheng,A.C., Bartberger,M.D., Hickman,D., Werner,J.A., Vargas,H.M., Everds,N.E., Vonderfecht,S.L., Dunn,R.T.2., Wood,S., Fremeau,R.T., Jr., White,R.D. and Patel,V.F.
    Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious beta-secretase inhibitors for the potential treatment of Alzheimer's disease
    Bioorg Med Chem Lett25, 767-774. PubMed  Europe PubMed DOI  I
  212. Cheng,Y., Brown,J., Judd,T.C., Lopez,P., Qian,W., Powers,T.S., Chen,J.J., Bartberger,M.D., Chen,K., Dunn RT 2nd, Epstein,O., Fremeau RT Jr, Harried,S., Hickman,D., Hitchcock,S.A., Luo,Y., Minatti,A.E., Patel,V.F., Vargas,H.M., Wahl,R.C., Weiss,M.M., Wen,P.H., White,R.D., Whittington,D.A., Zheng,X.M. and Wood,S.
    An orally available BACE1 inhibitor that affords robust CNS Abeta reduction without cardiovascular liabilities
    ACS Med Chem Lett6, 210-215. PubMed  Europe PubMed DOI  I
  213. Das,S., Chakraborty,S. and Basu,S.
    Fragment-based designing for the generation of novel leads against BACE1
    Cent Nerv Syst Agents Med Chem15, 52-64. PubMed  Europe PubMed  I
  214. Devi,L. and Ohno,M.
    A combination Alzheimer's therapy targeting BACE1 and neprilysin in 5XFAD transgenic mice
    Mol Brain8, 19- PubMed  Europe PubMed DOI
  215. Dislich,B., Wohlrab,F., Bachhuber,T., Muller,S.A., Kuhn,P.H., Hogl,S., Meyer-Luehmann,M. and Lichtenthaler,S.F.
    Label-free quantitative proteomics of mouse cerebrospinal fluid detects beta-site APP cleaving enzyme (BACE1) protease substrates in vivo
    Mol Cell Proteomics14, 2550-2563. PubMed  Europe PubMed DOI
  216. Dorresteijn,B., Rotman,M., Faber,D., Schravesande,R., Suidgeest,E., van der Weerd,L., van der Maarel,S.M., Verrips,C.T. and El Khattabi,M.
    Camelid heavy chain only antibody fragment domain against beta-site of amyloid precursor protein cleaving enzyme 1 inhibits beta-secretase activity in vitro and in vivo
    FEBS J282, 3618-3631. PubMed  Europe PubMed DOI
  217. Edraki,N., Firuzi,O., Fatahi,Y., Mahdavi,M., Asadi,M., Emami,S., Divsalar,K., Miri,R., Iraji,A., Khoshneviszadeh,M., Firoozpour,L., Shafiee,A. and Foroumadi,A.
    N-(2-(Piperazin-1-yl)phenyl)arylamide derivatives as beta-secretase (BACE1) inhibitors: simple synthesis by Ugi four-component reaction and biological evaluation
    Arch Pharm (Weinheim)348, 330-337. PubMed  Europe PubMed DOI  I
  218. Egbertson,M., McGaughey,G.B., Pitzenberger,S.M., Stauffer,S.R., Coburn,C.A., Stachel,S.J., Yang,W., Barrow,J.C., Neilson,L.A., McWherter,M., Perlow,D., Fahr,B., Munshi,S., Allison,T.J., Holloway,K., Selnick,H.G., Yang,Z., Swestock,J., Simon,A.J., Sankaranarayanan,S., Colussi,D., Tugusheva,K., Lai,M.T., Pietrak,B., Haugabook,S., Jin,L., Chen,I.W., Holahan,M., Stranieri-Michener,M., Cook,J.J., Vacca,J. and Graham,S.L.
    Methyl-substitution of an iminohydantoin spiropiperidine beta-secretase (BACE-1) inhibitor has a profound effect on its potency
    Bioorg Med Chem Lett25, 4812-4819. PubMed  Europe PubMed DOI  I
  219. Filser,S., Ovsepian,S.V., Masana,M., Blazquez-Llorca,L., Brandt Elvang,A., Volbracht,C., Muller,M.B., Jung,C.K. and Herms,J.
    Pharmacological inhibition of BACE1 impairs synaptic plasticity and cognitive functions
    Biol Psychiatry77, 729-739. PubMed  Europe PubMed DOI  I
  220. Ghosh,A.K. and Tang,J.
    Prospects of beta-secretase inhibitors for the treatment of Alzheimer's disease
    ChemMedChem10, 1463-1466. PubMed  Europe PubMed DOI  I
  221. Ghosh,A.K., Brindisi,M., Yen,Y.C., Xu,X., Huang,X., Devasamudram,T., Bilcer,G., Lei,H., Koelsch,G., Mesecar,A.D. and Tang,J.
    Structure-based design, synthesis and biological evaluation of novel beta-secretase inhibitors containing a pyrazole or thiazole moiety as the P3 ligand
    Bioorg Med Chem Lett25, 668-672. PubMed  Europe PubMed DOI  S  I
  222. Gunnarsson,A., Snijder,A., Hicks,J., Gunnarsson,J., Hook,F. and Geschwindner,S.
    Drug discovery at the single molecule level: inhibition-in-solution assay of membrane-reconstituted beta-secretase using single-molecule imaging
    Anal Chem87, 4100-4103. PubMed  Europe PubMed DOI
  223. Hattori,Y., Kobayashi,K., Deguchi,A., Nohara,Y., Akiyama,T., Teruya,K., Sanjoh,A., Nakagawa,A., Yamashita,E. and Akaji,K.
    Evaluation of transition-state mimics in a superior BACE1 cleavage sequence as peptide-mimetic BACE1 inhibitors
    Bioorg Med Chem23, 5626-5640. PubMed  Europe PubMed DOI  I
  224. Hu,J., Lin,T., Gao,Y., Xu,J., Jiang,C., Wang,G., Bu,G., Xu,H., Chen,H. and Zhang,Y.W.
    The resveratrol trimer miyabenol C inhibits beta-secretase activity and beta-amyloid generation
    PLoS ONE10, e0115973-e0115973. PubMed  Europe PubMed DOI  I
  225. Kim,M.O., Blachly,P.G. and McCammon,J.A.
    Conformational dynamics and binding free energies of inhibitors of BACE-1: from the perspective of protonation equilibria
    PLoS Comput Biol11, e1004341-e1004341. PubMed  Europe PubMed DOI  I
  226. Kizuka,Y., Kitazume,S., Fujinawa,R., Saito,T., Iwata,N., Saido,T.C., Nakano,M., Yamaguchi,Y., Hashimoto,Y., Staufenbiel,M., Hatsuta,H., Murayama,S., Manya,H., Endo,T. and Taniguchi,N.
    An aberrant sugar modification of BACE1 blocks its lysosomal targeting in Alzheimer's disease
    EMBO Mol Med7, 175-189. PubMed  Europe PubMed DOI
  227. MacLeod,R., Hillert,E.K., Cameron,R.T. and Baillie,G.S.
    The role and therapeutic targeting of alpha-, beta- and gamma-secretase in Alzheimer's disease
    Future Sci OA1, FSO11-FSO11. PubMed  Europe PubMed DOI
  228. May,P.C., Willis,B.A., Lowe,S.L., Dean,R.A., Monk,S.A., Cocke,P.J., Audia,J.E., Boggs,L.N., Borders,A.R., Brier,R.A., Calligaro,D.O., Day,T.A., Ereshefsky,L., Erickson,J.A., Gevorkyan,H., Gonzales,C.R., James,D.E., Jhee,S.S., Komjathy,S.F., Li,L., Lindstrom,T.D., Mathes,B.M., Martenyi,F., Sheehan,S.M., Stout,S.L., Timm,D.E., Vaught,G.M., Watson,B.M., Winneroski,L.L., Yang,Z. and Mergott,D.J.
    The potent BACE1 inhibitor LY2886721 elicits robust central Abeta pharmacodynamic responses in mice, dogs, and humans
    J Neurosci35, 1199-1210. PubMed  Europe PubMed DOI  I
  229. Miri,R., Firuzi,O., Razzaghi-Asl,N., Javidnia,K. and Edraki,N.
    Inhibitors of Alzheimer's BACE-1 with 3,5-bis-N-(aryl/heteroaryl) carbamoyl-4-aryl-1,4-dihydropyridine structure
    Arch Pharm Res38, 456-469. PubMed  Europe PubMed DOI  I
  230. Neumann,U., Rueeger,H., Machauer,R., Veenstra,S.J., Lueoend,R.M., Tintelnot-Blomley,M., Laue,G., Beltz,K., Vogg,B., Schmid,P., Frieauff,W., Shimshek,D.R., Staufenbiel,M. and Jacobson,L.H.
    A novel BACE inhibitor NB-360 shows a superior pharmacological profile and robust reduction of amyloid-beta and neuroinflammation in APP transgenic mice
    Mol Neurodegener10, 44-44. PubMed  Europe PubMed DOI  I
  231. Prati,F., De Simone,A., Bisignano,P., Armirotti,A., Summa,M., Pizzirani,D., Scarpelli,R., Perez,D.I., Andrisano,V., Perez-Castillo,A., Monti,B., Massenzio,F., Polito,L., Racchi,M., Favia,A.D., Bottegoni,G., Martinez,A., Bolognesi,M.L. and Cavalli,A.
    Multitarget drug discovery for Alzheimer's disease: triazinones as BACE-1 and GSK-3beta inhibitors
    Angew Chem Int Ed Engl54, 1578-1582. PubMed  Europe PubMed DOI  I
  232. Prati,F., De Simone,A., Armirotti,A., Summa,M., Pizzirani,D., Scarpelli,R., Bertozzi,S.M., Perez,D.I., Andrisano,V., Perez-Castillo,A., Monti,B., Massenzio,F., Polito,L., Racchi,M., Sabatino,P., Bottegoni,G., Martinez,A., Cavalli,A. and Bolognesi,M.L.
    3,4-Dihydro-1,3,5-triazin-2(1H)-ones as the first dual BACE-1/GSK-3beta fragment hits against Alzheimer's disease
    ACS Chem Neurosci6, 1665-1682. PubMed  Europe PubMed DOI  I
  233. Raj,N., Helen,A., Manoj,N., Harish,G., Thomas,V., Singh,S., Sehrawat,S., Seth,S., Nair,A.S., Grover,A. and Dhar,P.K.
    In silico study of peptide inhibitors against BACE 1
    Syst Synth Biol9, 67-72. PubMed  Europe PubMed DOI  I
  234. Rauf,A., Uddin,G., Khan,A., Siddiqui,B.S., Arfan,M., Dalvandi,K. and Hadda,T.B.
    Pistagremic acid, a novel beta-secretase enzyme (BACE1) inhibitor from Pistacia integerrima Stewart
    Nat Prod Res29, 1735-1738. PubMed  Europe PubMed DOI  I
  235. Rombouts,F.J., Tresadern,G., Delgado,O., Martinez-Lamenca,C., Van Gool,M., Garcia-Molina,A., Alonso De Diego,S.A., Oehlrich,D., Prokopcova,H., Alonso,J.M., Austin,N., Borghys,H., Van Brandt,S., Surkyn,M., De Cleyn,M., Vos,A., Alexander,R., Macdonald,G., Moechars,D., Gijsen,H. and Trabanco,A.A.
    1,4-Oxazine beta-secretase 1 (BACE1) inhibitors: from hit generation to orally bioavailable brain penetrant leads
    J Med Chem58, 8216-8235. PubMed  Europe PubMed DOI  I
  236. Sandgren,V., Belda,O., Kvarnstrom,I., Lindberg,J., Samuelsson,B. and Dahlgren,A.
    Design and synthesis of novel arylketo-containing P1-P3 linked macro-cyclic BACE-1 inhibitors
    Open Med Chem J9, 13-26. PubMed  Europe PubMed DOI  I
  237. Semighini,E.P.
    In silico design of beta-secretase inhibitors in Alzheimer's disease
    Chem Biol Drug Des86, 284-290. PubMed  Europe PubMed DOI  I
  238. Song,W.J., Son,M.Y., Lee,H.W., Seo,H., Kim,J.H. and Chung,S.H.
    Enhancement of BACE1 activity by p25/Cdk5-mediated phosphorylation in Alzheimer's disease
    PLoS ONE10, e0136950-e0136950. PubMed  Europe PubMed DOI
  239. Takahashi,R., Ma,S., Yue,Q., Kim-Kang,H., Yi,Y., Lyssikatos,J.P., Regal,K., Hunt,K.W., Kallan,N.C., Siu,M., Hop,C.E., Liu,X. and Khojasteh,S.C.
    Dose-dependent exposure and metabolism of GNE-892, a beta-secretase inhibitor, in monkeys: contributions by P450, AO, and P-gp
    Eur J Drug Metab Pharmacokinet40, 171-185. PubMed  Europe PubMed DOI  I
  240. Tian,Y.L., Lv,M., Li,J.J., Xu,T., Zhai,H.L. and Zhang,X.Y.
    Study on the active mechanism of beta-secretase inhibitors by molecular simulations
    Eur J Pharm Sci76, 138-148. PubMed  Europe PubMed DOI  I
  241. Vega-Hissi,E.G., Tosso,R., Enriz,R.D. and Gutierrez,L.J.
    Molecular insight into the interaction mechanisms of amino-2H-imidazole derivatives with BACE1 protease: a QM/MM and QTAIM study
    Int J Quantum Chem155, 389-397. DOI  I
  242. Vila-Real,H., Coelho,H., Rocha,J., Fernandes,A., Ventura,M.R., Maycock,C.D., Iranzo,O. and Simplicio,A.L.
    Peptidomimetic beta-secretase inhibitors comprising a sequence of amyloid-beta peptide for Alzheimer's disease
    J Med Chem58, 5408-5418. PubMed  Europe PubMed DOI  I
  243. Winneroski,L.L., Schiffler,M.A., Erickson,J.A., May,P.C., Monk,S.A., Timm,D.E., Audia,J.E., Beck,J.P., Boggs,L.N., Borders,A.R., Boyer,R.D., Brier,R.A., Hudziak,K.J., Klimkowski,V.J., Garcia Losada,P., Mathes,B.M., Stout,S.L., Watson,B.M. and Mergott,D.J.
    Preparation and biological evaluation of conformationally constrained BACE1 inhibitors
    Bioorg Med Chem23, 3260-3268. PubMed  Europe PubMed DOI  I
  244. Wolfe,M.S.
    Cutting in on a secretase pas de deux
    Cell Res25, 1091-1092. PubMed  Europe PubMed DOI
  245. Zhang,H., Gao,Y., Qiao,P.F., Zhao,F.L. and Yan,Y.
    PPAR-alpha agonist regulates amyloid-beta generation via inhibiting BACE-1 activity in human neuroblastoma SH-SY5Y cells transfected with APPswe gene
    Mol Cell Biochem408, 37-46. PubMed  Europe PubMed DOI  I
  246. 2014

  247. The BACE race is on
    Nat Rev Drug Discov13, 165-165. DOI  I
  248. Bajda,M., Jonczyk,J., Malawska,B. and Filipek,S.
    Application of computational methods for the design of BACE-1 inhibitors: validation of in silico modelling
    Int J Mol Sci15, 5128-5139. PubMed  Europe PubMed DOI  I
  249. Barman,A. and Prabhakar,R.
    Computational insights into substrate and site specificities, catalytic mechanism, and protonation states of the catalytic Asp dyad of beta-secretase
    Scientifica (Cairo)2014, 598728-598728. PubMed  Europe PubMed DOI
  250. Caldwell,J.P., Mazzola,R.D., Durkin,J., Chen,J., Chen,X., Favreau,L., Kennedy,M., Kuvelkar,R., Lee,J., McHugh,N., McKittrick,B., Orth,P., Stamford,A., Strickland,C., Voigt,J., Wang,L., Zhang,L., Zhang,Q. and Zhu,Z.
    Discovery of potent iminoheterocycle BACE1 inhibitors
    Bioorg Med Chem Lett24, 5455-5459. PubMed  Europe PubMed DOI  I
  251. Cruz,D.S. and Castilho,M.S.
    2D QSAR studies on series of human beta-secretase (BACE-1) inhibitors
    Med Chem10, 162-173. PubMed  Europe PubMed DOI  I
  252. Cully,M.
    Deal watch: Lilly buys back into the BACE race for Alzheimer's disease
    Nat Rev Drug Discov13, 804-804. PubMed  Europe PubMed DOI  I
  253. De Simone,A., Seidl,C., Santos,C.A. and Andrisano,V.
    Liquid chromatographic enzymatic studies with on-line beta-secretase immobilized enzyme reactor and 4-(4-dimethylaminophenylazo) benzoic acid/5-[(2-aminoethyl) amino] naphthalene-1-sulfonic acid peptide as fluorogenic substrate
    J Chromatogr B Analyt Technol Biomed Life Sci953-954, 108-114. PubMed  Europe PubMed DOI  A
  254. Dhanjal,J.K., Goyal,S., Sharma,S., Hamid,R. and Grover,A.
    Mechanistic insights into mode of action of potent natural antagonists of BACE-1 for checking Alzheimer's plaque pathology
    Biochem Biophys Res Commun443, 1054-1059. PubMed  Europe PubMed DOI  I
  255. Dineen,T.A., Chen,K., Cheng,A.C., Derakhchan,K., Epstein,O., Esmay,J., Hickman,D., Kreiman,C.E., Marx,I.E., Wahl,R.C., Wen,P.H., Weiss,M.M., Whittington,D.A., Wood,S., Fremeau RT Jr, White,R.D. and Patel,V.F.
    Inhibitors of beta-site amyloid precursor protein cleaving enzyme (BACE1): identification of (S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5'H-spiro[chromeno[ 2,3-b]pyridine-5,4'-oxazol]-2'-amine (AMG-8718)
    J Med Chem57, 9811-9831. PubMed  Europe PubMed DOI  I
  256. Ghosh,A.K. and Osswald,H.L.
    BACE1 (beta-secretase) inhibitors for the treatment of Alzheimer's disease
    Chem Soc Rev43, 6765-6813. PubMed  Europe PubMed DOI  I
  257. Gurjar,A.S., Andrisano,V., Simone,A.D. and Velingkar,V.S.
    Design, synthesis, in silico and in vitro screening of 1,2,4-thiadiazole analogues as non-peptide inhibitors of beta-secretase
    Bioorg Chem57, 90-98. PubMed  Europe PubMed DOI  I
  258. He,W., Hu,J., Xia,Y. and Yan,R.
    beta-Site amyloid precursor protein cleaving enzyme 1 (BACE1) regulates notch signaling by controlling the cleavage of Jagged 1 (Jag1) and Jagged 2 (Jag2) proteins
    J Biol Chem289, 20630-20637. PubMed  Europe PubMed DOI
  259. John,B.A., Meister,M., Banning,A. and Tikkanen,R.
    Flotillins bind to the dileucine sorting motif of beta-site amyloid precursor protein-cleaving enzyme 1 and influence its endosomal sorting
    FEBS J281, 2074-2087. PubMed  Europe PubMed DOI
  260. Kandalepas,P.C. and Vassar,R.
    The normal and pathologic roles of the Alzheimer's beta-secretase, BACE1
    Curr Alzheimer Res11, 441-449. PubMed  Europe PubMed DOI
  261. Lim,J.-H., Lee,B.R., Park,H.W., Hong,B.S., Lim,B.O. and Kim,Y.J.
    beta-Secretase (BACE1) purification by refolding method and complex with hispidin
    J Korean Chem Soc58, 553-559. DOI  E
  262. Liu,P., Niu,Y., Wang,C., Sun,Q., Zhai,Y., Yu,J., Sun,J., Xu,F., Yan,G., Huang,W., Liang,L. and Xu,P.
    4-Oxo-1,4-dihydro-quinoline-3-carboxamides as BACE-1 inhibitors: synthesis, biological evaluation and docking studies
    Eur J Med Chem79, 413-421. PubMed  Europe PubMed DOI  I
  263. Menting,K.W. and Claassen,J.A.
    beta-secretase inhibitor; a promising novel therapeutic drug in Alzheimer's disease
    Front Aging Neurosci6, 165-165. PubMed  Europe PubMed DOI  I
  264. Mirsafian,H., Mat Ripen,A., Merican,A.F. and Mohamad,S.B.
    Amino Acid Sequence and Structural Comparison of BACE1 and BACE2 Using Evolutionary Trace Method
    ScientificWorldJournal2014, 482463-482463. PubMed  Europe PubMed DOI
  265. Nordeman,P., Estrada,S., Odell,L.R., Larhed,M. and Antoni,G.
    (11)C-Labeling of a potent hydroxyethylamine BACE-1 inhibitor and evaluation in vitro and in vivo
    Nucl Med Biol41, 536-543. PubMed  Europe PubMed DOI  I
  266. Polgar,T. and Keseru,G.M.
    Structure-based beta-secretase (BACE1) inhibitors
    Curr Pharm Des20, 3373-3379. PubMed  Europe PubMed DOI  I
  267. Roos,K., Viklund,J., Meuller,J., Kaspersson,K. and Svensson,M.
    Potency prediction of beta-secretase (BACE-1) inhibitors using density functional methods
    J Chem Inf Model54, 818-825. PubMed  Europe PubMed DOI  I
  268. Thomas,A.A., Hunt,K.W., Volgraf,M., Watts,R.J., Liu,X., Vigers,G., Smith,D., Sammond,D., Tang,T.P., Rhodes,S.P., Metcalf,A.T., Brown,K.D., Otten,J.N., Burkard,M., Cox,A.A., Do,M.K., Dutcher,D., Rana,S., DeLisle,R.K., Regal,K., Wright,A.D., Groneberg,R., Scearce-Levie,K., Siu,M., Purkey,H.E., Lyssikatos,J.P. and Gunawardana,I.W.
    Discovery of 7-tetrahydropyran-2-yl chromans: beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid beta-protein (Abeta) in the central nervous system
    J Med Chem57, 878-902. PubMed  Europe PubMed DOI  I
  269. Thomas,A.A., Hunt,K.W., Newhouse,B., Watts,R.J., Liu,X., Vigers,G., Smith,D., Rhodes,S.P., Brown,K.D., Otten,J.N., Burkard,M., Cox,A.A., Geck Do,M.K., Dutcher,D., Rana,S., DeLisle,R.K., Regal,K., Wright,A.D., Groneberg,R., Liao,J., Scearce-Levie,K., Siu,M., Purkey,H.E. and Lyssikatos,J.P.
    8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors
    J Med Chem57, 10112-10129. PubMed  Europe PubMed DOI  I
  270. Vassar,R., Kuhn,P.H., Haass,C., Kennedy,M.E., Rajendran,L., Wong,P.C. and Lichtenthaler,S.F.
    Function, therapeutic potential and cell biology of BACE proteases: current status and future prospects
    J Neurochem130, 4-28. PubMed  Europe PubMed DOI  K
  271. Videira,R., Castanheira,P., Graos,M., Resende,R., Salgueiro,L., Faro,C. and Cavaleiro,C.
    Dose-dependent inhibition of BACE-1 by the monoterpenoid 2,3,4,4-tetramethyl-5-methylenecyclopent-2-enone in cellular and mouse models of Alzheimer's disease
    J Nat Prod77, 1275-1279. PubMed  Europe PubMed DOI  I
  272. Viklund,J., Kolmodin,K., Nordvall,G., Swahn,B.-M., Svensson,M., Gravenfors,Y. and Rahm,F.
    Creation of novel cores for beta-secretase (BACE-1) inhibitors: A multiparameter lead generation strategy
    ACS Med Chem Lett5, 440-445. PubMed  Europe PubMed DOI  I
  273. Volgraf,M., Chan,L., Huestis,M.P., Purkey,H.E., Burkard,M., Geck Do,M., Harris,J., Hunt,K.W., Liu,X., Lyssikatos,J.P., Rana,S., Thomas,A.A., Vigers,G.P. and Siu,M.
    Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors
    Bioorg Med Chem Lett24, 2477-2480. PubMed  Europe PubMed DOI  I
  274. Wang,D., Ge,B., Yang,S., Miao,H. and Ding,Y.
    Synthesis of aryl substituted quinones as beta-secretase inhibitors: ligand-free direct arylation of quinones with aryl halides
    Russ J Gen Chem84, 1615-1621. DOI  I
  275. Wang,X., Kim,J.R., Lee,S.B., Kim,Y.J., Jung,M.Y., Kwon,H.W. and Ahn,Y.J.
    Effects of curcuminoids identified in rhizomes of Curcuma longa on BACE-1 inhibitory and behavioral activity and lifespan of Alzheimer's disease Drosophila models
    BMC Complement Altern Med14, 88-88. PubMed  Europe PubMed DOI  I
  276. Wu,Q., Tang,Z.H., Peng,J., Liao,L., Pan,L.H., Wu,C.Y., Jiang,Z.S., Wang,G.X. and Liu,L.S.
    The dual behavior of PCSK9 in the regulation of apoptosis is crucial in Alzheimer's disease progression (Review)
    Biomed Rep2, 167-171. PubMed  Europe PubMed DOI  V
  277. Yan,R. and Vassar,R.
    Targeting the beta secretase BACE1 for Alzheimer's disease therapy
    Lancet Neurol13, 319-329. PubMed  Europe PubMed DOI  I
  278. 2013
  279. Abdel-Magid,A.F.
    beta-Secretase inhibitors for the treatment of Alzheimer's disease and Down's Syndrome
    ACS Med Chem Lett4, 578-579. PubMed  Europe PubMed DOI  I
  280. Andreoli,F., Doukara,A.L., Mehdid,M.A., Vanthuyne,N., Roussel,C., Dessolin,J. and Kraus,J.L.
    Novel phenyl(thio)ureas bearing (thio)oxothiazoline group as potential BACE-1 inhibitors: synthesis and biological evaluation
    J Enzyme Inhib Med Chem28, 153-162. PubMed  Europe PubMed DOI  I
  281. Barman,A. and Prabhakar,R.
    Elucidating the catalytic mechanism of beta-secretase (BACE1): A quantum mechanics/molecular mechanics (QM/MM) approach
    J Mol Graph Model40, 1-9. PubMed  Europe PubMed DOI
  282. Bowers,S., Xu,Y.Z., Yuan,S., Probst,G.D., Hom,R.K., Chan,W., Konradi,A.W., Sham,H.L., Zhu,Y.L., Beroza,P., Pan,H., Brecht,E., Yao,N., Lougheed,J., Tam,D., Ren,Z., Ruslim,L., Bova,M.P. and Artis,D.R.
    Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates
    Bioorg Med Chem Lett23, 2181-2186. PubMed  Europe PubMed DOI  I
  283. Butini,S., Gabellieri,E., Brindisi,M., Casagni,A., Guarino,E., Huleatt,P.B., Relitti,N., La Pietra,V., Marinelli,L., Giustiniano,M., Novellino,E., Campiani,G. and Gemma,S.
    Novel peptidomimetics as BACE-1 inhibitors: synthesis, molecular modeling, and biological studies
    Bioorg Med Chem Lett23, 85-89. PubMed  Europe PubMed DOI  I
  284. Butini,S., Brogi,S., Novellino,E., Campiani,G., Ghosh,A.K., Brindisi,M. and Gemma,S.
    The structural evolution of beta-secretase inhibitors: a focus on the development of small-molecule inhibitors
    Curr Top Med Chem13, 1787-1807. PubMed  Europe PubMed  I
  285. Cheng,X., Zhou,Y., Gu,W., Wu,J., Nie,A., Cheng,J., Zhou,J., Zhou,W. and Zhang,Y.
    The selective BACE1 inhibitor VIa reduces amyloid-beta production in cell and mouse models of Alzheimer's disease
    J Alzheimers Dis37, 823-834. PubMed  Europe PubMed DOI  I
  286. Cheret,C., Willem,M., Fricker,F.R., Wende,H., Wulf-Goldenberg,A., Tahirovic,S., Nave,K.A., Saftig,P., Haass,C., Garratt,A.N., Bennett,D.L. and Birchmeier,C.
    Bace1 and neuregulin-1 cooperate to control formation and maintenance of muscle spindles
    EMBO J32, 2015-2028. PubMed  Europe PubMed DOI
  287. De Simone,A., Mancini,F., Real Fernandez,F., Rovero,P., Bertucci,C. and Andrisano,V.
    Surface plasmon resonance, fluorescence, and circular dichroism studies for the characterization of the binding of BACE-1 inhibitors
    Anal Bioanal Chem405, 827-835. PubMed  Europe PubMed DOI  I
  288. De Simone,A., Mancini,F., Cosconati,S., Marinelli,L., La Pietra,V., Novellino,E. and Andrisano,V.
    Human recombinant beta-secretase immobilized enzyme reactor for fast hits' selection and characterization from a virtual screening library
    J Pharm Biomed Anal73, 131-134. PubMed  Europe PubMed DOI  I
  289. Deng,Y., Wang,Z., Wang,R., Zhang,X., Zhang,S., Wu,Y., Staufenbiel,M., Cai,F. and Song,W.
    Amyloid-beta protein (Abeta) Glu11 is the major beta-secretase site of beta-site amyloid-beta precursor protein-cleaving enzyme 1 (BACE1), and shifting the cleavage site to Abeta Asp1 contributes to Alzheimer pathogenesis
    Eur J Neurosci37, 1962-1969. PubMed  Europe PubMed DOI  P
  290. Descamps,O., Spilman,P., Zhang,Q., Libeu,C.P., Poksay,K., Gorostiza,O., Campagna,J., Jagodzinska,B., Bredesen,D.E. and John,V.
    AbetaPP-selective BACE inhibitors (ASBI): novel class of therapeutic agents for Alzheimer's disease
    J Alzheimers Dis37, 343-355. PubMed  Europe PubMed DOI  I
  291. Devi,L. and Ohno,M.
    Mechanisms that lessen benefits of beta-secretase reduction in a mouse model of Alzheimer's disease
    Transl Psychiatry3, e284-e284. PubMed  Europe PubMed DOI
  292. Dominguez,J.L., Villaverde,M.C. and Sussman,F.
    Effect of pH and ligand charge state on BACE-1 fragment docking performance
    J Comput Aided Mol Des27, 403-417. PubMed  Europe PubMed DOI  I
  293. Edraki,N., Firuzi,O., Foroumadi,A., Miri,R., Madadkar-Sobhani,A., Khoshneviszadeh,M. and Shafiee,A.
    Phenylimino-2H-chromen-3-carboxamide derivatives as novel small molecule inhibitors of beta-secretase (BACE1)
    Bioorg Med Chem21, 2396-2412. PubMed  Europe PubMed DOI  I
  294. Eketjall,S., Janson,J., Jeppsson,F., Svanhagen,A., Kolmodin,K., Gustavsson,S., Radesater,A.C., Eliason,K., Briem,S., Appelkvist,P., Niva,C., Berg,A.L., Karlstrom,S., Swahn,B.M. and Falting,J.
    AZ-4217: A high potency BACE inhibitor displaying acute central efficacy in different in vivo models and reduced amyloid deposition in Tg2576 mice
    J Neurosci33, 10075-10084. PubMed  Europe PubMed DOI  I
  295. Fernandez-Bachiller,M.I., Horatscheck,A., Lisurek,M. and Rademann,J.
    Alzheimer's disease: Identification and development of beta-secretase (BACE-1) binding fragments and inhibitors by dynamic ligation screening (DLS)
    ChemMedChem8, 1041-1056. PubMed  Europe PubMed DOI  A  I
  296. Ghemtio,L. and Muzet,N.
    Retrospective molecular docking study of WY-25105 ligand to beta-secretase and bias of the three-dimensional structure flexibility
    J Mol Model19, 2971-2979. PubMed  Europe PubMed DOI  I
  297. Ginman,T., Viklund,J., Malmstrom,J., Blid,J., Emond,R., Forsblom,R., Johansson,A., Kers,A., Lake,F., Sehgelmeble,F., Sterky,K.J., Bergh,M., Lindgren,A., Johansson,P., Jeppsson,F., Falting,J., Gravenfors,Y. and Rahm,F.
    Core refinement toward permeable beta-secretase (BACE-1) inhibitors with low hERG activity
    J Med Chem56, 4181-4205. PubMed  Europe PubMed DOI  I
  298. Hamada,Y.
    [Significance of quantum chemical interactions for medicinal science and design of beta-secretase inhibitors]
    Yakugaku Zasshi133, 1113-1120. PubMed  Europe PubMed DOI  I
  299. Hamada,Y. and Kiso,Y.
    Advances in the identification of beta-secretase inhibitors
    Expert Opin Drug Discov8, 709-731. PubMed  Europe PubMed DOI  I
  300. Hilpert,H., Guba,W., Woltering,T.J., Wostl,W., Pinard,E., Mauser,H., Mayweg,A.V., Rogers-Evans,M., Humm,R., Krummenacher,D., Muser,T., Schnider,C., Jacobsen,H., Ozmen,L., Bergadano,A., Banner,D.W., Hochstrasser,R., Kuglstatter,A., David-Pierson,P., Fischer,H., Polara,A. and Narquizian,R.
    beta-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease
    J Med Chem56, 3980-3995. PubMed  Europe PubMed DOI  I
  301. Hogl,S., van Bebber,F., Dislich,B., Kuhn,P.H., Haass,C., Schmid,B. and Lichtenthaler,S.F.
    Label-free quantitative analysis of the membrane proteome of Bace1 protease knock-out zebrafish brains
    Proteomics13, 1519-1527. PubMed  Europe PubMed DOI  K  P
  302. Holsinger,R.M., Goense,N., Bohorquez,J. and Strappe,P.
    Splice variants of the Alzheimer's disease beta-secretase, BACE1
    Neurogenetics14, 1-9. PubMed  Europe PubMed DOI  M
  303. Hu,X., Schlanger,R., He,W., Macklin,W.B. and Yan,R.
    Reversing hypomyelination in BACE1-null mice with Akt-DD overexpression
    FASEB J27, 1868-1873. PubMed  Europe PubMed DOI  K
  304. Hu,X., He,W., Luo,X., Tsubota,K.E. and Yan,R.
    BACE1 regulates hippocampal astrogenesis via the Jagged1-Notch pathway
    Cell Rep4, 40-49. PubMed  Europe PubMed DOI
  305. Huang,D., Liu,Y., Shi,B., Li,Y., Wang,G. and Liang,G.
    Comprehensive 3D-QSAR and binding mode of BACE-1 inhibitors using R-group search and molecular docking
    J Mol Graph Model45, 65-83. PubMed  Europe PubMed DOI  I
  306. Hunt,K.W., Cook,A.W., Watts,R.J., Clark,C.T., Vigers,G., Smith,D., Metcalf,A.T., Gunawardana,I.W., Burkard,M., Cox,A.A., Geck Do,M.K., Dutcher,D., Thomas,A.A., Rana,S., Kallan,N.C., DeLisle,R.K., Rizzi,J.P., Regal,K., Sammond,D., Groneberg,R., Siu,M., Purkey,H., Lyssikatos,J.P., Marlow,A., Liu,X. and Tang,T.P.
    Spirocyclic beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloid beta in a higher species
    J Med Chem56, 3379-3403. PubMed  Europe PubMed DOI
  307. Kashima,Y. and Miyazawa,M.
    Structure-activity relationships for bergenin analogues as beta-secretase (BACE1) inhibitors
    J Oleo Sci62, 391-401. PubMed  Europe PubMed DOI  I
  308. Lee,C.W., Lira,R., Dutra,J., Ogilvie,K., O'Neill,B.T., Brodney,M., Helal,C., Young,J., Lachapelle,E., Sakya,S. and Murray,J.C.
    Stereoselective synthesis of spiropiperidines as BACE-1 aspartyl protease inhibitors via late stage N-arylation of a 1,8-diazaspiro[4.5]dec-3-en-2-one pharmacophore
    J Org Chem78, 2661-2669. PubMed  Europe PubMed DOI  I
  309. Li,X., Hong,L., Coughlan,K., Wang,L., Cao,L. and Tang,J.
    Structure-activity relationship of memapsin 2: implications on physiological functions and Alzheimer's disease
    Acta Biochim Biophys Sin (Shanghai)45, 613-621. PubMed  Europe PubMed DOI  P
  310. Lindgren,A., Eklund,G., Turek,D., Malmquist,J., Swahn,B.M., Holenz,J., von Berg,S., Karlstrom,S. and Bueters,T.
    Biotransformation of two beta-secretase inhibitors including ring opening and contraction of a pyrimidine ring
    Drug Metab Dispos41, 1134-1147. PubMed  Europe PubMed DOI  I
  311. Liu,Z.H., Li,S.L., Liang,Z.B., Zhao,Y., Zhang,Y.L., Yang,Y.Q., Wang,M.J. and Li,F.
    Targeting beta-secretase with RNAi in neural stem cells for Alzheimer's disease therapy
    Neural Regen Res8, 3095-3106. PubMed  Europe PubMed DOI  K
  312. Mondal,K., Regnstrom,K., Morishige,W., Barbour,R., Probst,G., Xu,Y.Z., Artis,D.R., Yao,N., Beroza,P. and Bova,M.P.
    Thermodynamic and kinetic characterization of hydroxyethylamine beta-secretase-1 inhibitors
    Biochem Biophys Res Commun441, 291-296. PubMed  Europe PubMed DOI  I
  313. Mori,T., Koyama,N., Guillot-Sestier,M.V., Tan,J. and Town,T.
    Ferulic acid is a nutraceutical beta-secretase modulator that improves behavioral impairment and Alzheimer-like pathology in transgenic mice
    PLoS ONE8, e55774-e55774. PubMed  Europe PubMed DOI
  314. Munter,L.M., Sieg,H., Bethge,T., Liebsch,F., Bierkandt,F.S., Schleeger,M., Bittner,H.J., Heberle,J., Jakubowski,N., Hildebrand,P.W. and Multhaup,G.
    Model peptides uncover the role of the beta-secretase transmembrane sequence in metal ion mediated oligomerization
    J Am Chem Soc135, 19354-19361. PubMed  Europe PubMed DOI
  315. Muthusamy,K., Singh,K., Chinnasamy,S., Nagamani,S., Krishnasamy,G., Thiyagarajan,C., Premkumar,P. and Anusuyadevi,M.
    High throughput virtual screening and E-pharmacophore filtering in the discovery of new BACE-1 inhibitors
    Interdiscip Sci5, 119-126. PubMed  Europe PubMed DOI  I
  316. Ng,R.A., Sun,M., Bowers,S., Hom,R.K., Probst,G.D., John,V., Fang,L.Y., Maillard,M., Gailunas,A., Brogley,L., Neitz,R.J., Tung,J.S., Pleiss,M.A., Konradi,A.W., Sham,H.L., Dappen,M.S., Adler,M., Yao,N., Zmolek,W., Nakamura,D., Quinn,K.P., Sauer,J.M., Bova,M.P., Ruslim,L., Artis,D.R. and Yednock,T.A.
    Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: Prime side chromane-containing inhibitors
    Bioorg Med Chem Lett23, 4674-4679. PubMed  Europe PubMed DOI  I
  317. Palakurti,R., Sriram,D., Yogeeswari,P. and Vadrevu,R.
    Multiple e-pharmacophore modeling combined with high-throughput virtual screening and docking to identify potential inhibitors of beta- secretase(BACE1)
    Mol Inform32, 385-398. PubMed  Europe PubMed DOI  I
  318. Pandey,Y. and Gupta,S.P.
    Design of some new potent beta-secretase inhibitors based on QSAR and molecular modeling study on a series of hydroxyethylamine derivatives
    Lett Drug Des Discov10, 253-265.  I
  319. Pennington,L.D., Whittington,D.A., Bartberger,M.D., Jordan,S.R., Monenschein,H., Nguyen,T.T., Yang,B.H., Xue,Q.M., Vounatsos,F., Wahl,R.C., Chen,K., Wood,S., Citron,M., Patel,V.F., Hitchcock,S.A. and Zhong,W.
    Hydroxyethylamine-based inhibitors of BACE1: P(1)-P(3) macrocyclization can improve potency, selectivity, and cell activity
    Bioorg Med Chem Lett23, 4459-4464. PubMed  Europe PubMed DOI  I
  320. Razzaghi-Asl,N., Ebadi,A., Edraki,N., Shahabipour,S. and Miri,R.
    Fragment-based binding efficiency indices in bioactive molecular design: a computational approach to BACE-1 inhibitors
    Iran J Pharm Res12, 423-436. PubMed  Europe PubMed  I
  321. Razzaghi-Asl,N., Firuzi,O., Hemmateenejad,B., Javidnia,K., Edraki,N. and Miri,R.
    Design and synthesis of novel 3,5-bis-N-(aryl/heteroaryl) carbamoyl-4-aryl-1,4-dihydropyridines as small molecule BACE-1 inhibitors
    Bioorg Med Chem21, 6893-6909. PubMed  Europe PubMed DOI  I
  322. Rosse,G.
    Dihydrooxazines as inhibitors of BACE-1 or BACE-2
    ACS Med Chem Lett4, 433-434. PubMed  Europe PubMed DOI  I
  323. Rueeger,H., Lueoend,R., Machauer,R., Veenstra,S.J., Jacobson,L.H., Staufenbiel,M., Desrayaud,S., Rondeau,J.M., Mobitz,H. and Neumann,U.
    Discovery of cyclic sulfoxide hydroxyethylamines as potent and selective beta-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure based design and in vivo reduction of amyloid beta-peptides
    Bioorg Med Chem Lett23, 5300-5306. PubMed  Europe PubMed DOI  I
  324. Sachse,C.C., Kim,Y.H., Agsten,M., Huth,T., Alzheimer,C., Kovacs,D.M. and Kim,D.Y.
    BACE1 and presenilin/gamma-secretase regulate proteolytic processing of KCNE1 and 2, auxiliary subunits of voltage-gated potassium channels
    FASEB J27, 2458-2467. PubMed  Europe PubMed DOI
  325. Sai Madhukar,S., Solomon,A., Das,V., Anil Kumar,K. and Krupanidhi,S.
    In silico design of inhibitors for beta-secretase: Implications for Alzheimer's disease
    Curr Trends Biotechnol Pharm7, 558-566.  I
  326. Sandgren,V., Back,M., Kvarnstrom,I. and Dahlgren,A.
    Design and synthesis of hydroxyethylene-based BACE-1 inhibitors incorporating extended P1 substituents
    Open Med Chem J7, 1-15. PubMed  Europe PubMed DOI  I
  327. Saric,A., Brugge,L.Z., Muller-Pompalla,D., Rysiok,T., Ousson,S., Permanne,B., Quattropani,A., Busch,M., Beher,D. and Hussain,I.
    Development and characterization of a novel membrane assay for full-length BACE-1 at pH 6.0
    J Biomol Screen18, 277-285. PubMed  Europe PubMed DOI  A
  328. Shangguan,S., Wang,F., Liao,Y., Yu,H., Li,J., Huang,W., Hu,H., Yu,L., Hu,Y. and Sheng,R.
    Design, synthesis and evaluation of 3-(2-aminoheterocycle)-4-benzyloxyphenylbenzamide derivatives as BACE-1 inhibitors
    Molecules18, 3577-3594. PubMed  Europe PubMed DOI  I
  329. Southan,C. and Hancock,J.M.
    A tale of two drug targets: the evolutionary history of BACE1 and BACE2
    Front Genet4, 293-293. PubMed  Europe PubMed DOI
  330. Stamford,A. and Strickland,C.
    Inhibitors of BACE for treating Alzheimer's disease: a fragment-based drug discovery story
    Curr Opin Chem Biol17, 320-328. PubMed  Europe PubMed DOI  I
  331. Stutzer,I., Selevsek,N., Esterhazy,D., Schmidt,A., Aebersold,R. and Stoffel,M.
    Systematic proteomic analysis identifies beta-site amyloid precursor protein cleaving enzyme 2 and 1 (BACE2 and BACE1) substrates in pancreatic beta-cells
    J Biol Chem288, 10536-10547. PubMed  Europe PubMed DOI  P
  332. Wang,H., Li,R. and Shen,Y.
    beta-Secretase: its biology as a therapeutic target in diseases
    Trends Pharmacol Sci34, 215-225. PubMed  Europe PubMed DOI  V  T
  333. Woltering,T.J., Wostl,W., Hilpert,H., Rogers-Evans,M., Pinard,E., Mayweg,A., Gobel,M., Banner,D.W., Benz,J., Travagli,M., Pollastrini,M., Marconi,G., Gabellieri,E., Guba,W., Mauser,H., Andreini,M., Jacobsen,H., Power,E. and Narquizian,R.
    BACE1 inhibitors: a head group scan on a series of amides
    Bioorg Med Chem Lett23, 4239-4243. PubMed  Europe PubMed DOI  I
  334. Xu,Y.Z., Yuan,S., Bowers,S., Hom,R.K., Chan,W., Sham,H.L., Zhu,Y.L., Beroza,P., Pan,H., Brecht,E., Yao,N., Lougheed,J., Yan,J., Tam,D., Ren,Z., Ruslim,L., Bova,M.P. and Artis,D.R.
    Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors
    Bioorg Med Chem Lett23, 3075-3080. PubMed  Europe PubMed DOI  I
  335. Yonezawa,S., Fujiwara,K., Yamamoto,T., Hattori,K., Yamakawa,H., Muto,C., Hosono,M., Tanaka,Y., Nakano,T., Takemoto,H., Arisawa,M. and Shuto,S.
    Conformational restriction approach to beta-secretase (BACE1) inhibitors III: Effective investigation of the binding mode by combinational use of X-ray analysis, isothermal titration calorimetry and theoretical calculations
    Bioorg Med Chem21, 6506-6522. PubMed  Europe PubMed DOI  I
  336. Zou,Y., Li,L., Chen,W., Chen,T., Ma,L., Wang,X., Xiong,B., Xu,Y. and Shen,J.
    Virtual screening and structure-based discovery of indole acylguanidines as potent beta-secretase (BACE1) inhibitors
    Molecules18, 5706-5722. PubMed  Europe PubMed DOI  I
  337. 2012
  338. Barman,A. and Prabhakar,R.
    Protonation States of the Catalytic Dyad of beta-Secretase (BACE1) in the Presence of Chemically Diverse Inhibitors: A Molecular Docking Study
    J Chem Inf Model52, 1275-1287. PubMed  Europe PubMed DOI  I
  339. Brodney,M.A., Barreiro,G., Ogilvie,K., Hajos-Korcsok,E., Murray,J., Vajdos,F., Ambroise,C., Christoffersen,C., Fisher,K., Lanyon,L., Liu,J., Nolan,C.E., Withka,J.M., Borzilleri,K.A., Efremov,I., Oborski,C.E., Varghese,A. and O'Neill,B.T.
    Spirocyclic sulfamides as beta-secretase 1 (BACE-1) inhibitors for the treatment of Alzheimer's disease: utilization of structure based drug design, WaterMap, and CNS penetration studies to identify centrally efficacious inhibitors
    J Med Chem55, 9224-9239. PubMed  Europe PubMed DOI  I
  340. Cai,J., Qi,X., Kociok,N., Skosyrski,S., Emilio,A., Ruan,Q., Han,S., Liu,L., Chen,Z., Bowes Rickman,C., Golde,T., Grant,M.B., Saftig,P., Serneels,L., De Strooper,B., Joussen,A.M. and Boulton,M.E.
    beta-Secretase (BACE1) inhibition causes retinal pathology by vascular dysregulation and accumulation of age pigment
    EMBO Mol Med4, 980-991. PubMed  Europe PubMed DOI  K  I
  341. Cao,L., Rickenbacher,G.T., Rodriguez,S., Moulia,T.W. and Albers,M.W.
    The precision of axon targeting of mouse olfactory sensory neurons requires the BACE1 protease
    Sci Rep2, 231-231. PubMed  Europe PubMed DOI
  342. Cheng,X.R., Zhou,J.W., Zhou,Y., Cheng,J.P., Yang,R.F., Zhou,W.X., Zhang,Y.X. and Yun,L.H.
    The green tea polyphenol (2)-epigallocatechin-3-gallate (EGCG) is not a beta-secretase inhibitor
    Bioorg Med Chem Lett22, 1408-1414. PubMed  Europe PubMed DOI
  343. Chiriano,G., De Simone,A., Mancini,F., Perez,D.I., Cavalli,A., Bolognesi,M.L., Legname,G., Martinez,A., Andrisano,V., Carloni,P. and Roberti,M.
    A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: structure-based design, synthesis, and biological evaluation
    Eur J Med Chem48, 206-213. PubMed  Europe PubMed DOI  I
  344. Cumming,J.N., Smith,E.M., Wang,L., Misiaszek,J., Durkin,J., Pan,J., Iserloh,U., Wu,Y., Zhu,Z., Strickland,C., Voigt,J., Chen,X., Kennedy,M.E., Kuvelkar,R., Hyde,L.A., Cox,K., Favreau,L., Czarniecki,M.F., Greenlee,W.J., McKittrick,B.A., Parker,E.M. and Stamford,A.W.
    Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor
    Bioorg Med Chem Lett22, 2444-2449. PubMed  Europe PubMed DOI  I
  345. Devi,L. and Ohno,M.
    Mitochondrial dysfunction and accumulation of the beta-secretase-cleaved C-terminal fragment of APP in Alzheimer's disease transgenic mice
    Neurobiol Dis45, 417-424. PubMed  Europe PubMed DOI
  346. Dineen,T.A., Weiss,M.M., Williamson,T., Acton,P., Babu-Khan,S., Bartberger,M.D., Brown,J., Chen,K., Cheng,Y., Citron,M., Croghan,M.D., Dunn RT 2nd, Esmay,J., Graceffa,R.F., Harried,S.S., Hickman,D., Hitchcock,S.A., Horne,D.B., Huang,H., Imbeah-Ampiah,R., Judd,T., Kaller,M.R., Kreiman,C.R., La,D.S., Li,V., Lopez,P., Louie,S., Monenschein,H., Nguyen,T.T., Pennington,L.D., San Miguel,T., Sickmier,E.A., Vargas,H.M., Wahl,R.C., Wen,P.H., Whittington,D.A., Wood,S., Xue,Q., Yang,B.H., Patel,V.F. and Zhong,W.
    Design and synthesis of potent, orally efficacious hydroxyethylamine derived beta-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors
    J Med Chem55, 9025-9044. PubMed  Europe PubMed DOI  I
  347. Dislich,B. and Lichtenthaler,S.F.
    The membrane-bound aspartyl protease BACE1: molecular and functional properties in Alzheimer's disease and beyond
    Front Physiol3, 8-8. PubMed  Europe PubMed DOI  V
  348. Efremov,I.V., Vajdos,F.F., Borzilleri,K.A., Capetta,S., Chen,H., Dorff,P.H., Dutra,J.K., Goldstein,S.W., Mansour,M., McColl,A., Noell,S., Oborski,C.E., O'Connell,T.N., O'Sullivan,T.J., Pandit,J., Wang,H., Wei,B. and Withka,J.M.
    Discovery and optimization of a novel spiropyrrolidine inhibitor of beta-secretase (BACE1) through fragment-based drug design
    J Med Chem55, 9069-9088. PubMed  Europe PubMed DOI  I
  349. Esterhazy,D., Akpinar,P. and Stoffel,M.
    Tmem27 dimerization, deglycosylation, plasma membrane depletion, and the extracellular Phe-Phe motif are negative regulators of cleavage by Bace2
    Biol Chem393, 473-484. PubMed  Europe PubMed DOI
  350. Fisette,J.F., Montagna,D.R., Mihailescu,M.R. and Wolfe,M.S.
    A G-Rich Element Forms a G-Quadruplex and Regulates Bace1 mRNA Alternative Splicing
    J Neurochem121, 763-773. PubMed  Europe PubMed DOI  R
  351. Folk,D.S., Torosian,J.C., Hwang,S., McCafferty,D.G. and Franz,K.J.
    Monitoring beta-secretase activity in living cells with a membrane-anchored FRET probe
    Angew Chem Int Ed Engl51, 10795-10799. PubMed  Europe PubMed DOI  L
  352. Gerritz,S.W., Zhai,W., Shi,S., Zhu,S., Toyn,J.H., Meredith,J.E., Jr., Iben,L.G., Burton,C.R., Albright,C.F., Good,A.C., Tebben,A.J., Muckelbauer,J.K., Camac,D.M., Metzler,W., Cook,L.S., Padmanabha,R., Lentz,K.A., Sofia,M.J., Poss,M.A., Macor,J.E. and Thompson,L.A., III
    Acyl guanidine inhibitors of beta-secretase (BACE-1): optimization of a micromolar hit to a nanomolar lead via iterative solid- and solution-phase library synthesis
    J Med Chem55, 9208-9223. PubMed  Europe PubMed DOI  S  I
  353. Ghosh,A.K., Pandey,S., Gangarajula,S., Kulkarni,S., Xu,X., Rao,K.V., Huang,X. and Tang,J.
    Structure-based design, synthesis, and biological evaluation of dihydroquinazoline-derived potent beta-secretase inhibitors
    Bioorg Med Chem Lett22, 5460-5465. PubMed  Europe PubMed DOI  I
  354. Ghosh,A.K., Venkateswara Rao,K., Yadav,N.D., Anderson,D.D., Gavande,N., Huang,X., Terzyan,S. and Tang,J.
    Structure-based design of highly selective beta-secretase inhibitors: synthesis, biological evaluation, and protein-ligand X-ray crystal structure
    J Med Chem55, 9195-9207. PubMed  Europe PubMed DOI  S  I
  355. Ghosh,A.K., Brindisi,M. and Tang,J.
    Developing beta-secretase inhibitors for treatment of Alzheimer's disease
    J Neurochem120 Suppl 1, 71-83. PubMed  Europe PubMed DOI  V  I
  356. Gravenfors,Y., Viklund,J., Blid,J., Ginman,T., Karlstrom,S., Kihlstrom,J., Kolmodin,K., Lindstrom,J., von Berg,S., von Kieseritzky,F., Bogar,K., Slivo,C., Swahn,B.M., Olsson,L.L., Johansson,P., Eketjall,S., Falting,J., Jeppsson,F., Stromberg,K., Janson,J. and Rahm,F.
    New aminoimidazoles as beta-secretase (BACE-1) inhibitors showing amyloid-beta (Abeta) lowering in brain
    J Med Chem55, 9297-9311. PubMed  Europe PubMed DOI  I
  357. Hitt,B., Riordan,S.M., Kukreja,L., Eimer,W.A., Rajapaksha,T.W. and Vassar,R.
    beta-Site amyloid precursor protein (APP)-cleaving enzyme 1 (BACE1)-deficient mice exhibit a close homolog of L1 (CHL1) loss-of-function phenotype involving axon guidance defects
    J Biol Chem287, 38408-38425. PubMed  Europe PubMed DOI  K
  358. Huang,H., La,D.S., Cheng,A.C., Whittington,D.A., Patel,V.F., Chen,K., Dineen,T.A., Epstein,O., Graceffa,R., Hickman,D., Kiang,Y.H., Louie,S., Luo,Y., Wahl,R.C., Wen,P.H., Wood,S. and Fremeau,R.T., Jr.
    Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and CNS penetrable BACE inhibitors for the treatment of Alzheimer's disease
    J Med Chem55, 9156-9169. PubMed  Europe PubMed DOI  I
  359. Jeppsson,F., Eketjall,S., Janson,J., Karlstrom,S., Gustavsson,S., Olsson,L.L., Radesater,A.C., Ploeger,B., Cebers,G., Kolmodin,K., Swahn,B.M., von Berg,S., Bueters,T. and Falting,J.
    Discovery of AZD3839, a potent and selective BACE1 inhibitor clinical candidate for the treatment of Alzheimer disease
    J Biol Chem287, 41245-41257. PubMed  Europe PubMed DOI  I
  360. Kacker,P., Masetti,M., Mangold,M., Bottegoni,G. and Cavalli,A.
    Combining dyad protonation and active site plasticity in BACE-1 structure-based drug design
    J Chem Inf Model52, 1079-1085. PubMed  Europe PubMed DOI  I
  361. Kacker,P., Bottegoni,G. and Cavalli,A.
    Computational methods in the discovery and design of BACE-1 inhibitors
    Curr Med Chem19, 6095-6111. PubMed  Europe PubMed  I
  362. Kandalepas,P.C. and Vassar,R.
    Identification and biology of beta-secretase
    J Neurochem120 Suppl 1, 55-61. PubMed  Europe PubMed DOI  V
  363. Kang,J.E., Cho,J.K., Curtis-Long,M.J., Ryu,H.W., Kim,J.H., Kim,H.J., Yuk,H.J., Kim,D.W. and Park,K.H.
    Inhibitory evaluation of sulfonamide chalcones on beta-secretase and acylcholinesterase
    Molecules18, 140-153. PubMed  Europe PubMed DOI  I
  364. Kim,H.S., Youm,J.W., Moon,K.B., Ha,J.H., Kim,Y.H., Joung,H. and Jeon,J.H.
    Expression analysis of human beta-secretase in transgenic tomato fruits
    Protein Expr Purif82, 125-131. PubMed  Europe PubMed DOI  E
  365. Kumar,A.B., Anderson,J.M., Melendez,A.L. and Manetsch,R.
    Synthesis and structure-activity relationship studies of 1,3-disubstituted 2-propanols as BACE-1 inhibitors
    Bioorg Med Chem Lett22, 4740-4744. PubMed  Europe PubMed DOI  I
  366. Liu,Y., Zhang,W., Li,L., Salvador,L.A., Chen,T., Chen,W., Felsenstein,K.M., Ladd,T.B., Price,A.R., Golde,T.E., He,J., Xu,Y., Li,Y. and Luesch,H.
    Cyanobacterial peptides as a prototype for the design of potent beta-secretase inhibitors and the development of selective chemical probes for other aspartic proteases
    J Med Chem55, 10749-10765. PubMed  Europe PubMed DOI  I
  367. Lu,Q., Chen,W.Y., Zhu,Z.Y., Chen,J., Xu,Y.C., Kaewpet,M., Rukachaisirikul,V., Chen,L.L. and Shen,X.
    L655,240, acting as a competitive BACE1 inhibitor, efficiently decreases beta-amyloid peptide production in HEK293-APPswe cells
    Acta Pharmacol Sin33, 1459-1468. PubMed  Europe PubMed DOI  I
  368. Mandal,M., Zhu,Z.N., Cumming,J.N., Liu,X.X., Strickland,C., Mazzola,R.D., Caldwell,J.P., Leach,P., Grzelak,M., Hyde,L., Zhang,Q., Terracina,G., Zhang,L.L., Chen,X., Kuvelkar,R., Kennedy,M.E., Favreau,L., Cox,K., Orth,P., Buevich,A., Voig,J., Wang,H.W., Kazakevich,I., McKittrick,B.A., Greenlee,W., Parker,E.M. and Stamford,A.W.
    Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation
    J Med Chem55, 9331-9345. PubMed  Europe PubMed DOI  I
  369. Monenschein,H., Horne,D.B., Bartberger,M.D., Hitchcock,S.A., Nguyen,T.T., Patel,V.F., Pennington,L.D. and Zhong,W.
    Structure guided P1' modifications of HEA derived beta-secretase inhibitors for the treatment of Alzheimer's disease
    Bioorg Med Chem Lett22, 3607-3611. PubMed  Europe PubMed DOI  I
  370. Niu,Y., Ma,C., Jin,H., Xu,F., Gao,H., Liu,P., Li,Y., Wang,C., Yang,G. and Xu,P.
    The discovery of novel beta-secretase inhibitors: pharmacophore modeling, virtual screening, and docking studies
    Chem Biol Drug Des79, 972-980. PubMed  Europe PubMed DOI  I
  371. Razzaghi-Asl,N., Ebadi,A., Edraki,N., Mehdipour,A., Shahabipour,S. and Miri,R.
    Response surface methodology in docking study of small molecule BACE-1 inhibitors
    J Mol Model18, 4567-4576. PubMed  Europe PubMed DOI  I
  372. Rueeger,H., Lueoend,R., Rogel,O., Rondeau,J.M., Mobitz,H., Machauer,R., Jacobson,L., Staufenbiel,M., Desrayaud,S. and Neumann,U.
    Discovery of cyclic sulfone hydroxyethylamines as potent and selective beta-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure-based design and in vivo reduction of amyloid beta-peptides
    J Med Chem55, 3364-3386. PubMed  Europe PubMed DOI  I
  373. Sandgren,V., Agback,T., Johansson,P.O., Lindberg,J., Kvarnstrom,I., Samuelsson,B., Belda,O. and Dahlgren,A.
    Highly potent macrocyclic BACE-1 inhibitors incorporating a hydroxyethylamine core: design, synthesis and X-ray crystal structures of enzyme inhibitor complexes
    Bioorg Med Chem20, 4377-4389. PubMed  Europe PubMed DOI  I
  374. Sasaki,H., Kitoh,Y., Miki,K., Kinoshita,K., Koyama,K., Kaneda,M. and Takahashi,K.
    Structure-activity relationships of biflavonoids for beta-secretase (BACE-1) inhibitory activity
    Heterocycles85, 2749-2756. DOI  I
  375. Sathya,M., Premkumar,P., Karthick,C., Moorthi,P., Jayachandran,K.S. and Anusuyadevi,M.
    BACE1 in Alzheimer's disease
    Clin Chim Acta414, 171-178. PubMed  Europe PubMed DOI  V
  376. Sheean,P., Rout,M.K., Head,R.J. and Bennett,L.E.
    Modulation of in vitro activity of zymogenic and mature recombinant human beta-secretase by dietary plants
    FEBS J279, 1291-1305. PubMed  Europe PubMed DOI
  377. Stamford,A.W., Scott,J.D., Li,S.W., Babu,S., Tadesse,D., Hunter,R., Wu,Y., Misiaszek,J., Cumming,J.N., Gilbert,E.J., Huang,C., McKittrick,B.A., Hong,L., Guo,T., Zhu,Z., Strickland,C., Orth,P., Voigt,J.H., Kennedy,M.E., Chen,X., Kuvelkar,R., Hodgson,R., Hyde,L.A., Cox,K., Favreau,L., Parker,E.M. and Greenlee,W.J.
    Discovery of an orally available, brain penetrant BACE1 inhibitor that affords robust CNS Abeta reduction
    ACS Med Chem Lett3, 897-902. PubMed  Europe PubMed DOI  I
  378. Sund,C., Belda,O., Borkakoti,N., Lindberg,J., Derbyshire,D., Vrang,L., Hamelink,E., Hgren,C., Woestenenk,E., Wikstrom,K., Eneroth,A., Lindstrom,E. and Kalayanov,G.
    Design and synthesis of potent hydroxyethylamine (HEA) BACE-1 inhibitors carrying prime side 4,5,6,7-tetrahydrobenzazole and 4,5,6,7-tetrahydropyridinoazole templates
    Bioorg Med Chem Lett22, 6721-6727. PubMed  Europe PubMed DOI  I
  379. Swahn,B.M., Kolmodin,K., Karlstrom,S., von Berg,S., Soderman,P., Holenz,J., Berg,S., Lindstrom,J., Sundstrom,M., Turek,D., Kihlstrom,J., Slivo,C., Andersson,L., Pyring,D., Rotticci,D., Ohberg,L., Kers,A., Bogar,K., von Kieseritzky,F., Bergh,M., Olsson,L.L., Janson,J., Eketjall,S., Georgievska,B., Jeppsson,F. and Falting,J.
    Design and synthesis of beta-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors with in vivo brain reduction of beta-amyloid peptides
    J Med Chem55, 9346-9361. PubMed  Europe PubMed DOI  I
  380. Swahn,B.M., Holenz,J., Kihlstrom,J., Kolmodin,K., Lindstrom,J., Plobeck,N., Rotticci,D., Sehgelmeble,F., Sundstrom,M., Berg,S., Falting,J., Georgievska,B., Gustavsson,S., Neelissen,J., Ek,M., Olsson,L.L. and Berg,S.
    Aminoimidazoles as BACE-1 inhibitors: the challenge to achieve in vivo brain efficacy
    Bioorg Med Chem Lett22, 1854-1859. PubMed  Europe PubMed DOI  S  I
  381. Tamayev,R., Matsuda,S. and D'Adamio,L.
    beta - but not gamma-secretase proteolysis of APP causes synaptic and memory deficits in a mouse model of dementia
    Mol Neurodegener7 Suppl 1, L9-L9.
  382. Tang,J. and Koelsch,G.
    Memapsin 2
    [ISSN:978-0-12-407744-7]3, 87-93. DOI
  383. Vassar,R.
    BACE1, the Alzheimer's beta-secretase enzyme, in health and disease
    Mol Neurodegener7 Suppl 1, L3-L3. DOI  V
  384. Velanac,V., Unterbarnscheidt,T., Hinrichs,W., Gummert,M.N., Fischer,T.M., Rossner,M.J., Trimarco,A., Brivio,V., Taveggia,C., Willem,M., Haass,C., Mobius,W., Nave,K.A. and Schwab,M.H.
    BACE1 processing of NRG1 type III produces a myelin-inducing signal but is not essential for the stimulation of myelination
    Glia60, 203-217. PubMed  Europe PubMed DOI
  385. Weiss,M.M., Williamson,T., Babu-Khan,S., Bartberger,M.D., Brown,J., Chen,K., Cheng,Y., Citron,M., Croghan,M.D., Dineen,T.A., Esmay,J., Graceffa,R.F., Harried,S.S., Hickman,D., Hitchcock,S.A., Horne,D.B., Huang,H., Imbeah-Ampiah,R., Judd,T., Kaller,M.R., Kreiman,C.R., La,D.S., Li,V., Lopez,P., Louie,S., Monenschein,H., Nguyen,T.T., Pennington,L.D., Rattan,C., San Miguel,T., Sickmier,E.A., Wahl,R.C., Wen,P.H., Wood,S., Xue,Q., Yang,B.H., Patel,V.F. and Zhong,W.
    Design and preparation of a potent series of hydroxyethylamine containing beta-secretase inhibitors that demonstrate robust reduction of central beta-amyloid
    J Med Chem55, 9009-9024. PubMed  Europe PubMed DOI  I
  386. Wyss,D.F., Wang,Y.S., Eaton,H.L., Strickland,C., Voigt,J.H., Zhu,Z. and Stamford,A.W.
    Combining NMR and X-ray crystallography in fragment-based drug discovery: discovery of highly potent and selective BACE-1 inhibitors
    Top Curr Chem317, 83-114. PubMed  Europe PubMed DOI  I
  387. Xu,Y., Li,M.J., Greenblatt,H., Chen,W., Paz,A., Dym,O., Peleg,Y., Chen,T., Shen,X., He,J., Jiang,H., Silman,I. and Sussman,J.L.
    Flexibility of the flap in the active site of BACE1 as revealed by crystal structures and molecular dynamics simulations
    Acta Crystallogr D Biol Crystallogr68, 13-25. PubMed  Europe PubMed DOI
  388. Yonezawa,S., Yamamoto,T., Yamakawa,H., Muto,C., Hosono,M., Hattori,K., Higashino,K., Yutsudo,T., Iwamoto,H., Kondo,Y., Sakagami,M., Togame,H., Tanaka,Y., Nakano,T., Takemoto,H., Arisawa,M. and Shuto,S.
    Conformational restriction approach to beta-secretase (BACE1) inhibitors: effect of a cyclopropane ring to induce an alternative binding mode
    J Med Chem55, 8838-8858. PubMed  Europe PubMed DOI  I
  389. Zhou,L., Barao,S., Laga,M., Bockstael,K., Borgers,M., Gijsen,H., Annaert,W., Moechars,D., Mercken,M., Gevaer,K. and De Strooper,B.
    The neural cell adhesion molecules L1 and CHL1 are cleaved by BACE1 protease in vivo
    J Biol Chem287, 25927-25940. PubMed  Europe PubMed DOI
  390. Zhu,Z.
    Iminoheterocycle as a druggable motif: BACE1 inhibitors and beyond
    Trends Pharmacol Sci33, 233-240. PubMed  Europe PubMed DOI  I
  391. 2011
  392. Al-Tel,T.H., Semreen,M.H., Al-Qawasmeh,R.A., Schmidt,M.F., El-Awadi,R., Ardah,M., Zaarour,R., Rao,S.N. and El-Agnaf,O.
    Design, synthesis, and qualitative structure-activity evaluations of novel beta-secretase inhibitors as potential Alzheimer's drug leads
    J Med Chem54, 8373-8385. PubMed  Europe PubMed DOI  I
  393. Barman,A., Schurer,S. and Prabhakar,R.
    Computational modeling of substrate specificity and catalysis of the beta-secretase (BACE1) enzyme
    Biochemistry50, 4337-4349. PubMed  Europe PubMed DOI
  394. Boy,K.M., Guernon,J.M., Shi,J., Toyn,J.H., Meredith,J.E., Barten,D.M., Burton,C.R., Albright,C.F., Marcinkeviciene,J., Good,A.C., Tebben,A.J., Muckelbauer,J.K., Camac,D.M., Lentz,K.A., Bronson,J.J., Olson,R.E., Macor,J.E. and Thompson,L.A., III
    Monosubstituted gamma-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of beta-secretase (BACE)
    Bioorg Med Chem Lett21, 6916-6924. PubMed  Europe PubMed DOI  I
  395. Chakraborty,S., Kumar,S. and Basu,S.
    Conformational transition in the substrate binding domain of beta-secretase exploited by NMA and its implication in inhibitor recognition: BACE1-myricetin a case study
    Neurochem Int58, 914-923. PubMed  Europe PubMed DOI  S  I
  396. Chang,W.P., Huang,X., Downs,D., Cirrito,J.R., Koelsch,G., Holtzman,D.M., Ghosh,A.K. and Tang,J.
    Beta-secretase inhibitor GRL-8234 rescues age-related cognitive decline in APP transgenic mice
    FASEB J25, 775-784. PubMed  Europe PubMed DOI  I
  397. Cheng,Y., Judd,T.C., Bartberger,M.D., Brown,J., Chen,K., Fremeau RT Jr, Hickman,D., Hitchcock,S.A., Jordan,B., Li,V., Lopez,P., Louie,S.W., Luo,Y., Michelsen,K., Nixey,T., Powers,T.S., Rattan,C., Sickmier,E.A., St Jean DJ Jr, Wahl,R.C., Wen,P.H. and Wood,S.
    From fragment screening to in vivo efficacy: optimization of a series of 2-aminoquinolines as potent inhibitors of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1)
    J Med Chem54, 5836-5857. PubMed  Europe PubMed DOI  I
  398. Evin,G., Lessene,G. and Wilkins,S.
    BACE Inhibitors as potential drugs for the treatment of Alzheimer's disease: focus on bioactivity
    Recent Pat CNS Drug Discov6, 91-106. PubMed  Europe PubMed DOI  V  I
  399. Farah,M.H., Pan,B.H., Hoffman,P.N., Ferraris,D., Tsukamoto,T., Nguyen,T., Wong,P.C., Price,D.L., Slusher,B.S. and Griffin,J.W.
    Reduced BACE1 Activity Enhances Clearance of Myelin Debris and Regeneration of Axons in the Injured Peripheral Nervous System
    J Neurosci31, 5744-5754. PubMed  Europe PubMed DOI  K
  400. Gueto-Tettay,C., Drosos,J.C. and Vivas-Reyes,R.
    Quantum mechanics study of the hydroxyethylamines-BACE-1 active site interaction energies
    J Comput Aided Mol Des25, 583-597. PubMed  Europe PubMed DOI  I
  401. Halima,S.B. and Rajendran,L.
    Membrane anchored and lipid raft targeted beta-secretase inhibitors for Alzheimer's disease therapy
    J Alzheimers Dis24 Suppl 2, 143-152. PubMed  Europe PubMed DOI  I
  402. Hogl,S., Kuhn,P.H., Colombo,A. and Lichtenthaler,S.F.
    Determination of the proteolytic cleavage sites of the amyloid precursor-like protein 2 by the proteases ADAM10, BACE1 and gamma-secretase
    PLoS ONE6, e21337-e21337. PubMed  Europe PubMed DOI  P
  403. John,S., Thangapandian,S., Sakkiah,S. and Lee,K.W.
    Potent BACE-1 inhibitor design using pharmacophore modeling, in silico screening and molecular docking studies
    BMC Bioinformatics12 Suppl 1, S28-S28. PubMed  Europe PubMed DOI  I
  404. Laws,S.M., Eckart,K., Friedrich,P., Kurz,A., Forstl,H. and Riemenschneider,M.
    Lack of evidence to support the association of polymorphisms within the alpha- and beta-secretase genes (ADAM10/BACE1) with Alzheimer's disease
    Neurobiol Aging32, 541-543. PubMed  Europe PubMed DOI  M
  405. Ma,L., Yang,Z., Li,C., Zhu,Z., Shen,X. and Hu,L.
    Design, synthesis and SAR study of hydroxychalcone inhibitors of human beta-secretase (BACE1)
    J Enzyme Inhib Med Chem26, 643-648. PubMed  Europe PubMed DOI  I
  406. Malamas,M.S., Erdei,J., Gunawan,I., Barnes,K., Hui,Y., Johnson,M., Robichaud,A., Zhou,P., Yan,Y., Solvibile,W., Turner,J., Fan,K.Y., Chopra,R., Bard,J. and Pangalos,M.N.
    New pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: exploring the S2' region
    Bioorg Med Chem Lett21, 5164-5170. PubMed  Europe PubMed DOI  I
  407. Mancini,F., De Simone,A. and Andrisano,V.
    Beta-secretase as a target for Alzheimer's disease drug discovery: an overview of in vitro methods for characterization of inhibitors
    Anal Bioanal Chem400, 1979-1996. PubMed  Europe PubMed DOI  I
  408. Marcin,L.R., Higgins,M.A., Zusi,F.C., Zhang,Y., Dee,M.F., Parker,M.F., Muckelbauer,J.K., Camac,D.M., Morin,P.E., Ramamurthy,V., Tebben,A.J., Lentz,K.A., Grace,J.E., Marcinkeviciene,J.A., Kopcho,L.M., Burton,C.R., Barten,D.M., Toyn,J.H., Meredith,J.E., Albright,C.F., Bronson,J.J., Macor,J.E. and Thompson,L.A.
    Synthesis and SAR of indole- and 7-azaindole-1,3-dicarboxamide hydroxyethylamine inhibitors of BACE-1
    Bioorg Med Chem Lett21, 537-541. PubMed  Europe PubMed DOI  I
  409. May,P.C., Dean,R.A., Lowe,S.L., Martenyi,F., Sheehan,S.M., Boggs,L.N., Monk,S.A., Mathes,B.M., Mergott,D.J., Watson,B.M., Stout,S.L., Timm,D.E., Smith Labell,E., Gonzales,C.R., Nakano,M., Jhee,S.S., Yen,M., Ereshefsky,L., Lindstrom,T.D., Calligaro,D.O., Cocke,P.J., Greg Hall,D., Friedrich,S., Citron,M. and Audia,J.E.
    Robust central reduction of amyloid-beta in humans with an orally available, non-peptidic beta-secretase inhibitor
    J Neurosci31, 16507-16516. PubMed  Europe PubMed DOI  I
  410. Mishra,S. and Caflisch,A.
    Dynamics in the active site of beta-secretase: a network analysis of atomistic simulations
    Biochemistry50, 9328-9339. PubMed  Europe PubMed DOI
  411. Nino,H., Garcia-Pintos,I., Rodriguez-Borges,J.E., Escobar-Cubiella,M., Garcia-Mera,X. and Prado-Prado,F.
    Review of synthesis, biological assay and QSAR studies of beta-secretase inhibitors
    Curr Comput Aided Drug Des7, 263-275. PubMed  Europe PubMed  V  I
  412. Prado-Prado,F., Escobar-Cubiella,M. and Garcia-Mera,X.
    Review of bioinformatics and QSAR studies of beta-secretase inhibitors
    Curr Bioinform6, 3-15.  V  I
  413. Rajapaksha,T.W., Eimer,W.A., Bozza,T.C. and Vassar,R.
    The Alzheimer's beta-secretase enzyme BACE1 is required for accurate axon guidance of olfactory sensory neurons and normal glomerulus formation in the olfactory bulb
    Mol Neurodegener6, 88-88. PubMed  Europe PubMed DOI  K
  414. Rueeger,H., Rondeau,J.M., McCarthy,C., Mobitz,H., Tintelnot-Blomley,M., Neumann,U. and Desrayaud,S.
    Structure based design, synthesis and SAR of cyclic hydroxyethylamine (HEA) BACE-1 inhibitors
    Bioorg Med Chem Lett21, 1942-1947. PubMed  Europe PubMed DOI  I
  415. Schechter,I. and Ziv,E.
    Cathepsins S, B and L with aminopeptidases display beta-secretase activity associated with the pathogenesis of Alzheimer's disease
    Biol Chem392, 555-569. PubMed  Europe PubMed DOI
  416. Sorribas,A., Jimenez,J.I., Yoshida,W.Y. and Williams,P.G.
    Daedalols A-C, fungal-derived BACE1 inhibitors
    Bioorg Med Chem19, 6581-6586. PubMed  Europe PubMed DOI  I
  417. Sussman,F., Otero,J.M., Villaverde,M.C., Castro,M., Dominguez,J.L., Gonzalez-Louro,L., Estevez,R.J. and Estevez,J.C.
    On a possible neutral charge state for the catalytic dyad in beta-secretase when bound to hydroxyethylene transition state analogue inhibitors
    J Med Chem54, 3081-3085. PubMed  Europe PubMed DOI  I
  418. Takahashi,T. and Miyazawa,M.
    Serotonin derivatives as inhibitors of beta-secretase (BACE 1)
    Pharmazie66, 301-305. PubMed  Europe PubMed DOI  I
  419. Thompson,L.A., Shi,J., Decicco,C.P., Tebben,A.J., Olson,R.E., Boy,K.M., Guernon,J.M., Good,A.C., Liauw,A., Zheng,C., Copeland,R.A., Combs,A.P., Trainor,G.L., Camac,D.M., Muckelbauer,J.K., Lentz,K.A., Grace,J.E., Burton,C.R., Toyn,J.H., Barten,D.M., Marcinkeviciene,J., Meredith,J.E., Albright,C.F. and Macor,J.E.
    Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors
    Bioorg Med Chem Lett21, 6909-6915. PubMed  Europe PubMed DOI  I
  420. Tresadern,G., Delgado,F., Delgado,O., Gijsen,H., Macdonald,G.J., Moechars,D., Rombouts,F., Alexander,R., Spurlino,J., Gool,M.V., Vega,J.A. and Trabanco,A.A.
    Rational design and synthesis of aminopiperazinones as beta-secretase (BACE) inhibitors
    Bioorg Med Chem Lett21, 7255-7260. PubMed  Europe PubMed DOI  I
  421. Vassar,R. and Kandalepas,P.C.
    The beta-secretase enzyme BACE1 as a therapeutic target for Alzheimer's disease
    Alzheimers Res Ther3, 20-20. PubMed  Europe PubMed DOI  V  T
  422. Wang,P., Zhao,Y., Zhu,P. and Fang,W.
    [Expression and purification of human beta-secretase (BACE1) in Pichia pastoris]
    Sheng Wu Gong Cheng Xue Bao27, 1655-1666. PubMed  Europe PubMed  E
  423. Wangsell,F., Nordeman,P., Savmarker,J., Emanuelsson,R., Jansson,K., Lindberg,J., Rosenquist,S., Samuelsson,B. and Larhed,M.
    Investigation of alpha-phenylnorstatine and alpha-benzylnorstatine as transition state isostere motifs in the search for new BACE-1 inhibitors
    Bioorg Med Chem19, 145-155. PubMed  Europe PubMed DOI  I
  424. Yi,H., Lee,S.J., Lee,J., Myung,C.S., Park,W.K., Lim,H.J., Lee,G.H., Kong,J.Y. and Cho,H.
    Sphingosylphosphorylcholine attenuated beta-amyloid production by reducing BACE1 expression and catalysis in PC12 cells
    Neurochem Res36, 2083-2090. PubMed  Europe PubMed DOI
  425. Zhi,P., Chia,C. and Gleeson,P.A.
    Intracellular trafficking of the beta-secretase and processing of amyloid precursor protein
    IUBMB Life63, 721-729. PubMed  Europe PubMed DOI
  426. Zhou,L., Chavez-Gutierrez,L., Bockstael,K., Sannerud,R., Annaert,W., May,P.C., Karran,E. and De Strooper,B.
    Inhibition of beta-secretase in vivo via antibody binding to unique loops (D and F) of BACE1
    J Biol Chem286, 8677-8687. PubMed  Europe PubMed DOI
  427. 2010
  428. Al-Nadaf,A., Abu Sheikha,G. and Taha,M.O.
    Elaborate ligand-based pharmacophore exploration and QSAR analysis guide the synthesis of novel pyridinium-based potent beta-secretase inhibitory leads
    Bioorg Med Chem18, 3088-3115. PubMed  Europe PubMed DOI  I
  429. Bertini,S., Ghilardi,E., Asso,V., Granchi,C., Minutolo,F. and Macchia,M.
    Biphenyl-derivatives possessing tertiary amino groups as beta-secretase (BACE1) inhibitors
    Lett Drug Des Discov7, 507-515. DOI  I
  430. Bjorklund,C., Adolfsson,H., Jansson,K., Lindberg,J., Vrang,L., Hallberg,A., Rosenquist,S. and Samuelsson,B.
    Discovery of potent BACE-1 inhibitors containing a new hydroxyethylene (HE) scaffold: exploration of P1' alkoxy residues and an aminoethylene (AE) central core
    Bioorg Med Chem18, 1711-1723. PubMed  Europe PubMed DOI  I
  431. Bjorklund,C., Oscarson,S., Benkestock,K., Borkakoti,N., Jansson,K., Lindberg,J., Vrang,L., Hallberg,A., Rosenquist,A. and Samuelsson,B.
    Design and synthesis of potent and selective BACE-1 inhibitors
    J Med Chem53, 1458-1464. PubMed  Europe PubMed DOI  I
  432. Choi,S.J., Cho,J.H., Im,I., Lee,S.D., Jang,J.Y., Oh,Y.M., Jung,Y.K., Jeon,E.S. and Kim,Y.C.
    Design and synthesis of 1,4-dihydropyridine derivatives as BACE-1 inhibitors
    Eur J Med Chem45, 2578-2590. PubMed  Europe PubMed DOI  I
  433. Clarke,B., Cutler,L., Demont,E., Dingwall,C., Dunsdon,R., Hawkins,J., Howes,C., Hussain,I., Maile,G., Matico,R., Mosley,J., Naylor,A., O'Brien,A., Redshaw,S., Rowland,P., Soleil,V., Smith,K.J., Sweitzer,S., Theobald,P., Vesey,D., Walter,D.S. and Wayne,G.
    BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296
    Bioorg Med Chem Lett20, 4639-4644. PubMed  Europe PubMed DOI  I
  434. Cumming,J., Babu,S., Huang,Y., Carrol,C., Chen,X., Favreau,L., Greenlee,W., Guo,T., Kennedy,M., Kuvelkar,R., Le,T., Li,G., McHugh,N., Orth,P., Ozgur,L., Parker,E., Saionz,K., Stamford,A., Strickland,C., Tadesse,D., Voigt,J., Zhang,L. and Zhang,Q.
    Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization
    Bioorg Med Chem Lett20, 2837-2842. PubMed  Europe PubMed DOI  S  I
  435. De Strooper,B., Vassar,R. and Golde,T.
    The secretases: enzymes with therapeutic potential in Alzheimer disease
    Nat Rev Neurol6, 99-107. PubMed  Europe PubMed DOI  I
  436. Dominguez,J.L., Christopeit,T., Villaverde,M.C., Gossas,T., Otero,J.M., Nystrom,S., Baraznenok,V., Lindstrom,E., Danielson,U.H. and Sussman,F.
    Effect of the protonation state of the titratable residues on the inhibitor affinity to BACE-1
    Biochemistry49, 7255-7263. PubMed  Europe PubMed DOI  I
  437. Evin,G., Barakat,A. and Masters,C.L.
    BACE: therapeutic target and potential biomarker for Alzheimer's disease
    Int J Biochem Cell Biol42, 1923-1926. PubMed  Europe PubMed DOI  K  V  T
  438. Fukumoto,H., Takahashi,H., Tarui,N., Matsui,J., Tomita,T., Hirode,M., Sagayama,M., Maeda,R., Kawamoto,M., Hirai,K., Terauchi,J., Sakura,Y., Kakihana,M., Kato,K., Iwatsubo,T. and Miyamoto,M.
    A noncompetitive BACE1 inhibitor TAK-070 ameliorates Abeta pathology and behavioral deficits in a mouse model of Alzheimer's disease
    J Neurosci30, 11157-11166. PubMed  Europe PubMed DOI  I
  439. Hanessian,S., Shao,Z., Betschart,C., Rondeau,J.M., Neumann,U. and Tintelnot-Blomley,M.
    Structure-based design and synthesis of novel P2/P3 modified, non-peptidic beta-secretase (BACE-1) inhibitors
    Bioorg Med Chem Lett20, 1924-1927. PubMed  Europe PubMed DOI  S  I
  440. Huang,W., Lv,D., Yu,H., Sheng,R., Kim,S.C., Wu,P., Luo,K., Li,J. and Hu,Y.
    Dual-target-directed 1,3-diphenylurea derivatives: BACE 1 inhibitor and metal chelator against Alzheimer's disease
    Bioorg Med Chem18, 5610-5615. PubMed  Europe PubMed DOI  I
  441. Huang,Y., Strobel,E.D., Ho,C.Y., Reynolds,C.H., Conway,K.A., Piesvaux,J.A., Brenneman,D.E., Yohrling,G.J., Moore Arnold,H., Rosenthal,D., Alexander,R.S., Tounge,B.A., Mercken,M., Vandermeeren,M., Parker,M.H., Reitz,A.B. and Baxter,E.W.
    Macrocyclic BACE inhibitors: optimization of a micromolar hit to nanomolar leads
    Bioorg Med Chem Lett20, 3158-3160. PubMed  Europe PubMed DOI  I
  442. Jiang,Y., Mullaney,K.A., Peterhoff,C.M., Che,S., Schmidt,S.D., Boyer-Boiteau,A., Ginsberg,S.D., Cataldo,A.M., Mathews,P.M. and Nixon,R.A.
    Alzheimer's-related endosome dysfunction in Down syndrome is Abeta-independent but requires APP and is reversed by BACE-1 inhibition
    Proc Natl Acad Sci U S A107, 1630-1635. PubMed  Europe PubMed DOI
  443. Jiaranaikulwanitch,J., Boonyarat,C., Fokin,V.V. and Vajragupta,O.
    Triazolyl tryptoline derivatives as beta-secretase inhibitors
    Bioorg Med Chem Lett20, 6572-6576. PubMed  Europe PubMed DOI  I
  444. Jin,S., Agerman,K., Kolmodin,K., Gustafsson,E., Dahlqvist,C., Jureus,A., Liu,G., Falting,J., Berg,S., Lundkvist,J. and Lendahl,U.
    Evidence for dimeric BACE-mediated APP processing
    Biochem Biophys Res Commun393, 21-27. PubMed  Europe PubMed DOI
  445. Kihara,T., Shimmyo,Y., Akaike,A., Niidome,T. and Sugimoto,H.
    Abeta-induced BACE-1 cleaves N-terminal sequence of mPGES-2
    Biochem Biophys Res Commun393, 728-733. PubMed  Europe PubMed DOI  P
  446. Klaver,D.W., Wilce,M.C., Cui,H., Hung,A.C., Gasperini,R., Foa,L. and Small,D.H.
    Is BACE1 a suitable therapeutic target for the treatment of Alzheimer's disease? Current strategies and future directions
    Biol Chem391, 849-859. PubMed  Europe PubMed DOI  I
  447. Klaver,D.W., Wilce,M.C., Gasperini,R., Freeman,C., Juliano,J.P., Parish,C., Foa,L., Aguilar,M.I. and Small,D.H.
    Glycosaminoglycan-induced activation of the beta-secretase (BACE1) of Alzheimer's disease
    J Neurochem112, 1552-1561. PubMed  Europe PubMed DOI
  448. Lerchner,A., Machauer,R., Betschart,C., Veenstra,S., Rueeger,H., McCarthy,C., Tintelnot-Blomley,M., Jaton,A.L., Rabe,S., Desrayaud,S., Enz,A., Staufenbiel,M., Paganetti,P., Rondeau,J.M. and Neumann,U.
    Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application
    Bioorg Med Chem Lett20, 603-607. PubMed  Europe PubMed DOI  I
  449. Li,X., Bo,H., Zhang,X.C., Hartsuck,J.A. and Tang,J.
    Predicting memapsin 2 (beta-secretase) hydrolytic activity
    Protein Sci19, 2175-2185. PubMed  Europe PubMed DOI  P
  450. Liu,S., Zhou,L.H., Wang,H.Q. and Yao,Z.B.
    Superimposing the 27 crystal protein/inhibitor complexes of beta-secretase to calculate the binding affinities by the linear interaction energy method
    Bioorg Med Chem Lett20, 6533-6537. PubMed  Europe PubMed DOI  S  I
  451. Liu,S., Wang,H., Zhou,L. and Yao,Z.
    Precise location of proton of beta-secretase for catalytic aspartates (Asp 32 and Asp 228) in Alzheimer's patients
    Neural Regen Res5, 572-578. DOI
  452. Madden,J., Dod,J.R., Godemann,R., Kraemer,J., Smith,M., Biniszkiewicz,M., Hallett,D.J., Barker,J., Dyekjaer,J.D. and Hesterkamp,T.
    Fragment-based discovery and optimization of BACE1 inhibitors
    Bioorg Med Chem Lett20, 5329-5333. PubMed  Europe PubMed DOI  I
  453. Malamas,M.S., Barnes,K., Hui,Y., Johnson,M., Lovering,F., Condon,J., Fobare,W., Solvibile,W., Turner,J., Hu,Y., Manas,E.S., Fan,K., Olland,A., Chopra,R., Bard,J., Pangalos,M.N., Reinhart,P. and Robichaud,A.J.
    Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors
    Bioorg Med Chem Lett20, 2068-2073. PubMed  Europe PubMed DOI  I
  454. Malamas,M.S., Erdei,J., Gunawan,I., Turner,J., Hu,Y., Wagner,E., Fan,K., Chopra,R., Olland,A., Bard,J., Jacobsen,S., Magolda,R.L., Pangalos,M. and Robichaud,A.J.
    Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors
    J Med Chem53, 1146-1158. PubMed  Europe PubMed DOI  I
  455. Malamas,M.S., Barnes,K., Johnson,M., Hui,Y., Zhou,P., Turner,J., Hu,Y., Wagner,E., Fan,K., Chopra,R., Olland,A., Bard,J., Pangalos,M., Reinhart,P. and Robichaud,A.J.
    Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors
    Bioorg Med Chem18, 630-639. PubMed  Europe PubMed DOI  I
  456. Malamas,M.S., Robichaud,A., Erdei,J., Quagliato,D., Solvibile,W., Zhou,P., Morris,K., Turner,J., Wagner,E., Fan,K., Olland,A., Jacobsen,S., Reinhart,P., Riddell,D. and Pangalos,M.
    Design and synthesis of aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors with enhanced brain permeability
    Bioorg Med Chem Lett20, 6597-6605. PubMed  Europe PubMed DOI  I
  457. Meredith,J.A., Bjorklund,C., Adolfsson,H., Jansson,K., Hallberg,A., Rosenquist,A. and Samuelsson,B.
    P2'-truncated BACE-1 inhibitors with a novel hydroxethylene-like core
    Eur J Med Chem45, 542-554. PubMed  Europe PubMed DOI  I
  458. Niu,Y., Wang,Y., Zou,X., Yang,X., Ma,C., Lu,Y., Zhou,B., Yuan,Y., Du,G. and Xu,P.
    Synthesis and preliminary evaluation of peptidomimetic inhibitors of human beta-secretase
    Eur J Med Chem45, 2089-2094. PubMed  Europe PubMed DOI  I
  459. Nowak,P., Cole,D.C., Aulabaugh,A., Bard,J., Chopra,R., Cowling,R., Fan,K.Y., Hu,B., Jacobsen,S., Jani,M., Jin,G., Lo,M.C., Malamas,M.S., Manas,E.S., Narasimhan,R., Reinhart,P., Robichaud,A.J., Stock,J.R., Subrath,J., Svenson,K., Turner,J., Wagner,E., Zhou,P. and Ellingboe,J.W.
    Discovery and initial optimization of 5,5'-disubstituted aminohydantoins as potent beta-secretase (BACE1) inhibitors
    Bioorg Med Chem Lett20, 632-635. PubMed  Europe PubMed DOI  I
  460. Pandey,A., Mungalpara,J. and Mohan,C.G.
    Comparative molecular field analysis and comparative molecular similarity indices analysis of hydroxyethylamine derivatives as selective human BACE-1 inhibitor
    Mol Divers14, 39-49. PubMed  Europe PubMed DOI  I
  461. Probst,G.D., Bowers,S., Sealy,J.M., Stupi,B., Dressen,D., Jagodzinska,B.M., Aquino,J., Gailunas,A., Truong,A.P., Tso,L., Xu,Y.Z., Hom,R.K., John,V., Tung,J.S., Pleiss,M.A., Tucker,J.A., Konradi,A.W., Sham,H.L., Jagodzinski,J., Toth,G., Brecht,E., Yao,N., Pan,H., Lin,M., Artis,D.R., Ruslim,L., Bova,M.P., Sinha,S., Yednock,T.A., Gauby,S., Zmolek,W., Quinn,K.P. and Sauer,J.M.
    Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region
    Bioorg Med Chem Lett20, 6034-6039. PubMed  Europe PubMed DOI  I
  462. Sala Frigerio,C., Fadeeva,J.V., Minogue,A.M., Citron,M., Van Leuven,F., Staufenbiel,M., Paganetti,P., Selkoe,D.J. and Walsh,D.M.
    beta-Secretase cleavage is not required for generation of the intracellular C-terminal domain of the amyloid precursor family of proteins
    FEBS J277, 1503-1518. PubMed  Europe PubMed DOI
  463. Salum,L.B. and Valadares,N.F.
    Fragment-guided approach to incorporating structural information into a CoMFA study: BACE-1 as an example
    J Comput Aided Mol Des24, 803-817. PubMed  Europe PubMed DOI  I
  464. Sasaki,H., Miki,K., Kinoshita,K., Koyama,K., Juliawaty,L.D., Achmad,S.A., Hakim,E.H., Kaneda,M. and Takahashi,K.
    beta-Secretase (BACE-1) inhibitory effect of biflavonoids
    Bioorg Med Chem Lett20, 4558-4560. PubMed  Europe PubMed DOI  I
  465. Schieb,H., Weidlich,S., Schlechtingen,G., Linning,P., Jennings,G., Gruner,M., Wiltfang,J., Klafki,H.W. and Knolker,H.J.
    Structural design, solid-phase synthesis and activity of membrane-anchored beta-secretase inhibitors on Abeta generation from wild-type and Swedish-mutant APP
    Chemistry16, 14412-14423. PubMed  Europe PubMed DOI  I
  466. Teng,L., Zhao,J., Wang,F., Ma,L. and Pei,G.
    A GPCR/secretase complex regulates beta- and gamma-secretase specificity for Abeta production and contributes to AD pathogenesis
    Cell Res20, 138-153. PubMed  Europe PubMed DOI
  467. Truong,A.P., Toth,G., Probst,G.D., Sealy,J.M., Bowers,S., Wone,D.W., Dressen,D., Hom,R.K., Konradi,A.W., Sham,H.L., Wu,J., Peterson,B.T., Ruslim,L., Bova,M.P., Kholodenko,D., Motter,R.N., Bard,F., Santiago,P., Ni,H., Chian,D., Soriano,F., Cole,T., Brigham,E.F., Wong,K., Zmolek,W., Goldbach,E., Samant,B., Chen,L., Zhang,H., Nakamura,D.F., Quinn,K.P., Yednock,T.A. and Sauer,J.M.
    Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model
    Bioorg Med Chem Lett20, 6231-6236. PubMed  Europe PubMed DOI  I
  468. Truong,A.P., Probst,G.D., Aquino,J., Fang,L., Brogley,L., Sealy,J.M., Hom,R.K., Tucker,J.A., John,V., Tung,J.S., Pleiss,M.A., Konradi,A.W., Sham,H.L., Dappen,M.S., Toth,G., Yao,N., Brecht,E., Pan,H., Artis,D.R., Ruslim,L., Bova,M.P., Sinha,S., Yednock,T.A., Zmolek,W., Quinn,K.P. and Sauer,J.M.
    Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: structure-activity relationship of P2' substituents
    Bioorg Med Chem Lett20, 4789-4794. PubMed  Europe PubMed DOI  I
  469. Wang,Y.S., Strickland,C., Voigt,J.H., Kennedy,M.E., Beyer,B.M., Senior,M.M., Smith,E.M., Nechuta,T.L., Madison,V.S., Czarniecki,M., McKittrick,B.A., Stamford,A.W., Parker,E.M., Hunter,J.C., Greenlee,W.J. and Wyss,D.F.
    Application of fragment-based NMR screening, X-ray crystallography, structure-based design, and focused chemical library design to identify novel microM leads for the development of nM BACE-1 (beta-site APP cleaving enzyme 1) inhibitors
    J Med Chem53, 942-950. PubMed  Europe PubMed DOI  I
  470. Wangsell,F., Gustafsson,K., Kvarnstrom,I., Borkakoti,N., Edlund,M., Jansson,K., Lindberg,J., Hallberg,A., Rosenquist,A. and Samuelsson,B.
    Synthesis of potent BACE-1 inhibitors incorporating a hydroxyethylene isostere as central core
    Eur J Med Chem45, 870-882. PubMed  Europe PubMed DOI  I
  471. Xu,W., Chen,G., Zhu,W. and Zuo,Z.
    Identification of a sub-micromolar, non-peptide inhibitor of beta-secretase with low neural cytotoxicity through in silico screening
    Bioorg Med Chem Lett20, 5763-5766. PubMed  Europe PubMed DOI  I
  472. Xu,W., Chen,G., Zhu,W. and Zuo,Z.
    Molecular docking and structure-activity relationship studies on benzothiazole based non-peptidic BACE-1 inhibitors
    Bioorg Med Chem Lett20, 6203-6207. PubMed  Europe PubMed DOI  I
  473. Yamakawa,H., Yagishita,S., Futai,E. and Ishiura,S.
    beta-Secretase inhibitor potency is decreased by aberrant beta-cleavage location of the "Swedish mutant" amyloid precursor protein
    J Biol Chem285, 1634-1642. PubMed  Europe PubMed DOI  I
  474. Zhou,P., Li,Y., Fan,Y., Wang,Z., Chopra,R., Olland,A., Hu,Y., Magolda,R.L., Pangalos,M., Reinhart,P.H., Turner,M.J., Bard,J., Malamas,M.S. and Robichaud,A.J.
    Pyridinyl aminohydantoins as small molecule BACE1 inhibitors
    Bioorg Med Chem Lett20, 2326-2329. PubMed  Europe PubMed DOI  I
  475. Zhu,H., Young,M.B., Nantermet,P.G., Graham,S.L., Colussi,D., Lai,M.T., Pietrak,B., Price,E.A., Sankaranarayanan,S., Shi,X.P., Tugusheva,K., Holahan,M.A., Michener,M.S., Cook,J.J., Simon,A., Hazuda,D.J., Vacca,J.P. and Rajapakse,H.A.
    Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors
    Bioorg Med Chem Lett20, 1779-1782. PubMed  Europe PubMed DOI  I
  476. Zhu,Z., Sun,Z.Y., Ye,Y., Voigt,J., Strickland,C., Smith,E.M., Cumming,J., Wang,L., Wong,J., Wang,Y.S., Wyss,D.F., Chen,X., Kuvelkar,R., Kennedy,M.E., Favreau,L., Parker,E., McKittrick,B.A., Stamford,A., Czarniecki,M., Greenlee,W. and Hunter,J.C.
    Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: part I - inhibitor design and validation
    J Med Chem53, 951-965. PubMed  Europe PubMed DOI  S  I
  477. 2009
  478. Al-Tel,T.H., Al-Qawasmeh,R.A., Schmidt,M.F., Al-Aboudi,A., Rao,S.N., Sabri,S.S. and Voelter,W.
    Rational design and synthesis of potent dibenzazepine motifs as beta-secretase inhibitors
    J Med Chem52, 6484-6488. PubMed  Europe PubMed DOI  I
  479. Albert,J.S.
    Progress in the development of beta-secretase inhibitors for Alzheimer's disease
    Prog Med Chem48, 133-161. PubMed  Europe PubMed DOI  I
  480. Annies,M., Stefani,M., Hueber,A., Fischer,F. and Paganetti,P.
    Splicing of intron 3 of human BACE requires the flanking introns 2 and 4
    Biochem Biophys Res Commun388, 434-438. PubMed  Europe PubMed DOI  R
  481. Bloch,L., Sineshchekova,O., Reichenbach,D., Reiss,K., Saftig,P., Kuro-o,M. and Kaether,C.
    Klotho is a substrate for alpha-, beta- and gamma-secretase
    FEBS Lett583, 3221-3224. PubMed  Europe PubMed DOI
  482. Charrier,N., Clarke,B., Demont,E., Dingwall,C., Dunsdon,R., Hawkins,J., Hubbard,J., Hussain,I., Maile,G., Matico,R., Mosley,J., Naylor,A., O'Brien,A., Redshaw,S., Rowland,P., Soleil,V., Smith,K.J., Sweitzer,S., Theobald,P., Vesey,D., Walter,D.S. and Wayne,G.
    Second generation of BACE-1 inhibitors part 2: optimisation of the non-prime side substituent
    Bioorg Med Chem Lett19, 3669-3673. PubMed  Europe PubMed DOI  I
  483. Charrier,N., Clarke,B., Cutler,L., Demont,E., Dingwall,C., Dunsdon,R., Hawkins,J., Howes,C., Hubbard,J., Hussain,I., Maile,G., Matico,R., Mosley,J., Naylor,A., O'Brien,A., Redshaw,S., Rowland,P., Soleil,V., Smith,K.J., Sweitzer,S., Theobald,P., Vesey,D., Walter,D.S. and Wayne,G.
    Second generation of BACE-1 inhibitors. Part 1: the need for improved pharmacokinetics
    Bioorg Med Chem Lett19, 3664-3668. PubMed  Europe PubMed DOI  I
  484. Charrier,N., Clarke,B., Cutler,L., Demont,E., Dingwall,C., Dunsdon,R., Hawkins,J., Howes,C., Hubbard,J., Hussain,I., Maile,G., Matico,R., Mosley,J., Naylor,A., O'Brien,A., Redshaw,S., Rowland,P., Soleil,V., Smith,K.J., Sweitzer,S., Theobald,P., Vesey,D., Walter,D.S. and Wayne,G.
    Second generation of BACE-1 inhibitors part 3: towards non hydroxyethylamine transition state mimetics
    Bioorg Med Chem Lett19, 3674-3678. PubMed  Europe PubMed DOI  I
  485. Choi,Y.H., Yoo,M.Y., Choi,C.W., Cha,M.R., Yon,G.H., Kwon,D.Y., Kim,Y.S., Park,W.K. and Ryu,S.Y.
    A new specific BACE-1 inhibitor from the stembark extract of Vitis vinifera
    Planta Med75, 537-540. PubMed  Europe PubMed DOI  I
  486. Godemann,R., Madden,J., Kramer,J., Smith,M., Fritz,U., Hesterkamp,T., Barker,J., Hoppner,S., Hallett,D., Cesura,A., Ebneth,A. and Kemp,J.
    Fragment-based discovery of BACE1 inhibitors using functional assays
    Biochemistry48, 10743-10751. PubMed  Europe PubMed DOI  I
  487. Hayley,M., Perspicace,S., Schulthess,T. and Seelig,J.
    Calcium enhances the proteolytic activity of BACE1: an in vitro biophysical and biochemical characterization of the BACE1-calcium interaction
    Biochim Biophys Acta1788, 1933-1938. PubMed  Europe PubMed DOI
  488. Hemming,M.L., Elias,J.E., Gygi,S.P. and Selkoe,D.J.
    Identification of beta-secretase (BACE1) substrates using quantitative proteomics
    PLoS ONE4, e8477-e8477. PubMed  Europe PubMed DOI  P
  489. Hills,I.D., Holloway,M.K., de Leon,P., Nomland,A., Zhu,H., Rajapakse,H., Allison,T.J., Munshi,S.K., Colussi,D., Pietrak,B.L., Toolan,D., Haugabook,S.J., Graham,S.L. and Stachel,S.J.
    A conformational constraint improves a beta-secretase inhibitor but for an unexpected reason
    Bioorg Med Chem Lett19, 4993-4995. PubMed  Europe PubMed DOI  I
  490. Holloway,M.K., Hunt,P. and McGaughey,G.B.
    Structure and modeling in the design of beta- and gamma-secretase inhibitors
    Drug Dev Res70, 70-93. DOI  I
  491. Huang,W.H., Sheng,R. and Hu,Y.Z.
    Progress in the development of nonpeptidomimetic BACE 1 inhibitors for Alzheimer's disease
    Curr Med Chem16, 1806-1820. PubMed  Europe PubMed DOI  I
  492. Hunt,C.E. and Turner,A.J.
    Cell biology, regulation and inhibition of beta-secretase (BACE-1)
    FEBS J276, 1845-1859. PubMed  Europe PubMed DOI  V  I
  493. Kume,H., Murayama,K.S. and Araki,W.
    The two-hydrophobic domain tertiary structure of reticulon proteins is critical for modulation of beta-secretase BACE1
    J Neurosci Res87, 2963-2972. PubMed  Europe PubMed DOI
  494. Laras,Y., Garino,C., Dessolin,J., Weck,C., Moret,V., Rolland,A. and Kraus,J.L.
    New N(4)-substituted piperazine naphthamide derivatives as BACE-1 inhibitors
    J Enzyme Inhib Med Chem24, 181-187. PubMed  Europe PubMed DOI  I
  495. Lee,J.Y., Lee,S.A., Kim,J.K., Chae,C.B. and Kim,Y.
    Interaction models of substrate peptides and beta-secretase studied by NMR spectroscopy and molecular dynamics simulation
    Mol Cells27, 651-656. PubMed  Europe PubMed DOI
  496. Machauer,R., Veenstra,S., Rondeau,J.M., Tintelnot-Blomley,M., Betschart,C., Neumann,U. and Paganetti,P.
    Structure-based design and synthesis of macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors
    Bioorg Med Chem Lett19, 1361-1365. PubMed  Europe PubMed DOI  S  I
  497. Machauer,R., Laumen,K., Veenstra,S., Rondeau,J.M., Tintelnot-Blomley,M., Betschart,C., Jaton,A.L., Desrayaud,S., Staufenbiel,M., Rabe,S., Paganetti,P. and Neumann,U.
    Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo
    Bioorg Med Chem Lett19, 1366-1370. PubMed  Europe PubMed DOI  I
  498. Malamas,M.S., Erdei,J., Gunawan,I., Barnes,K., Johnson,M., Hui,Y., Turner,J., Hu,Y., Wagner,E., Fan,K., Olland,A., Bard,J. and Robichaud,A.J.
    Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors
    J Med Chem52, 6314-6323. PubMed  Europe PubMed DOI  I
  499. Mowrer,K.R. and Wolfe,M.S.
    Identification of a cis-acting element involved in the regulation of BACE1 mRNA alternative splicing
    J Neurochem109, 1008-1016. PubMed  Europe PubMed DOI  R
  500. Regina,G.L., Piscitelli,F. and Silvestri,R.
    Synthetic strategies of nonpeptidic beta-secretase (BACE1) inhibitors
    J Heterocycl Chem46, 10-17. DOI  I
  501. Rizzi,L., Vaiana,N., Sagui,F., Genesio,E., Pilli,E., Porcari,V. and Romeo,S.
    Design, synthesis and docking studies of hydroxyethylamine and hydroxyethylsulfide BACE-1 inhibitors
    Protein Pept Lett16, 86-90. PubMed  Europe PubMed DOI  I
  502. Sealy,J.M., Truong,A.P., Tso,L., Probst,G.D., Aquino,J., Hom,R.K., Jagodzinska,B.M., Dressen,D., Wone,D.W., Brogley,L., John,V., Tung,J.S., Pleiss,M.A., Tucker,J.A., Konradi,A.W., Dappen,M.S., Toth,G., Pan,H., Ruslim,L., Miller,J., Bova,M.P., Sinha,S., Quinn,K.P. and Sauer,J.M.
    Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents
    Bioorg Med Chem Lett19, 6386-6391. PubMed  Europe PubMed DOI
  503. Silvestri,R.
    Boom in the development of non-peptidic beta-secretase (BACE1) inhibitors for the treatment of Alzheimer's disease
    Med Res Rev29, 295-338. PubMed  Europe PubMed DOI  V  I
  504. Singh,R., Barman,A. and Prabhakar,R.
    Computational insights into aspartyl protease activity of presenilin 1 (PS1) generating Alzheimer amyloid beta-peptides (Abeta40 and Abeta42)
    J Phys Chem B113, 2990-2999. PubMed  Europe PubMed DOI
  505. Stachel,S.J., Coburn,C.A., Rush,D., Jones,K.L., Zhu,H., Rajapakse,H., Graham,S.L., Simon,A., Katharine Holloway,M., Allison,T.J., Munshi,S.K., Espeseth,A.S., Zuck,P., Colussi,D., Wolfe,A., Pietrak,B.L., Lai,M.T. and Vacca,J.P.
    Discovery of aminoheterocycles as a novel beta-secretase inhibitor class: pH dependence on binding activity part 1
    Bioorg Med Chem Lett19, 2977-2980. PubMed  Europe PubMed DOI  I
  506. Steele,T.G., Hills,I.D., Nomland,A.A., de Leon,P., Allison,T., McGaughey,G., Colussi,D., Tugusheva,K., Haugabook,S.J., Espeseth,A.S., Zuck,P., Graham,S.L. and Stachel,S.J.
    Identification of a small molecule beta-secretase inhibitor that binds without catalytic aspartate engagement
    Bioorg Med Chem Lett19, 17-20. PubMed  Europe PubMed DOI  I
  507. Tomita,T.
    Secretase inhibitors and modulators for Alzheimer's disease treatment
    Expert Rev Neurother9, 661-679. PubMed  Europe PubMed DOI  V
  508. Vassar,R., Kovacs,D.M., Yan,R. and Wong,P.C.
    The beta-secretase enzyme BACE in health and Alzheimer's disease: regulation, cell biology, function, and therapeutic potential
    J Neurosci29, 12787-12794. PubMed  Europe PubMed DOI  V
  509. Vetrivel,K.S., Meckler,X., Chen,Y., Nguyen,P.D., Seidah,N.G., Vassar,R., Wong,P.C., Fukata,M., Kounnas,M.Z. and Thinakaran,G.
    Alzheimer disease Abeta production in the absence of S-palmitoylation-dependent targeting of BACE1 to lipid rafts
    J Biol Chem284, 3793-3803. PubMed  Europe PubMed DOI
  510. Vijayan,R.S., Prabu,M., Mascarenhas,N.M. and Ghoshal,N.
    Hybrid structure-based virtual screening protocol for the identification of novel BACE1 inhibitors
    J Chem Inf Model49, 647-657. PubMed  Europe PubMed DOI  I
  511. Volbracht,C., Penzkofer,S., Mansson,D., Christensen,K.V., Fog,K., Schildknecht,S., Leist,M. and Nielsen,J.
    Measurement of cellular beta-site of APP cleaving enzyme 1 activity and its modulation in neuronal assay systems
    Anal Biochem387, 208-220. PubMed  Europe PubMed DOI  A
  512. Wangsell,F., Russo,F., Savmarker,J., Rosenquist,A., Samuelsson,B. and Larhed,M.
    Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic
    Bioorg Med Chem Lett19, 4711-4714. PubMed  Europe PubMed DOI  I
  513. Willem,M., Lammich,S. and Haass,C.
    Function, regulation and therapeutic properties of beta-secretase (BACE1)
    Semin Cell Dev Biol20, 175-182. PubMed  Europe PubMed DOI
  514. Xu,W., Chen,G., Liew,O.W., Zuo,Z., Jiang,H. and Zhu,W.
    Novel non-peptide beta-secretase inhibitors derived from structure-based virtual screening and bioassay
    Bioorg Med Chem Lett19, 3188-3192. PubMed  Europe PubMed DOI  I
  515. Yang,W., Fucini,R.V., Fahr,B.T., Randal,M., Lind,K.E., Lam,M.B., Lu,W., Lu,Y., Cary,D.R., Romanowski,M.J., Colussi,D., Pietrak,B., Allison,T.J., Munshi,S.K., Penny,D.M., Pham,P., Sun,J., Thomas,A.E., Wilkinson,J.M., Jacobs,J.W., McDowell,R.S. and Ballinger,M.D.
    Fragment-based discovery of nonpeptidic BACE-1 inhibitors using tethering
    Biochemistry48, 4488-4496. PubMed  Europe PubMed DOI  S  I
  516. Yi Mok,N., Chadwick,J., Kellett,K.A., Hooper,N.M., Johnson,A.P. and Fishwick,C.W.
    Discovery of novel non-peptide inhibitors of BACE-1 using virtual high-throughput screening
    Bioorg Med Chem Lett19, 6770-6774. PubMed  Europe PubMed DOI  I
  517. Zhu,Y., Xiao,K., Ma,L., Xiong,B., Fu,Y., Yu,H., Wang,W., Wang,X., Hu,D., Peng,H., Li,J., Gong,Q., Chai,Q., Tang,X., Zhang,H., Li,J. and Shen,J.
    Design, synthesis and biological evaluation of novel dual inhibitors of acetylcholinesterase and beta-secretase
    Bioorg Med Chem17, 1600-1613. PubMed  Europe PubMed DOI  I
  518. Zhu,Y.P., Xiao,K., Yu,H.P., Ma,L.P., Xiong,B., Zhang,H.Y., Wang,X., Li,J.Y., Li,J. and Shen,J.K.
    Discovery of potent beta-secretase (bace-1) inhibitors by the synthesis of isophthalamide-containing hybrids
    Acta Pharmacol Sin30, 259-269. PubMed  Europe PubMed DOI  I
  519. 2008
  520. Back,M., Nyhlen,J., Kvarnstrom,I., Appelgren,S., Borkakoti,N., Jansson,K., Lindberg,J., Nystrom,S., Hallberg,A., Rosenquist,S. and Samuelsson,B.
    Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: exploration of P1 phenoxy and benzyloxy residues
    Bioorg Med Chem16, 9471-9486. PubMed  Europe PubMed DOI  I
  521. Barrow,J.C., Stauffer,S.R., Rittle,K.E., Ngo,P.L., Yang,Z., Selnick,H.G., Graham,S.L., Munshi,S., McGaughey,G.B., Holloway,M.K., Simon,A.J., Price,E.A., Sankaranarayanan,S., Colussi,D., Tugusheva,K., Lai,M.T., Espeseth,A.S., Xu,M., Huang,Q., Wolfe,A., Pietrak,B., Zuck,P., Levorse,D.A., Hazuda,D. and Vacca,J.P.
    Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase
    J Med Chem51, 6259-6262. PubMed  Europe PubMed DOI  S  I
  522. Beswick,P., Charrier,N., Clarke,B., Demont,E., Dingwall,C., Dunsdon,R., Faller,A., Gleave,R., Hawkins,J., Hussain,I., Johnson,C.N., MacPherson,D., Maile,G., Matico,R., Milner,P., Mosley,J., Naylor,A., O'Brien,A., Redshaw,S., Riddell,D., Rowland,P., Skidmore,J., Soleil,V., Smith,K.J., Stanway,S., Stemp,G., Stuart,A., Sweitzer,S., Theobald,P., Vesey,D., Walter,D.S., Ward,J. and Wayne,G.
    BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells
    Bioorg Med Chem Lett18, 1022-1026. PubMed  Europe PubMed DOI  I
  523. Charrier,N., Clarke,B., Cutler,L., Demont,E., Dingwall,C., Dunsdon,R., East,P., Hawkins,J., Howes,C., Hussain,I., Jeffrey,P., Maile,G., Matico,R., Mosley,J., Naylor,A., O'Brien,A., Redshaw,S., Rowland,P., Soleil,V., Smith,K.J., Sweitzer,S., Theobald,P., Vesey,D., Walter,D.S. and Wayne,G.
    Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability
    J Med Chem51, 3313-3317. PubMed  Europe PubMed DOI  I
  524. Choi,Y.H., Yon,G.H., Hong,K.S., Yoo,D.S., Choi,C.W., Park,W.K., Kong,J.Y., Kim,Y.S. and Ryu,S.Y.
    In vitro BACE-1 inhibitory phenolic components from the seeds of Psoralea corylifolia
    Planta Med74, 1405-1408. PubMed  Europe PubMed DOI  I
  525. Clarke,B., Demont,E., Dingwall,C., Dunsdon,R., Faller,A., Hawkins,J., Hussain,I., MacPherson,D., Maile,G., Matico,R., Milner,P., Mosley,J., Naylor,A., O'Brien,A., Redshaw,S., Riddell,D., Rowland,P., Soleil,V., Smith,K.J., Stanway,S., Stemp,G., Sweitzer,S., Theobald,P., Vesey,D., Walter,D.S., Ward,J. and Wayne,G.
    BACE-1 inhibitors part 2: identification of hydroxy ethylamines (HEAs) with reduced peptidic character
    Bioorg Med Chem Lett18, 1017-1021. PubMed  Europe PubMed DOI  I
  526. Clarke,B., Demont,E., Dingwall,C., Dunsdon,R., Faller,A., Hawkins,J., Hussain,I., MacPherson,D., Maile,G., Matico,R., Milner,P., Mosley,J., Naylor,A., O'Brien,A., Redshaw,S., Riddell,D., Rowland,P., Soleil,V., Smith,K.J., Stanway,S., Stemp,G., Sweitzer,S., Theobald,P., Vesey,D., Walter,D.S., Ward,J. and Wayne,G.
    BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs)
    Bioorg Med Chem Lett18, 1011-1016. PubMed  Europe PubMed DOI  I
  527. Cole,D.C., Stock,J.R., Chopra,R., Cowling,R., Ellingboe,J.W., Fan,K.Y., Harrison,B.L., Hu,Y., Jacobsen,S., Jennings,L.D., Jin,G., Lohse,P.A., Malamas,M.S., Manas,E.S., Moore,W.J., O'Donnell,M.M., Olland,A.M., Robichaud,A.J., Svenson,K., Wu,J., Wagner,E. and Bard,J.
    Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets
    Bioorg Med Chem Lett18, 1063-1066. PubMed  Europe PubMed DOI  I
  528. Cole,S.L. and Vassar,R.
    The role of amyloid precursor protein processing by BACE1, the beta-secretase, in Alzheimer disease pathophysiology
    J Biol Chem283, 29621-29625. PubMed  Europe PubMed DOI  K  V  T
  529. Cole,S.L. and Vassar,R.
    BACE1 structure and function in health and Alzheimer's disease
    Curr Alzheimer Res5, 100-120. PubMed  Europe PubMed DOI  K
  530. Dunn,B.M.
    Editorial. BACE or beta-secretase - a target for drug discovery for treatment of Alzheimer's disease
    Protein Pept Lett15, 118-118. PubMed  Europe PubMed
  531. Emmons,T.L., Shuck,M.E., Babcock,M.S., Holloway,J.S., Leone,J.W., Durbin,J.D., Paddock,D.J., Prince,D.B., Heinrikson,R.L., Fischer,H.D., Bienkowski,M.J., Benson,T.E. and Tomasselli,A.G.
    Large-scale purification of human BACE expressed in mammalian cells and removal of the prosegment with HIV-1 protease to improve crystal diffraction
    Protein Pept Lett15, 119-130. PubMed  Europe PubMed  E
  532. Faghihi,M.A., Modarresi,F., Khalil,A.M., Wood,D.E., Sahagan,B.G., Morgan,T.E., Finch,C.E., St Laurent,G., III, Kenny,P.J. and Wahlestedt,C.
    Expression of a noncoding RNA is elevated in Alzheimer's disease and drives rapid feed-forward regulation of beta-secretase
    Nat Med14, 723-730. PubMed  Europe PubMed DOI
  533. Ghosh,A.K., Gemma,S. and Tang,J.
    beta-Secretase as a therapeutic target for Alzheimer's disease
    Neurotherapeutics5, 399-408. PubMed  Europe PubMed DOI  V  T
  534. Ghosh,A.K., Kumaragurubaran,N., Hong,L., Koelsh,G. and Tang,J.
    Memapsin 2 (beta-secretase) inhibitors: drug development
    Curr Alzheimer Res5, 121-131. PubMed  Europe PubMed DOI  T  I
  535. Ghosh,A.K., Kumaragurubaran,N., Hong,L., Kulkarni,S., Xu,X., Miller,H.B., Reddy,D.S., Weerasena,V., Turner,R., Chang,W., Koelsch,G. and Tang,J.
    Potent memapsin 2 (beta-secretase) inhibitors: design, synthesis, protein-ligand X-ray structure, and in vivo evaluation
    Bioorg Med Chem Lett18, 1031-1036. PubMed  Europe PubMed DOI  S  I
  536. Grimm,M.O., Grimm,H.S., Tomic,I., Beyreuther,K., Hartmann,T. and Bergmann,C.
    Independent inhibition of Alzheimer disease beta- and gamma-secretase cleavage by lowered cholesterol levels
    J Biol Chem283, 11302-11311. PubMed  Europe PubMed DOI
  537. Hoyos Flight,M.
    Neurodegenerative disease: inhibiting beta-secretase where it matters
    Nat Rev Neurosci9, 414-415. DOI
  538. Huang,W., Yu,H., Sheng,R., Li,J. and Hu,Y.
    Identification of pharmacophore model, synthesis and biological evaluation of N-phenyl-1-arylamide and N-phenylbenzenesulfonamide derivatives as BACE 1 inhibitors
    Bioorg Med Chem16, 10190-10197. PubMed  Europe PubMed DOI  I
  539. Iserloh,U., Pan,J., Stamford,A.W., Kennedy,M.E., Zhang,Q., Zhang,L., Parker,E.M., McHugh,N.A., Favreau,L., Strickland,C. and Voigt,J.
    Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor
    Bioorg Med Chem Lett18, 418-422. PubMed  Europe PubMed DOI  I
  540. Iserloh,U., Wu,Y., Cumming,J.N., Pan,J., Wang,L.Y., Stamford,A.W., Kennedy,M.E., Kuvelkar,R., Chen,X., Parker,E.M., Strickland,C. and Voigt,J.
    Potent pyrrolidine- and piperidine-based BACE-1 inhibitors
    Bioorg Med Chem Lett18, 414-417. PubMed  Europe PubMed DOI  I
  541. Jennings,L.D., Cole,D.C., Stock,J.R., Sukhdeo,M.N., Ellingboe,J.W., Cowling,R., Jin,G., Manas,E.S., Fan,K.Y., Malamas,M.S., Harrison,B.L., Jacobsen,S., Chopra,R., Lohse,P.A., Moore,W.J., O'Donnell,M.M., Hu,Y., Robichaud,A.J., Turner,M.J., Wagner,E. and Bard,J.
    Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1' substrate binding pocket
    Bioorg Med Chem Lett18, 767-771. PubMed  Europe PubMed DOI  I
  542. Jonas,M.C., Costantini,C. and Puglielli,L.
    PCSK9 is required for the disposal of non-acetylated intermediates of the nascent membrane protein BACE1
    EMBO Rep9, 916-922. PubMed  Europe PubMed DOI
  543. Kuglstatter,A., Stahl,M., Peters,J.U., Huber,W., Stihle,M., Schlatter,D., Benz,J., Ruf,A., Roth,D., Enderle,T. and Hennig,M.
    Tyramine fragment binding to BACE-1
    Bioorg Med Chem Lett18, 1304-1307. PubMed  Europe PubMed DOI  I
  544. Lv,L., Yang,Q.Y., Zhao,Y., Yao,C.S., Sun,Y., Yang,E.J., Song,K.S., Mook-Jung,I. and Fang,W.S.
    BACE1 (beta-secretase) inhibitory chromone glycosides from Aloe vera and Aloe nobilis
    Planta Med74, 540-545. PubMed  Europe PubMed DOI  I
  545. Park,H., Min,K., Kwak,H.S., Koo,K.D., Lim,D., Seo,S.W., Choi,J.U., Platt,B. and Choi,D.Y.
    Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives
    Bioorg Med Chem Lett18, 2900-2904. PubMed  Europe PubMed DOI  I
  546. Rajendran,L., Schneider,A., Schlechtingen,G., Weidlich,S., Ries,J., Braxmeier,T., Schwille,P., Schulz,J.B., Schroeder,C., Simons,M., Jennings,G., Knolker,H.J. and Simons,K.
    Efficient inhibition of the Alzheimer's disease beta-secretase by membrane targeting
    Science320, 520-523. PubMed  Europe PubMed DOI  I
  547. Sankaranarayanan,S., Price,E.A., Wu,G., Crouthamel,M.C., Shi,X.P., Tugusheva,K., Tyler,K.X., Kahana,J., Ellis,J., Jin,L., Steele,T., Stachel,S., Coburn,C. and Simon,A.J.
    In vivo beta-secretase 1 inhibition leads to brain Abeta lowering and increased alpha-secretase processing of amyloid precursor protein without effect on neuregulin-1
    J Pharmacol Exp Ther324, 957-969. PubMed  Europe PubMed DOI  I
  548. Schechter,I. and Ziv,E.
    Kinetic properties of cathepsin D and BACE 1 indicate the need to search for additional beta-secretase candidate(s)
    Biol Chem389, 313-320. PubMed  Europe PubMed DOI
  549. Shimizu,H., Tosaki,A., Kaneko,K., Hisano,T., Sakurai,T. and Nukina,N.
    Crystal structure of an active form of BACE1, an enzyme responsible for amyloid beta protein production
    Mol Cell Biol28, 3663-3671. PubMed  Europe PubMed DOI  S
  550. Shimmyo,Y., Kihara,T., Akaike,A., Niidome,T. and Sugimoto,H.
    Flavonols and flavones as BACE-1 inhibitors: structure-activity relationship in cell-free, cell-based and in silico studies reveal novel pharmacophore features
    Biochim Biophys Acta1780, 819-825. PubMed  Europe PubMed DOI  I
  551. Small,D.H., Klaver,D.W. and Beckman,M.
    Regulation of proBACE1 by glycosaminoglycans
    Neurodegener Dis5, 206-208. PubMed  Europe PubMed DOI
  552. Stockley,J.H. and O'Neill,C.
    Understanding BACE1: essential protease for amyloid-beta production in Alzheimer's disease
    Cell Mol Life Sci65, 3265-3289. PubMed  Europe PubMed DOI  V
  553. Tamagno,E., Guglielmotto,M., Aragno,M., Borghi,R., Autelli,R., Giliberto,L., Muraca,G., Danni,O., Zhu,X., Smith,M.A., Perry,G., Jo,D.G., Mattson,M.P. and Tabaton,M.
    Oxidative stress activates a positive feedback between the gamma- and beta-secretase cleavages of the beta-amyloid precursor protein
    J Neurochem104, 683-695. PubMed  Europe PubMed DOI
  554. Todd,S., McKnight,A.J., Liu,W.W., Carson,R., Heggarty,S., McGuinness,B., Irvine,G.B., Craig,D., Passmore,A.P. and Johnston,J.A.
    BACE1 polymorphisms do not influence platelet membrane beta-secretase activity or genetic susceptibility for Alzheimer's disease in the Northern Irish population
    Neuromolecular Med10, 368-376. PubMed  Europe PubMed DOI  M
  555. Tomasselli,A.G., Paddock,D.J., Emmons,T.L., Mildner,A.M., Leone,J.W., Lull,J.M., Cialdella,J.I., Prince,D.B., Fischer,H.D., Heinrikson,R.L. and Benson,T.E.
    High yield expression of human BACE constructs in Eschericia coli for refolding, purification, and high resolution diffracting crystal forms
    Protein Pept Lett15, 131-143. PubMed  Europe PubMed  E
  556. Wong,P.C.
    Translational control of BACE1 may go awry in Alzheimer's disease
    Neuron60, 941-943. PubMed  Europe PubMed DOI
  557. Woodard-Grice,A.V., McBrayer,A.C., Wakefield,J.K., Zhuo,Y. and Bellis,S.L.
    Proteolytic shedding of ST6Gal-I by BACE1 regulates the glycosylation and function of alpha4beta1 integrins
    J Biol Chem283, 26364-26373. PubMed  Europe PubMed DOI
  558. 2007
  559. Barazza,A., Gotz,M., Cadamuro,S.A., Goettig,P., Willem,M., Steuber,H., Kohler,T., Jestel,A., Reinemer,P., Renner,C., Bode,W. and Moroder,L.
    Macrocyclic statine-based inhibitors of BACE-1
    Chembiochem8, 2078-2091. PubMed  Europe PubMed DOI  I
  560. Barrow,J.C., Rittle,K.E., Ngo,P.L., Selnick,H.G., Graham,S.L., Pitzenberger,S.M., McGaughey,G.B., Colussi,D., Lai,M.T., Huang,Q., Tugusheva,K., Espeseth,A.S., Simon,A.J., Munshi,S.K. and Vacca,J.P.
    Design and synthesis of 2,3,5-substituted imidazolidin-4-one inhibitors of BACE-1
    ChemMedChem2, 995-999. PubMed  Europe PubMed DOI  I
  561. Baxter,E.W., Conway,K.A., Kennis,L., Bischoff,F., Mercken,M.H., Winter,H.L., Reynolds,C.H., Tounge,B.A., Luo,C., Scott,M.K., Huang,Y., Braeken,M., Pieters,S.M., Berthelot,D.J., Masure,S., Bruinzeel,W.D., Jordan,A.D., Parker,M.H., Boyd,R.E., Qu,J., Alexander,R.S., Brenneman,D.E. and Reitz,A.B.
    2-Amino-3,4-dihydroquinazolines as inhibitors of BACE-1 (beta-site APP cleaving enzyme): use of structure based design to convert a micromolar hit into a nanomolar lead
    J Med Chem50, 4261-4264. PubMed  Europe PubMed DOI  S  I
  562. Braun,H.A., Zall,A., Brockhaus,M., Schutz,M., Meusinger,R. and Schmidt,B.
    Aspartic protease inhibitors via C1-homologation of peptidic aldehydes and studies on reduced amide isosteres
    Tetrahedron Lett48, 7990-7993. DOI  I
  563. Chang,W.P., Downs,D., Huang,X.P., Da,H., Fung,K.M. and Tang,J.
    Amyloid-beta reduction by memapsin 2 (beta-secretase) immunization
    FASEB J21, 3184-3196. PubMed  Europe PubMed DOI
  564. Cole,S.L. and Vassar,R.
    The Alzheimer's disease beta-secretase enzyme, BACE1
    Mol Neurodegener2, 22-22. PubMed  Europe PubMed DOI  V
  565. Congreve,M., Aharony,D., Albert,J., Callaghan,O., Campbell,J., Carr,R.A., Chessari,G., Cowan,S., Edwards,P.D., Frederickson,M., McMenamin,R., Murray,C.W., Patel,S. and Wallis,N.
    Application of fragment screening by X-ray crystallography to the discovery of aminopyridines as inhibitors of beta-secretase
    J Med Chem50, 1124-1132. PubMed  Europe PubMed DOI  I
  566. Edwards,P.
    Tetramic and tetronic acids as beta-secretase inhibitors
    Drug Discov Today12, 345-346. DOI  I
  567. Edwards,P.D., Albert,J.S., Sylvester,M., Aharony,D., Andisik,D., Callaghan,O., Campbell,J.B., Carr,R.A., Chessari,G., Congreve,M., Frederickson,M., Folmer,R.H., Geschwindner,S., Koether,G., Kolmodin,K., Krumrine,J., Mauger,R.C., Murray,C.W., Olsson,L.L., Patel,S., Spear,N. and Tian,G.
    Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency
    J Med Chem50, 5912-5925. PubMed  Europe PubMed DOI  I
  568. Evin,G. and Kenche,V.B.
    BACE inhibitors as potential therapeutics for Alzheimer's disease
    Recent Patents CNS Drug Discov2, 188-199. PubMed  Europe PubMed DOI  V  T  I
  569. Fobare,W.F., Solvibile,W.R., Robichaud,A.J., Malamas,M.S., Manas,E., Turner,J., Hu,Y., Wagner,E., Chopra,R., Cowling,R., Jin,G. and Bard,J.
    Thiophene substituted acylguanidines as BACE1 inhibitors
    Bioorg Med Chem Lett17, 5353-5356. PubMed  Europe PubMed DOI  I
  570. Freskos,J.N., Fobian,Y.M., Benson,T.E., Moon,J.B., Bienkowski,M.J., Brown,D.L., Emmons,T.L., Heintz,R., Laborde,A., McDonald,J.J., Mischke,B.V., Molyneaux,J.M., Mullins,P.B., Bryan Prince,D., Paddock,D.J., Tomasselli,A.G. and Winterrowd,G.
    Design of potent inhibitors of human beta-secretase. Part 2
    Bioorg Med Chem Lett17, 78-81. PubMed  Europe PubMed DOI  I
  571. Freskos,J.N., Fobian,Y.M., Benson,T.E., Bienkowski,M.J., Brown,D.L., Emmons,T.L., Heintz,R., Laborde,A., McDonald,J.J., Mischke,B.V., Molyneaux,J.M., Moon,J.B., Mullins,P.B., Bryan Prince,D., Paddock,D.J., Tomasselli,A.G. and Winterrowd,G.
    Design of potent inhibitors of human beta-secretase. Part 1
    Bioorg Med Chem Lett17, 73-77. PubMed  Europe PubMed DOI  I
  572. Geschwindner,S., Olsson,L.L., Albert,J.S., Deinum,J., Edwards,P.D., de Beer,T. and Folmer,R.H.
    Discovery of a novel warhead against beta-secretase through fragment-based lead generation
    J Med Chem50, 5903-5911. PubMed  Europe PubMed DOI  I
  573. Ghosh,A.K., Bilcer,G., Hong,L., Koelsch,G. and Tang,J.
    Memapsin 2 (beta-secretase) inhibitor drug, between fantasy and reality
    Curr Alzheimer Res4, 418-422. PubMed  Europe PubMed DOI
  574. Ghosh,A.K., Kumaragurubaran,N., Hong,L., Kulkarni,S.S., Xu,X., Chang,W., Weerasena,V., Turner,R., Koelsch,G., Bilcer,G. and Tang,J.
    Design, synthesis, and X-ray structure of potent memapsin 2 (beta-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands
    J Med Chem50, 2399-2407. PubMed  Europe PubMed DOI  S  I
  575. Herzig,M.C., Paganetti,P., Staufenbiel,M. and Jucker,M.
    BACE1 and mutated presenilin-1 differently modulate Abeta40 and Abeta42 levels and cerebral amyloidosis in APPDutch transgenic mice
    Neurodegener Dis4, 127-135. PubMed  Europe PubMed DOI
  576. Hills,I.D. and Vacca,J.P.
    Progress toward a practical BACE-1 inhibitor
    Curr Opin Drug Discov Devel10, 383-391. PubMed  Europe PubMed  I
  577. Hussain,I., Hawkins,J., Harrison,D., Hille,C., Wayne,G., Cutler,L., Buck,T., Walter,D., Demont,E., Howes,C., Naylor,A., Jeffrey,P., Gonzalez,M.I., Dingwall,C., Michel,A., Redshaw,S. and Davis,J.B.
    Oral administration of a potent and selective non-peptidic BACE-1 inhibitor decreases beta-cleavage of amyloid precursor protein and amyloid-beta production in vivo
    J Neurochem100, 802-809. PubMed  Europe PubMed DOI  I
  578. Kortum,S.W., Benson,T.E., Bienkowski,M.J., Emmons,T.L., Prince,D.B., Paddock,D.J., Tomasselli,A.G., Moon,J.B., Laborde,A. and TenBrink,R.E.
    Potent and selective isophthalamide S2 hydroxyethylamine inhibitors of BACE1
    Bioorg Med Chem Lett17, 3378-3383. PubMed  Europe PubMed DOI  I
  579. Kuzuya,A., Uemura,K., Kitagawa,N., Aoyagi,N., Kihara,T., Ninomiya,H., Ishiura,S., Takahashi,R. and Shimohama,S.
    Presenilin 1 is involved in the maturation of beta-site amyloid precursor protein-cleaving enzyme 1 (BACE1)
    J Neurosci Res85, 153-165. PubMed  Europe PubMed DOI
  580. Lee,D.H., Lee,D.H. and Lee,J.S.
    Characterization of a new antidementia beta-secretase inhibitory peptide from Saccharomyces cerevisiae
    Enzyme Microb Technol42, 83-88. DOI  I
  581. Lee,H.W., Seo,H.S., Ha,I. and Chung,S.H.
    Overexpression of BACE1 stimulates spontaneous basal secretion in PC12 cells
    Neurosci Lett421, 178-183. PubMed  Europe PubMed DOI
  582. Lindsley,S.R., Moore,K.P., Rajapakse,H.A., Selnick,H.G., Young,M.B., Zhu,H., Munshi,S., Kuo,L., McGaughey,G.B., Colussi,D., Crouthamel,M.C., Lai,M.T., Pietrak,B., Price,E.A., Sankaranarayanan,S., Simon,A.J., Seabrook,G.R., Hazuda,D.J., Pudvah,N.T., Hochman,J.H., Graham,S.L., Vacca,J.P. and Nantermet,P.G.
    Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors
    Bioorg Med Chem Lett17, 4057-4061. PubMed  Europe PubMed DOI  I
  583. Lu,J., Zhang,Z., Yang,J., Chu,J., Li,P., Zeng,S. and Luo,Q.
    Visualization of beta-secretase cleavage in living cells using a genetically encoded surface-displayed FRET probe
    Biochem Biophys Res Commun362, 25-30. PubMed  Europe PubMed DOI  L
  584. [YEAR:22-2-2007]Maillard,M.C., Hom,R.K., Benson,T.E., Moon,J.B., Mamo,S., Bienkowski,M., Tomasselli,A.G., Woods,D.D., Prince,D.B., Paddock,D.J., Emmons,T.L., Tucker,J.A., Dappen,M.S., Brogley,L., Thorsett,E.D., Jewett,N., Sinha,S. and John,V.
    Design, synthesis, and crystal structure of hydroxyethyl secondary amine-based peptidomimetic inhibitors of human beta-secretase
    J Med Chem50, 776-781. PubMed  Europe PubMed DOI  I
  585. Manzenrieder,F., Frank,A.O., Huber,T., Dorner-Ciossek,C. and Kessler,H.
    Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human beta-secretase (BACE1)
    Bioorg Med Chem15, 4136-4143. PubMed  Europe PubMed DOI  I
  586. McConlogue,L., Buttini,M., Anderson,J.P., Brigham,E.F., Chen,K.S., Freedman,S.B., Games,D., Johnson-Wood,K., Lee,M., Zeller,M., Liu,W., Motter,R. and Sinha,S.
    Partial reduction of BACE1 has dramatic effects on Alzheimer plaque and synaptic pathology in APP transgenic mice
    J Biol Chem282, 26326-26334. PubMed  Europe PubMed DOI  K
  587. McGaughey,G.B. and Holloway,M.K.
    Structure-guided design of beta-secretase (BACE-1) inhibitors
    Expert Opin Drug Discov2, 1129-1138. PubMed  Europe PubMed DOI  V  I
  588. McGaughey,G.B., Colussi,D., Graham,S.L., Lai,M.T., Munshi,S.K., Nantermet,P.G., Pietrak,B., Rajapakse,H.A., Selnick,H.G., Stauffer,S.R. and Holloway,M.K.
    beta-Secretase (BACE-1) inhibitors: accounting for 10s loop flexibility using rigid active sites
    Bioorg Med Chem Lett17, 1117-1121. PubMed  Europe PubMed DOI  I
  589. Moore,K.P., Zhu,H., Rajapakse,H.A., McGaughey,G.B., Colussi,D., Price,E.A., Sankaranarayanan,S., Simon,A.J., Pudvah,N.T., Hochman,J.H., Allison,T., Munshi,S.K., Graham,S.L., Vacca,J.P. and Nantermet,P.G.
    Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors
    Bioorg Med Chem Lett17, 5831-5835. PubMed  Europe PubMed DOI  I
  590. Murray,C.W., Callaghan,O., Chessari,G., Cleasby,A., Congreve,M., Frederickson,M., Hartshorn,M.J., McMenamin,R., Patel,S. and Wallis,N.
    Application of fragment screening by X-ray crystallography to beta-secretase
    J Med Chem50, 1116-1123. PubMed  Europe PubMed DOI
  591. Na,C.H., Jeon,S.H., Zhang,G., Olson,G.L. and Chae,C.B.
    Inhibition of amyloid beta-peptide production by blockage of beta-secretase cleavage site of amyloid precursor protein
    J Neurochem101, 1583-1595. PubMed  Europe PubMed DOI
  592. Olson,R.E. and Marcin,L.R.
    Chapter 3 Secretase Inhibitors and Modulators for the Treatment of Alzheimer's Disease
    Annu Rep Med Chem42, 27-47. DOI  V  I
  593. Polgar,T., Magyar,C., Simon,I. and Keseru,G.M.
    Impact of ligand protonation on virtual screening against beta-secretase (BACE1)
    J Chem Inf Model47, 2366-2373. PubMed  Europe PubMed DOI
  594. Stanton,M.G., Stauffer,S.R., Gregro,A.R., Steinbeiser,M., Nantermet,P., Sankaranarayanan,S., Price,E.A., Wu,G., Crouthamel,M.C., Ellis,J., Lai,M.T., Espeseth,A.S., Shi,X.P., Jin,L., Colussi,D., Pietrak,B., Huang,Q., Xu,M., Simon,A.J., Graham,S.L., Vacca,J.P. and Selnick,H.
    Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid
    J Med Chem50, 3431-3433. PubMed  Europe PubMed DOI  I
  595. Stauffer,S.R., Stanton,M.G., Gregro,A.R., Steinbeiser,M.A., Shaffer,J.R., Nantermet,P.G., Barrow,J.C., Rittle,K.E., Collusi,D., Espeseth,A.S., Lai,M.T., Pietrak,B.L., Holloway,M.K., McGaughey,G.B., Munshi,S.K., Hochman,J.H., Simon,A.J., Selnick,H.G., Graham,S.L. and Vacca,J.P.
    Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind beta-secretase in a N-terminal 10s-loop down conformation
    Bioorg Med Chem Lett17, 1788-1792. PubMed  Europe PubMed DOI  I
  596. Sugimoto,I., Futakawa,S., Oka,R., Ogawa,K., Marth,J.D., Miyoshi,E., Taniguchi,N., Hashimoto,Y. and Kitazume,S.
    Beta-galactoside alpha2,6-sialyltransferase I cleavage by BACE1 enhances the sialylation of soluble glycoproteins. A novel regulatory mechanism for alpha2,6-sialylation
    J Biol Chem282, 34896-34903. PubMed  Europe PubMed DOI
  597. Tanahashi,H. and Tabira,T.
    A novel beta-site amyloid precursor protein cleaving enzyme (BACE) isoform regulated by nonsense-mediated mRNA decay and proteasome-dependent degradation
    Neurosci Lett428, 103-108. PubMed  Europe PubMed DOI  R
  598. Yang,X., Zou,X., Fu,Y., Mou,K., Fu,G., Ma,C. and Xu,P.
    Synthesis of beta-secretase inhibitors containing a hydroxyethylene dipeptide isostere
    Synthetic Communications37, 9-24. DOI  I
  599. Zhong,Z., Ewers,M., Teipel,S., Burger,K., Wallin,A., Blennow,K., He,P., McAllister,C., Hampel,H. and Shen,Y.
    Levels of beta-secretase (BACE1) in cerebrospinal fluid as a predictor of risk in mild cognitive impairment
    Arch Gen Psychiatry64, 718-726. PubMed  Europe PubMed DOI
  600. Zuo,Z., Gang,C., Zou,H., Mok,P.C., Zhu,W., Chen,K. and Jiang,H.
    Why does beta-secretase zymogen possess catalytic activity? Molecular modeling and molecular dynamics simulation studies
    Comput Biol Chem31, 186-195. PubMed  Europe PubMed DOI
  601. 2006
  602. Asai,M., Hattori,C., Iwata,N., Saido,T.C., Sasagawa,N., Szabo,B., Hashimoto,Y., Maruyama,K., Tanuma,S., Kiso,Y. and Ishiura,S.
    The novel beta-secretase inhibitor KMI-429 reduces amyloid beta peptide production in amyloid precursor protein transgenic and wild-type mice
    J Neurochem96, 533-540. PubMed  Europe PubMed DOI  I
  603. Avram,S., Milac,A.L., Mihailescu,D.F., Dabu,A. and Flonta,M.L.
    Computer-aided drug design applied to beta and gamma secretase inhibitors - perspectives for new Alzheimer disease therapy
    Curr Enzyme Inhib2, 311-328. DOI
  604. [YEAR:28-3-2006]Bridges,K.G., Chopra,R., Lin,L., Svenson,K., Tam,A., Jin,G., Cowling,R., Lovering,F., Akopian,T.N., DiBlasio-Smith,E., Annis-Freeman,B., Marvell,T.H., LaVallie,E.R., Zollner,R.S., Bard,J., Somers,W.S., Stahl,M.L. and Kriz,R.W.
    A novel approach to identifying beta-secretase inhibitors: bis-statine peptide mimetics discovered using structure and spot synthesis
    Peptides27, 1877-1885. PubMed  Europe PubMed DOI  I
  605. [YEAR:9-5-2006]Coburn,C.A., Stachel,S.J., Jones,K.G., Steele,T.G., Rush,D.M., Dimuzio,J., Pietrak,B.L., Lai,M.T., Huang,Q., Lineberger,J., Jin,L., Munshi,S., Katharine Holloway,M., Espeseth,A., Simon,A., Hazuda,D., Graham,S.L. and Vacca,J.P.
    BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres
    Bioorg Med Chem Lett16, 3635-3638. PubMed  Europe PubMed DOI  I
  606. [YEAR:19-10-2006]Cole,D.C., Manas,E.S., Stock,J.R., Condon,J.S., Jennings,L.D., Aulabaugh,A., Chopra,R., Cowling,R., Ellingboe,J.W., Fan,K.Y., Harrison,B.L., Hu,Y., Jacobsen,S., Jin,G., Lin,L., Lovering,F.E., Malamas,M.S., Stahl,M.L., Strand,J., Sukhdeo,M.N., Svenson,K., Turner,M.J., Wagner,E., Wu,J., Zhou,P. and Bard,J.
    Acylguanidines as small-molecule beta-secretase inhibitors
    J Med Chem49, 6158-6161. PubMed  Europe PubMed DOI  I
  607. Dong,W.J., Feng,G.F., Gong,H.L., Liu,S.H. and Hu,H.T.
    Specific suppression of beta-secretase gene expression by short interfering RNA in SK-N-SH cells
    Sichuan Da Xue Xue Bao Yi Xue Ban37, 821-824. PubMed  Europe PubMed
  608. Durham,T.B. and Shepherd,T.A.
    Progress toward the discovery and development of efficacious BACE inhibitors
    Curr Opin Drug Discov Devel9, 776-791. PubMed  Europe PubMed  I
  609. [YEAR:10-1-2006]Garino,C., Pietrancosta,N., Laras,Y., Moret,V., Rolland,A., Quelever,G. and Kraus,J.L.
    BACE-1 inhibitory activities of new substituted phenyl-piperazine coupled to various heterocycles: chromene, coumarin and quinoline
    Bioorg Med Chem Lett16, 1995-1999. PubMed  Europe PubMed DOI  I
  610. [YEAR:13-7-2006]Garino,C., Tomita,T., Pietrancosta,N., Laras,Y., Rosas,R., Herbette,G., Maigret,B., Quelever,G., Iwatsubo,T. and Kraus,J.L.
    Naphthyl and coumarinyl biarylpiperazine derivatives as highly potent human beta-secretase inhibitors. Design, synthesis, and enzymatic BACE-1 and cell assays
    J Med Chem49, 4275-4285. PubMed  Europe PubMed DOI  I
  611. [YEAR:26-4-2006]Ghosh,A.K., Kumaragurubaran,N., Hong,L., Lei,H., Hussain,K.A., Liu,C.F., Devasamudram,T., Weerasena,V., Turner,R., Koelsch,G., Bilcer,G. and Tang,J.
    Design, synthesis and X-ray structure of protein-ligand complexes: important insight into selectivity of memapsin 2 (beta-secretase) inhibitors
    J Am Chem Soc128, 5310-5311. PubMed  Europe PubMed DOI  S  I
  612. Guo,T. and Hobbs,D.W.
    Development of BACE1 inhibitors for Alzheimer's disease
    Curr Med Chem13, 1811-1829. PubMed  Europe PubMed DOI  V  I
  613. [YEAR:3-6-2006]Hamada,Y., Igawa,N., Ikari,H., Ziora,Z., Nguyen,J.T., Yamani,A., Hidaka,K., Kimura,T., Saito,K., Hayashi,Y., Ebina,M., Ishiura,S. and Kiso,Y.
    beta-Secretase inhibitors: modification at the P4 position and improvement of inhibitory activity in cultured cells
    Bioorg Med Chem Lett16, 4354-4359. PubMed  Europe PubMed DOI  I
  614. [YEAR:27-7-2006]Hanessian,S., Yang,G., Rondeau,J.M., Neumann,U., Betschart,C. and Tintelnot-Blomley,M.
    Structure-based design and synthesis of macroheterocyclic peptidomimetic inhibitors of the aspartic protease beta-site amyloid precursor protein cleaving enzyme (BACE)
    J Med Chem49, 4544-4567. PubMed  Europe PubMed DOI  I
  615. Hu,H.T., Dong,W.J. and Feng,G.F.
    [Specific suppression of beta-secretase gene expression by short interfering RNA in mammalian cells]
    Zhejiang Da Xue Xue Bao Yi Xue Ban35, 622-629. PubMed  Europe PubMed
  616. John,V.
    Human beta-secretase (BACE) and BACE inhibitors: progress report
    Curr Top Med Chem6, 569-578. PubMed  Europe PubMed DOI  V  I
  617. [YEAR:13-2-2006]Kimura,T., Hamada,Y., Stochaj,M., Ikari,H., Nagamine,A., Abdel-Rahman,H., Igawa,N., Hidaka,K., Nguyen,J.T., Saito,K., Hayashi,Y. and Kiso,Y.
    Design and synthesis of potent beta-secretase (BACE1) inhibitors with P1' carboxylic acid bioisosteres
    Bioorg Med Chem Lett16, 2380-2386. PubMed  Europe PubMed DOI  I
  618. Larbig,G. and Schmidt,B.
    Synthesis of tetramic and tetronic acids as beta-secretase inhibitors
    J Comb Chem8, 480-490. PubMed  Europe PubMed DOI  I
  619. Maloney,B., Ge,Y.W., Greig,N.H. and Lahiri,D.K.
    Characterization of the human beta-secretase 2 (BACE2) 5'-flanking region: identification of a 268-bp region as the basal BACE2 promoter
    J Mol Neurosci29, 81-99. PubMed  Europe PubMed DOI
  620. [YEAR:5-10-2006]Moitessier,N., Therrien,E. and Hanessian,S.
    A method for induced-fit docking, scoring, and ranking of flexible ligands. Application to peptidic and pseudopeptidic beta-secretase (BACE 1) inhibitors
    J Med Chem49, 5885-5894. PubMed  Europe PubMed DOI  I
  621. [YEAR:14-12-2006]Rajapakse,H.A., Nantermet,P.G., Selnick,H.G., Munshi,S., McGaughey,G.B., Lindsley,S.R., Young,M.B., Lai,M.T., Espeseth,A.S., Shi,X.P., Colussi,D., Pietrak,B., Crouthamel,M.C., Tugusheva,K., Huang,Q., Xu,M., Simon,A.J., Kuo,L., Hazuda,D.J., Graham,S. and Vacca,J.P.
    Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1)
    J Med Chem49, 7270-7273. PubMed  Europe PubMed DOI  I
  622. [YEAR:21-10-2006]Rojo,I., Martin,J.A., Broughton,H., Timm,D., Erickson,J., Yang,H.C. and McCarthy,J.R.
    Macrocyclic peptidomimetic inhibitors of beta-secretase (BACE): first X-ray structure of a macrocyclic peptidomimetic-BACE complex
    Bioorg Med Chem Lett16, 191-195. PubMed  Europe PubMed DOI  S  I
  623. Schmidt,B., Baumann,S., Braun,H.A. and Larbig,G.
    Inhibitors and modulators of beta- and gamma-secretase
    Curr Top Med Chem6, 377-392. PubMed  Europe PubMed DOI  I
  624. [YEAR:19-10-2006]Stachel,S.J., Coburn,C.A., Sankaranarayanan,S., Price,E.A., Wu,G., Crouthamel,M., Pietrak,B.L., Huang,Q., Lineberger,J., Espeseth,A.S., Jin,L., Ellis,J., Holloway,M.K., Munshi,S., Allison,T., Hazuda,D., Simon,A.J., Graham,S.L. and Vacca,J.P.
    Macrocyclic inhibitors of beta-secretase: functional activity in an animal model
    J Med Chem49, 6147-6150. PubMed  Europe PubMed DOI  I
  625. [YEAR:13-4-2006]Verheijen,J.H., Huisman,L.G., van Lent,N., Neumann,U., Paganetti,P., Hack,C.E., Bouwman,F., Lindeman,J., Bollen,E.L. and Hanemaaijer,R.
    Detection of a soluble form of BACE-1 in human cerebrospinal fluid by a sensitive activity assay
    Clin Chem52, 1168-1174. PubMed  Europe PubMed DOI  A
  626. [YEAR:21-9-2006]Willem,M., Garratt,A.N., Novak,B., Citron,M., Kaufmann,S., Rittger,A., DeStrooper,B., Saftig,P., Birchmeier,C. and Haass,C.
    Control of peripheral nerve myelination by the beta-secretase BACE1
    Science314, 664-666. PubMed  Europe PubMed DOI  K
  627. [YEAR:27-2-2006]Xiao,K., Li,X., Li,J., Ma,L., Hu,B., Yu,H., Fu,Y., Wang,R., Ma,Z., Qiu,B., Li,J., Hu,D., Wang,X. and Shen,J.
    Design, synthesis, and evaluation of Leu*Ala hydroxyethylene-based non-peptide beta-secretase (BACE) inhibitors
    Bioorg Med Chem14, 4535-4551. PubMed  Europe PubMed DOI  I
  628. [YEAR:9-2-2006]Yang,W., Lu,W., Lu,Y., Zhong,M., Sun,J., Thomas,A.E., Wilkinson,J.M., Fucini,R.V., Lam,M., Randal,M., Shi,X.P., Jacobs,J.W., McDowell,R.S., Gordon,E.M. and Ballinger,M.D.
    Aminoethylenes: a tetrahedral intermediate isostere yielding potent inhibitors of the aspartyl protease BACE-1
    J Med Chem49, 839-842. PubMed  Europe PubMed DOI  S  I
  629. [YEAR:8-2-2006]Yoon,S.Y., Choi,J.E., Yoon,J.H., Huh,J.W. and Kim,D.H.
    BACE inhibitor reduces APP-beta-C-terminal fragment accumulation in axonal swellings of okadaic acid-induced neurodegeneration
    Neurobiol Dis22, 435-444. PubMed  Europe PubMed DOI
  630. Yu,N., Hayik,S.A., Wang,B., Liao,N., Reynolds,C.H. and Merz,K.M.
    Assigning the protonation states of the key aspartates in beta-secretase using QM/MM X-ray structure refinement
    J Chem Theory Comput2, 1057-1069. PubMed  Europe PubMed DOI  S
  631. 2005
  632. [YEAR:18-2-2005]Angeletti,B., Waldron,K.J., Freeman,K.B., Bawagan,H., Hussain,I., Miller,C.C., Lau,K.F., Tennant,M.E., Dennison,C., Robinson,N.J. and Dingwall,C.
    BACE1 cytoplasmic domain interacts with the copper chaperone for superoxide dismutase-1 and binds copper
    J Biol Chem280, 17930-17937. PubMed  Europe PubMed DOI
  633. [YEAR:4-8-2005]Byun,H.G., Kim,Y.T., Park,P.J., Lin,X.L. and Kim,S.K.
    Chitooligosaccharides as a novel beta-secretase inhibitor
    Carbohydr Polym61, 198-202.  I
  634. [YEAR:13-9-2005]Chang,K.H., Baek,N.I., Yang,J.M., Lee,J.M., Bo,J.H. and Chung,I.S.
    Expression and characterization of recombinant beta-secretase from Trichoplusia ni BTI Tn5B1-4 cells transformed with cDNAs encoding human beta1,4-galactosyltransferase and Gal beta1,4-GlcNAc alpha 2,6-sialytransferase
    Protein Expr Purif44, 87-93. PubMed  Europe PubMed DOI  E
  635. [YEAR:6-4-2005]Chang,K.H., Yang,J.M., Chun,H.O. and Chung,I.S.
    Enhanced activity of recombinant beta-secretase from Drosophila melanogaster S2 cells transformed with cDNAs encoding human beta1,4-galactosyltransferase and Galbeta1,4-GlcNAc alpha2,6-sialyltransferase
    J Biotechnol116, 359-367. PubMed  Europe PubMed DOI  E
  636. Ghosh,A.K., Kumaragurubaran,N. and Tang,J.
    Recent developments of structure based beta-secretase inhibitors for Alzheimer's disease
    Curr Top Med Chem5, 1609-1622. PubMed  Europe PubMed DOI  V  I
  637. [YEAR:3-1-2005]Ghosh,A.K., Devasamudram,T., Hong,L., DeZutter,C., Xu,X., Weerasena,V., Koelsch,G., Bilcer,G. and Tang,J.
    Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (beta-secretase)
    Bioorg Med Chem Lett15, 15-20. PubMed  Europe PubMed DOI  I
  638. Gorfe,A.A. and Caflisch,A.
    Functional plasticity in the substrate binding site of beta-secretase
    Structure13, 1487-1498. PubMed  Europe PubMed DOI
  639. [YEAR:11-8-2005]Hanessian,S., Yun,H., Hou,Y., Yang,G., Bayrakdarian,M., Therrien,E., Moitessier,N., Roggo,S., Veenstra,S., Tintelnot-Blomley,M., Rondeau,J.M., Ostermeier,C., Strauss,A., Ramage,P., Paganetti,P., Neumann,U. and Betschart,C.
    Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics
    J Med Chem48, 5175-5190. PubMed  Europe PubMed DOI  I
  640. [YEAR:21-12-2005]He,X., Li,F., Chang,W.P. and Tang,J.
    GGA proteins mediate the recycling pathway of memapsin 2 (BACE)
    J Biol Chem280, 11696-11703. PubMed  Europe PubMed DOI
  641. [YEAR:11-8-2005]Huang,D., Luthi,U., Kolb,P., Edler,K., Cecchini,M., Audetat,S., Barberis,A. and Caflisch,A.
    Discovery of cell-permeable non-peptide inhibitors of beta-secretase by high-throughput docking and continuum electrostatics calculations
    J Med Chem48, 5108-5111. PubMed  Europe PubMed DOI  I
  642. [YEAR:22-8-2005]Kalvodova,L., Kahya,N., Schwille,P., Ehehalt,R., Verkade,P., Drechsel,D. and Simons,K.
    Lipids as modulators of proteolytic activity of BACE: involvement of cholesterol, glycosphingolipids, and anionic phospholipids in vitro
    J Biol Chem280, 36815-36823. PubMed  Europe PubMed DOI
  643. [YEAR:3-1-2005]Kimura,T., Shuto,D., Hamada,Y., Igawa,N., Kasai,S., Liu,P., Hidaka,K., Hamada,T., Hayashi,Y. and Kiso,Y.
    Design and synthesis of highly active Alzheimer's beta-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability
    Bioorg Med Chem Lett15, 211-215. PubMed  Europe PubMed DOI  I
  644. [YEAR:13-9-2005]Kitazume,S., Nakagawa,K., Oka,R., Tachida,Y., Ogawa,K., Luo,Y., Citron,M., Shitara,H., Taya,C., Yonekawa,H., Paulson,J.C., Miyoshi,E., Taniguchi,N. and Hashimoto,Y.
    In vivo cleavage of alpha2,6-sialyltransferase by Alzheimer beta-secretase
    J Biol Chem280, 8589-8595. PubMed  Europe PubMed DOI
  645. [YEAR:30-8-2005]Kornacker,M.G., Lai,Z., Witmer,M., Ma,J., Hendrick,J., Lee,V.G., Riexinger,D.J., Mapelli,C., Metzler,W. and Copeland,R.A.
    An inhibitor binding pocket distinct from the catalytic active site on human beta-APP cleaving enzyme
    Biochemistry44, 11567-11573. PubMed  Europe PubMed DOI
  646. [YEAR:14-12-2005]Laird,F.M., Cai,H., Savonenko,A.V., Farah,M.H., He,K., Melnikova,T., Wen,H., Chiang,H.C., Xu,G., Koliatsos,V.E., Borchelt,D.R., Price,D.L., Lee,H.K. and Wong,P.C.
    BACE1, a major determinant of selective vulnerability of the brain to amyloid-beta amyloidogenesis, is essential for cognitive, emotional, and synaptic functions
    J Neurosci25, 11693-11709. PubMed  Europe PubMed DOI  K
  647. [YEAR:17-1-2005]Lee,E.B., Zhang,B., Liu,K., Greenbaum,E.A., Doms,R.W., Trojanowski,J.Q. and Lee,V.M.
    BACE overexpression alters the subcellular processing of APP and inhibits Abeta deposition in vivo
    J Cell Biol168, 291-302. PubMed  Europe PubMed DOI  K
  648. [YEAR:7-3-2005]Lefranc-Jullien,S., Lisowski,V., Hernandez,J.F., Martinez,J. and Checler,F.
    Design and characterization of a new cell-permeant inhibitor of the beta-secretase BACE1
    Br J Pharmacol145, 228-235. PubMed  Europe PubMed DOI  I
  649. [YEAR:1-7-2005]Pietrak,B.L., Crouthamel,M.C., Tugusheva,K., Lineberger,J.E., Xu,M., DiMuzio,J.M., Steele,T., Espeseth,A.S., Stachel,S.J., Coburn,C.A., Graham,S.L., Vacca,J.P., Shi,X.P., Simon,A.J., Hazuda,D.J. and Lai,M.T.
    Biochemical and cell-based assays for characterization of BACE-1 inhibitors
    Anal Biochem342, 144-151. PubMed  Europe PubMed DOI  A
  650. [YEAR:2-6-2005]Polgar,T. and Keseru,G.M.
    Virtual screening for beta-secretase (BACE1) inhibitors reveals the importance of protonation states at Asp32 and Asp228
    J Med Chem48, 3749-3755. PubMed  Europe PubMed DOI  I
  651. Porcari,V., Magnoni,L., Terstappen,G.C. and Fecke,W.
    A continuous time-resolved fluorescence assay for identification of BACE1 inhibitors
    Assay Drug Dev Technol3, 287-297. PubMed  Europe PubMed DOI  A
  652. Rossner,S., Lange-Dohna,C., Zeitschel,U. and Perez-Polo,J.R.
    Alzheimer's disease beta-secretase BACE1 is not a neuron-specific enzyme
    J Neurochem92, 226-234. PubMed  Europe PubMed DOI
  653. Tang,J., He,X., Huang,X. and Hong,L.
    Recent developments on the studies of human memapsin 2 (beta-secretase)
    Curr Alzheimer Res2, 261-264. PubMed  Europe PubMed DOI  V
  654. Thompson,L.A., Bronson,J.J. and Zusi,F.C.
    Progress in the discovery of BACE inhibitors
    Curr Pharm Des11, 3383-3404. PubMed  Europe PubMed DOI  V  I
  655. Tong,Y., Zhou,W., Fung,V., Christensen,M.A., Qing,H., Sun,X. and Song,W.
    Oxidative stress potentiates BACE1 gene expression and Abeta generation
    J Neural Transm (Vienna)112, 455-469. PubMed  Europe PubMed DOI
  656. [YEAR:11-1-2005]Turner,R.T., III, Hong,L., Koelsch,G., Ghosh,A.K. and Tang,J.
    Structural locations and functional roles of new subsites S5, S6, and S7 in memapsin 2 (beta-secretase)
    Biochemistry44, 105-112. PubMed  Europe PubMed DOI
  657. Vassar,R.
    beta-Secretase, APP and Abeta in Alzheimer's disease
    Subcell Biochem38, 79-103. PubMed  Europe PubMed
  658. [YEAR:4-3-2005]von Arnim,C.A., Kinoshita,A., Peltan,I.D., Tangredi,M.M., Herl,L., Lee,B.M., Spoelgen,R., Hshieh,T.T., Ranganathan,S., Battey,F.D., Liu,C.X., Bacskai,B.J., Sever,S., Irizarry,M.C., Strickland,D.K. and Hyman,B.T.
    The low density lipoprotein receptor-related protein (LRP) is a novel beta-secretase (BACE1) substrate
    J Biol Chem280, 17777-17785. PubMed  Europe PubMed DOI
  659. Wong,H.K., Sakurai,T., Oyama,F., Kaneko,K., Wada,K., Miyazaki,H., Kurosawa,M., De Strooper,B., Saftig,P. and Nukina,N.
    beta Subunits of voltage-gated sodium channels are novel substrates of beta-site amyloid precursor protein-cleaving enzyme (BACE1) and gamma-secretase
    J Biol Chem280, 23009-23017. PubMed  Europe PubMed DOI
  660. [YEAR:15-3-2005]Zuo,Z., Luo,X., Zhu,W., Shen,J., Shen,X., Jiang,H. and Chen,K.
    Molecular docking and 3D-QSAR studies on the binding mechanism of statine-based peptidomimetics with beta-secretase
    Bioorg Med Chem13, 2121-2131. PubMed  Europe PubMed DOI  I
  661. 2004
  662. [YEAR:9-2-2004]Brady,S.F., Singh,S., Crouthamel,M.C., Holloway,M.K., Coburn,C.A., Garsky,V.M., Bogusky,M., Pennington,M.W., Vacca,J.P., Hazuda,D. and Lai,M.T.
    Rational design and synthesis of selective BACE-1 inhibitors
    Bioorg Med Chem Lett14, 601-604. PubMed  Europe PubMed DOI  I
  663. Chang,W.P., Koelsch,G., Wong,S., Downs,D., Da,H., Weerasena,V., Gordon,B., Devasamudram,T., Bilcer,G., Ghosh,A.K. and Tang,J.
    In vivo inhibition of Abeta production by memapsin 2 (beta-secretase) inhibitors
    J Neurochem89, 1409-1416. PubMed  Europe PubMed DOI  I
  664. [YEAR:27-9-2004]Chiocco,M.J., Kulnane,L.S., Younkin,L., Younkin,S., Evin,G. and Lamb,B.T.
    Altered amyloid-beta metabolism and deposition in genomic-based beta-secretase transgenic mice
    J Biol Chem279, 52535-52542. PubMed  Europe PubMed DOI
  665. Christensen,M.A., Zhou,W., Qing,H., Lehman,A., Philipsen,S. and Song,W.
    Transcriptional regulation of BACE1, the beta-amyloid precursor protein beta-secretase, by Sp1
    Mol Cell Biol24, 865-874. PubMed  Europe PubMed DOI
  666. Citron,M.
    Beta-secretase inhibition for the treatment of Alzheimer's disease - promise and challenge
    Trends Pharmacol Sci25, 92-97. PubMed  Europe PubMed DOI
  667. [YEAR:2-12-2004]Coburn,C.A., Stachel,S.J., Li,Y.M., Rush,D.M., Steele,T.G., Chen-Dodson,E., Holloway,M.K., Xu,M., Huang,Q., Lai,M.T., Dimuzio,J., Crouthamel,M.C., Shi,X.P., Sardana,V., Chen,Z., Munshi,S., Kuo,L., Makara,G.M., Annis,D.A., Tadikonda,P.K., Nash,H.M., Vacca,J.P. and Wang,T.
    Identification of a small molecule nonpeptide active site beta-secretase inhibitor that displays a nontraditional binding mode for aspartyl proteases
    J Med Chem47, 6117-6119. PubMed  Europe PubMed DOI  I
  668. Cumming,J.N., Iserloh,U. and Kennedy,M.E.
    Design and development of BACE-1 inhibitors
    Curr Opin Drug Discov Devel7, 536-556. PubMed  Europe PubMed  I
  669. Dominguez,D.I., Hartmann,D. and De Strooper,B.
    BACE1 and presenilin: two unusual aspartyl proteases involved in Alzheimer's disease
    Neurodegener Dis1, 168-174. PubMed  Europe PubMed DOI
  670. [YEAR:1-4-2004]Ge,Y.W., Maloney,B., Sambamurti,K. and Lahiri,D.K.
    Functional characterization of the 5' flanking region of the BACE gene: identification of a 91 bp fragment involved in basal level of BACE promoter expression
    FASEB J18, 1037-1039. PubMed  Europe PubMed DOI
  671. [YEAR:1-1-2004]Hom,R.K., Gailunas,A.F., Mamo,S., Fang,L.Y., Tung,J.S., Walker,D.E., Davis,D., Thorsett,E.D., Jewett,N.E., Moon,J.B. and John,V.
    Design and synthesis of hydroxyethylene-based peptidomimetic inhibitors of human beta-secretase
    J Med Chem47, 158-164. PubMed  Europe PubMed DOI  I
  672. [YEAR:27-4-2004]Hong,L. and Tang,J.
    Flap position of free memapsin 2 (beta-secretase), a model for flap opening in aspartic protease catalysis
    Biochemistry43, 4689-4695. PubMed  Europe PubMed DOI  S
  673. [YEAR:5-7-2004]Hu,B., Fan,K.Y., Bridges,K., Chopra,R., Lovering,F., Cole,D., Zhou,P., Ellingboe,J., Jin,G., Cowling,R. and Bard,J.
    Synthesis and SAR of bis-statine based peptides as BACE 1 inhibitors
    Bioorg Med Chem Lett14, 3457-3460. PubMed  Europe PubMed DOI  I
  674. Hussain,I.
    The potential for BACE1 inhibitors in the treatment of Alzheimer's disease
    IDrugs7, 653-658. PubMed  Europe PubMed  I
  675. [YEAR:22-3-2004]Kimura,T., Shuto,D., Kasai,S., Liu,P., Hidaka,K., Hamada,T., Hayashi,Y., Hattori,C., Asai,M., Kitazume,S., Saido,T.C., Ishiura,S. and Kiso,Y.
    KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine
    Bioorg Med Chem Lett14, 1527-1531. PubMed  Europe PubMed DOI  I
  676. Kitazume,S., Suzuki,M., Saido,T.C. and Hashimoto,Y.
    Involvement of proteases in glycosyltransferase secretion: Alzheimer's beta-secretase-dependent cleavage and a following processing by an aminopeptidase
    Glycoconj J21, 25-29. PubMed  Europe PubMed DOI
  677. Kitazume,S., Saido,T.C. and Hashimoto,Y.
    Alzheimer's beta-secretase cleaves a glycosyltransferase as a physiological substrate
    Glycoconj J20, 59-62. PubMed  Europe PubMed DOI
  678. [YEAR:5-1-2004]Lamar,J., Hu,J., Bueno,A.B., Yang,H.C., Guo,D., Copp,J.D., McGee,J., Gitter,B., Timm,D., May,P., McCarthy,J. and Chen,S.H.
    Phe*-Ala-based pentapeptide mimetics are BACE inhibitors: P2 and P3 SAR
    Bioorg Med Chem Lett14, 239-243. PubMed  Europe PubMed DOI  I
  679. Lammich,S., Schobel,S., Zimmer,A.K., Lichtenthaler,S.F. and Haass,C.
    Expression of the Alzheimer protease BACE1 is suppressed via its 5'-untranslated region
    EMBO Rep5, 620-625. PubMed  Europe PubMed DOI
  680. [YEAR:29-12-2004]Li,Q. and Sudhof,T.C.
    Cleavage of amyloid-beta precursor protein and amyloid-beta precursor-like protein by BACE 1
    J Biol Chem279, 10542-10550. PubMed  Europe PubMed DOI
  681. Liu,D., Wang,Y.S., Gesell,J.J., Wilson,E., Beyer,B.M. and Wyss,D.F.
    Backbone resonance assignments of the 45.3 kDa catalytic domain of human BACE1
    J Biomol NMR29, 425-426. PubMed  Europe PubMed DOI
  682. Mohajeri,M.H., Saini,K.D. and Nitsch,R.M.
    Transgenic BACE expression in mouse neurons accelerates amyloid plaque pathology
    J Neural Transm111, 413-425. PubMed  Europe PubMed DOI
  683. [YEAR:8-1-2004]Ohno,M., Sametsky,E.A., Younkin,L.H., Oakley,H., Younkin,S.G., Citron,M., Vassar,R. and Disterhoft,J.F.
    BACE1 deficiency rescues memory deficits and cholinergic dysfunction in a mouse model of Alzheimer's disease
    Neuron41, 27-33. PubMed  Europe PubMed DOI
  684. Pastorino,L., Ikin,A.F., Lamprianou,S., Vacaresse,N., Revelli,J.P., Platt,K., Paganetti,P., Mathews,P.M., Harroch,S. and Buxbaum,J.D.
    BACE (beta-secretase) modulates the processing of APLP2 in vivo
    Mol Cell Neurosci25, 642-649. PubMed  Europe PubMed DOI
  685. [YEAR:15-10-2004]Patel,S., Vuillard,L., Cleasby,A., Murray,C.W. and Yon,J.
    Apo and inhibitor complex structures of BACE (beta-secretase)
    J Mol Biol343, 407-416. PubMed  Europe PubMed DOI  S  I
  686. [YEAR:10-9-2004]Qahwash,I., He,W., Tomasselli,A., Kletzien,R.F. and Yan,R.
    Processing amyloid precursor protein at the beta-site requires proper orientation to be accessed by BACE1
    J Biol Chem279, 39010-39016. PubMed  Europe PubMed DOI
  687. Qing,H., Zhou,W., Christensen,M.A., Sun,X., Tong,Y. and Song,W.
    Degradation of BACE by the ubiquitin-proteasome pathway
    FASEB J18, 1571-1573. PubMed  Europe PubMed DOI
  688. [YEAR:7-10-2004]Rajamani,R. and Reynolds,C.H.
    Modeling the protonation states of the catalytic aspartates in beta-secretase
    J Med Chem47, 5159-5166. PubMed  Europe PubMed DOI
  689. [YEAR:2-3-2004]Rogers,G.W., Jr., Edelman,G.M. and Mauro,V.P.
    Differential utilization of upstream AUGs in the beta-secretase mRNA suggests that a shunting mechanism regulates translation
    Proc Natl Acad Sci U S A101, 2794-2799. PubMed  Europe PubMed DOI
  690. [YEAR:1-4-2004]Sambamurti,K., Kinsey,R., Maloney,B., Ge,Y.W. and Lahiri,D.K.
    Gene structure and organization of the human beta-secretase (BACE) promoter
    FASEB J18, 1034-1036. PubMed  Europe PubMed DOI
  691. Sardana,V., Xu,B., Zugay-Murphy,J., Chen,Z., Sardana,M., Darke,P.L., Munshi,S. and Kuo,L.C.
    A general procedure for the purification of human beta-secretase expressed in Escherichia coli
    Protein Expr Purif34, 190-196. PubMed  Europe PubMed DOI
  692. Shiba,T., Kametaka,S., Kawasaki,M., Shibata,M., Waguri,S., Uchiyama,Y. and Wakatsuki,S.
    Insights into the phosphoregulation of beta-secretase sorting signal by the VHS domain of GGA1
    Traffic5, 437-448. PubMed  Europe PubMed DOI
  693. [YEAR:16-12-2004]Stachel,S.J., Coburn,C.A., Steele,T.G., Jones,K.G., Loutzenhiser,E.F., Gregro,A.R., Rajapakse,H.A., Lai,M.T., Crouthamel,M.C., Xu,M., Tugusheva,K., Lineberger,J.E., Pietrak,B.L., Espeseth,A.S., Shi,X.P., Chen-Dodson,E., Holloway,M.K., Munshi,S., Simon,A.J., Kuo,L. and Vacca,J.P.
    Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1)
    J Med Chem47, 6447-6450. PubMed  Europe PubMed DOI  I
  694. Tang,J. and Koelsch,G.
    Memapsin 2
    [ISSN:0-12-079610-4]2, 66-69.  V
  695. Vassar,R.
    BACE1: the beta-secretase enzyme in Alzheimer's disease
    J Mol Neurosci23, 105-114. PubMed  Europe PubMed DOI  K
  696. [YEAR:15-10-2004]von Arnim,C.A., Tangredi,M.M., Peltan,I.D., Lee,B.M., Irizarry,M.C., Kinoshita,A. and Hyman,B.T.
    Demonstration of BACE (beta-secretase) phosphorylation and its interaction with GGA1 in cells by fluorescence-lifetime imaging microscopy
    J Cell Sci117, 5437-5445. PubMed  Europe PubMed DOI
  697. [YEAR:6-5-2004]Wang,W., Reichert,P., Beyer,B.M., Liu,J.J., Lee,J., Zhang,L., Liu,Y.H., Taremi,S.S., Le,H.V. and Strickland,C.
    Crystallization of glycosylated human BACE protease domain expressed in Trichoplusia ni
    Biochim Biophys Acta1698, 255-259. PubMed  Europe PubMed DOI
  698. [YEAR:12-10-2004]Westmeyer,G.G., Willem,M., Lichtenthaler,S.F., Lurman,G., Multhaup,G., Assfalg-Machleidt,I., Reiss,K., Saftig,P. and Haass,C.
    Dimerization of beta-site beta-amyloid precursor protein-cleaving enzyme
    J Biol Chem279, 53205-53212. PubMed  Europe PubMed DOI
  699. Willem,M., Dewachter,I., Smyth,N., Van Dooren,T., Borghgraef,P., Haass,C. and Van Leuven,F.
    beta-Site amyloid precursor protein cleaving enzyme 1 increases amyloid deposition in brain parenchyma but reduces cerebrovascular amyloid angiopathy in aging BACE x APP[V717I] double-transgenic mice
    Am J Pathol165, 1621-1631. PubMed  Europe PubMed  K
  700. Xiong,B., Huang,X.Q., Shen,L.L., Shen,J.H., Luo,X.M., Shen,X., Jiang,H.L. and Chen,K.X.
    Conformational flexibility of beta-secretase: molecular dynamics simulation and essential dynamics analysis
    Acta Pharmacol Sin25, 705-713. PubMed  Europe PubMed
  701. [YEAR:3-12-2004]Yamamoto,R., Yoneda,S. and Hara,H.
    Neuroprotective effects of beta-secretase inhibitors against rat retinal ganglion cell death
    Neurosci Lett370, 61-64. PubMed  Europe PubMed DOI  I
  702. Yang,H.C., Chai,X., Mosior,M., Kohn,W., Boggs,L.N., Erickson,J.A., McClure,D.B., Yeh,W.K., Zhang,L., Gonzalez-DeWhitt,P., Mayer,J.P., Martin,J.A., Hu,J., Chen,S.H., Bueno,A.B., Little,S.P., McCarthy,J.R. and May,P.C.
    Biochemical and kinetic characterization of BACE1: investigation into the putative species-specificity for beta- and beta'-cleavage sites by human and murine BACE1
    J Neurochem91, 1249-1259. PubMed  Europe PubMed DOI
  703. Zhou,W., Qing,H., Tong,Y. and Song,W.
    BACE1 Gene Expression and Protein Degradation
    Ann N Y Acad Sci1035, 49-67. PubMed  Europe PubMed DOI
  704. 2003
  705. [YEAR:11-7-2003]Andrau,D., Dumanchin-Njock,C., Ayral,E., Vizzavona,J., Farzan,M., Boisbrun,M., Fulcrand,P., Hernandez,J.F., Martinez,J., Lefranc-Jullien,S. and Checler,F.
    BACE1- and BACE2-expressing human cells: characterization of beta-amyloid precursor protein-derived catabolites, design of a novel fluorimetric assay, and identification of new in vitro inhibitors
    J Biol Chem278, 25859-25866. PubMed  Europe PubMed DOI  A
  706. Basi,G., Frigon,N., Barbour,R., Doan,T., Gordon,G., McConlogue,L., Sinha,S. and Zeller,M.
    Antagonistic effects of beta-site amyloid precursor protein-cleaving enzymes 1 and 2 on beta-amyloid peptide production in cells
    J Biol Chem278, 31512-31520. PubMed  Europe PubMed DOI
  707. [YEAR:15-5-2003]Gold,G., Blouin,J.L., Herrmann,F.R., Michon,A., Mulligan,R., Duriaux Sail,G., Bouras,C., Giannakopoulos,P. and Antonarakis,S.E.
    Specific BACE1 genotypes provide additional risk for late-onset alzheimer disease in APOE epsilon 4 carriers
    Am J Med Genet B Neuropsychiatr Genet119B, 44-47. PubMed  Europe PubMed DOI  M
  708. Harrison,S.M., Harper,A.J., Hawkins,J., Duddy,G., Grau,E., Pugh,P.L., Winter,P.H., Shilliam,C.S., Hughes,Z.A., Dawson,L.A., Gonzalez,M.I., Upton,N., Pangalos,M.N. and Dingwall,C.
    BACE1 (beta-secretase) transgenic and knockout mice: identification of neurochemical deficits and behavioral changes
    Mol Cell Neurosci24, 646-655. PubMed  Europe PubMed DOI
  709. [YEAR:28-10-2003]He,X., Zhu,G., Koelsch,G., Rodgers,K.K., Zhang,X.C. and Tang,J.
    Biochemical and structural characterization of the interaction of memapsin 2 (beta-secretase) cytosolic domain with the VHS domain of GGA proteins
    Biochemistry42, 12174-12180. PubMed  Europe PubMed DOI
  710. [YEAR:1-11-2003]Hook,V.Y. and Reisine,T.D.
    Cysteine proteases are the major beta-secretase in the regulated secretory pathway that provides most of the beta-amyloid in Alzheimer's disease: role of BACE 1 in the constitutive secretory pathway
    J Neurosci Res74, 393-405. PubMed  Europe PubMed DOI
  711. [YEAR:9-5-2003]Huse,J.T., Byant,D., Yang,Y., Pijak,D.S., D'Souza,I., Lah,J.J., Lee,V.M., Doms,R.W. and Cook,D.G.
    Endoproteolysis of beta-secretase (beta-site amyloid precursor protein-cleaving enzyme) within its catalytic domain. A potential mechanism for regulation
    J Biol Chem278, 17141-17149. PubMed  Europe PubMed DOI
  712. [YEAR:19-9-2003]Hussain,I., Hawkins,J., Shikotra,A., Riddell,D.R., Faller,A. and Dingwall,C.
    Characterization of the ectodomain shedding of the beta-site amyloid precursor protein-cleaving enzyme 1 (BACE1)
    J Biol Chem278, 36264-36268. PubMed  Europe PubMed DOI
  713. [YEAR:23-10-2003]John,V., Beck,J.P., Bienkowski,M.J., Sinha,S. and Heinrikson,R.L.
    Human beta-secretase (BACE) and BACE inhibitors
    J Med Chem46, 4625-4630. PubMed  Europe PubMed DOI  V  I
  714. [YEAR:1-8-2003]Kennedy,M.E., Wang,W., Song,L., Lee,J., Zhang,L., Wong,G., Wang,L. and Parker,E.
    Measuring human beta-secretase (BACE1) activity using homogeneous time-resolved fluorescence
    Anal Biochem319, 49-55. PubMed  Europe PubMed DOI  A  I
  715. [YEAR:1-7-2003]Kirschling,C.M., Kolsch,H., Frahnert,C., Rao,M.L., Maier,W. and Heun,R.
    Polymorphism in the BACE gene influences the risk for Alzheimer's disease
    Neuroreport14, 1243-1246. PubMed  Europe PubMed DOI  M
  716. [YEAR:25-4-2003]Kitazume,S., Tachida,Y., Oka,R., Kotani,N., Ogawa,K., Suzuki,M., Dohmae,N., Takio,K., Saido,T.C. and Hashimoto,Y.
    Characterization of alpha 2,6-sialyltransferase cleavage by Alzheimer's beta -secretase (BACE1)
    J Biol Chem278, 14865-14871. PubMed  Europe PubMed DOI
  717. [YEAR:1-7-2003]Lange-Dohna,C., Zeitschel,U., Gaunitz,F., Perez-Polo,J.R., Bigl,V. and Rossner,S.
    Cloning and expression of the rat BACE1 promoter
    J Neurosci Res73, 73-80. PubMed  Europe PubMed DOI
  718. Lichtenthaler,S.F., Dominguez,D.I., Westmeyer,G.G., Reiss,K., Haass,C., Saftig,P., De Strooper,B. and Seed,B.
    The cell adhesion protein P-selectin glycoprotein ligand-1 is a substrate for the aspartyl protease BACE1
    J Biol Chem278, 48713-48719. PubMed  Europe PubMed DOI
  719. Marlow,L., Cain,M., Pappolla,M.A. and Sambamurti,K.
    Beta-secretase processing of the Alzheimer's amyloid protein precursor (APP)
    J Mol Neurosci20, 233-239. PubMed  Europe PubMed DOI
  720. [YEAR:31-12-2003]Park,H. and Lee,S.
    Determination of the active site protonation state of beta-secretase from molecular dynamics simulation and docking experiment: implications for structure-based inhibitor design
    J Am Chem Soc125, 16416-16422. PubMed  Europe PubMed DOI  I
  721. [YEAR:13-10-2003]Scholefield,Z., Yates,E.A., Wayne,G., Amour,A., McDowell,W. and Turnbull,J.E.
    Heparan sulfate regulates amyloid precursor protein processing by BACE1, the Alzheimer's beta-secretase
    J Cell Biol163, 97-107. PubMed  Europe PubMed DOI
  722. Tamagno,E., Guglielmotto,M., Bardini,P., Santoro,G., Davit,A., Di Simone,D., Danni,O. and Tabaton,M.
    Dehydroepiandrosterone reduces expression and activity of BACE in NT2 neurons exposed to oxidative stress
    Neurobiol Dis14, 291-301. PubMed  Europe PubMed DOI
  723. Tang,J., Ghosh,A.K., Hong,L., Koelsch,G., Turner,R.T., III and Chang,W.
    Study of memapsin 2 (beta-secretase) and strategy of inhibitor design
    J Mol Neurosci20, 299-304. PubMed  Europe PubMed DOI  I
  724. Tomasselli,A.G., Qahwash,I., Emmons,T.L., Lu,Y., Leone,J.W., Lull,J.M., Fok,K.F., Bannow,C.A., Smith,C.W., Bienkowski,M.J., Heinrikson,R.L. and Yan,R.
    Employing a superior BACE1 cleavage sequence to probe cellular APP processing
    J Neurochem84, 1006-1017. PubMed  Europe PubMed DOI
  725. [YEAR:14-2-2003]Toulokhonova,L., Metzler,W.J., Witmer,M.R., Copeland,R.A. and Marcinkeviciene,J.
    Kinetic studies on beta-site amyloid precursor protein-cleaving enzyme (BACE). Confirmation of an iso mechanism
    J Biol Chem278, 4582-4589. PubMed  Europe PubMed DOI  I
  726. [YEAR:22-5-2003]Tounge,B.A. and Reynolds,C.H.
    Calculation of the binding affinity of beta-secretase inhibitors using the linear interaction energy method
    J Med Chem46, 2074-2082. PubMed  Europe PubMed DOI  I
  727. Vattemi,G., Engel,W.K., McFerrin,J., Pastorino,L., Buxbaum,J.D. and Askanas,V.
    BACE1 and BACE2 in pathologic and normal human muscle
    Exp Neurol179, 150-158. PubMed  Europe PubMed DOI
  728. [YEAR:4-7-2003]Zohar,O., Cavallaro,S., D'Agata,V. and Alkon,D.L.
    Quantification and distribution of beta-secretase alternative splice variants in the rat and human brain
    Brain Res Mol Brain Res115, 63-68. PubMed  Europe PubMed DOI  R
  729. 2002
  730. Bodendorf,U., Danner,S., Fischer,F., Stefani,M., Sturchler-Pierrat,C., Wiederhold,K.H., Staufenbiel,M. and Paganetti,P.
    Expression of human beta-secretase in the mouse brain increases the steady-state level of beta-amyloid
    J Neurochem80, 799-806. PubMed  Europe PubMed DOI
  731. Bruinzeel,W., Yon,J., Giovannelli,S. and Masure,S.
    Recombinant insect cell expression and purification of human beta-secretase (BACE-1) for X-ray crystallography
    Protein Expr Purif26, 139-148. PubMed  Europe PubMed DOI
  732. [YEAR:5-4-2002]Chou,K.C. and Howe,W.J.
    Prediction of the tertiary structure of the beta-secretase zymogen
    Biochem Biophys Res Commun292, 702-708. PubMed  Europe PubMed DOI
  733. [YEAR:1-11-2002]Citron,M.
    Beta-secretase as a target for the treatment of Alzheimer's disease
    J Neurosci Res70, 373-379. PubMed  Europe PubMed DOI  K
  734. [YEAR:26-4-2002]Ehehalt,R., Michel,B., De Pietri Tonelli,D., Zacchetti,D., Simons,K. and Keller,P.
    Splice variants of the beta-site APP-cleaving enzyme BACE1 in human brain and pancreas
    Biochem Biophys Res Commun293, 30-37. PubMed  Europe PubMed DOI  R
  735. Fischer,F., Molinari,M., Bodendorf,U. and Paganetti,P.
    The disulphide bonds in the catalytic domain of BACE are critical but not essential for amyloid precursor protein processing activity
    J Neurochem80, 1079-1088. PubMed  Europe PubMed DOI
  736. Ghosh,A.K., Hong,L. and Tang,J.
    beta-Secretase as a therapeutic target for inhibitor drugs
    Curr Med Chem9, 1135-1144. PubMed  Europe PubMed  I
  737. [YEAR:15-2-2002]Gruninger-Leitch,F., Schlatter,D., Kung,E., Nelbock,P. and Dobeli,H.
    Substrate and inhibitor profile of BACE (beta-secretase) and comparison with other mammalian aspartic proteases
    J Biol Chem277, 4687-4693. PubMed  Europe PubMed DOI  P  I
  738. [YEAR:31-7-2002]He,X., Chang,W.P., Koelsch,G. and Tang,J.
    Memapsin 2 (beta-secretase) cytosolic domain binds to the VHS domains of GGA1 and GGA2: implications on the endocytosis mechanism of memapsin 2
    FEBS Lett524, 183-187. PubMed  Europe PubMed DOI
  739. Hong,L., Turner,R.T., III, Koelsch,G., Ghosh,A.K. and Tang,J.
    Memapsin 2 (beta-secretase) as a therapeutic target
    Biochem Soc Trans30, 530-534. PubMed  Europe PubMed DOI  I
  740. [YEAR:10-9-2002]Hong,L., Turner,R.T., III, Koelsch,G., Shin,D., Ghosh,A.K. and Tang,J.
    Crystal structure of memapsin 2 (beta-secretase) in complex with an inhibitor OM00-3
    Biochemistry41, 10963-10967. PubMed  Europe PubMed DOI  S  I
  741. [YEAR:5-3-2002]Liu,K., Doms,R.W. and Lee,V.M.
    Glu11 site cleavage and N-terminally truncated A beta production upon BACE overexpression
    Biochemistry41, 3128-3136. PubMed  Europe PubMed DOI
  742. Pastorino,L., Ikin,A.F., Nairn,A.C., Pursnani,A. and Buxbaum,J.D.
    The carboxyl-terminus of BACE contains a sorting signal that regulates BACE trafficking but not the formation of total A(beta)
    Mol Cell Neurosci19, 175-185. PubMed  Europe PubMed DOI
  743. [YEAR:17-1-2002]Tung,J.S., Davis,D.L., Anderson,J.P., Walker,D.E., Mamo,S., Jewett,N., Hom,R.K., Sinha,S., Thorsett,E.D. and John,V.
    Design of substrate-based inhibitors of human beta-secretase
    J Med Chem45, 259-262. PubMed  Europe PubMed DOI  I
  744. [YEAR:9-7-2002]Turner,R.T., III, Loy,J.A., Nguyen,C., Devasamudram,T., Ghosh,A.K., Koelsch,G. and Tang,J.
    Specificity of memapsin 1 and its implications on the design of memapsin 2 (beta-secretase) inhibitor selectivity
    Biochemistry41, 8742-8746. PubMed  Europe PubMed DOI  P  I
  745. [YEAR:7-12-2002]Vassar,R.
    beta-Secretase (BACE) as a drug target for Alzheimer's disease
    Adv Drug Deliv Rev54, 1589-1602. PubMed  Europe PubMed DOI
  746. 2001
  747. [YEAR:6-4-2001]Benjannet,S., Elagoz,A., Wickham,L., Mamarbachi,M., Munzer,J.S., Basak,A., Lazure,C., Cromlish,J.A., Sisodia,S., Checler,F., Chretien,M. and Seidah,N.G.
    Post-translational processing of beta-secretase (beta-amyloid-converting enzyme) and its ectodomain shedding. The pro- and transmembrane/cytosolic domains affect its cellular activity and amyloid-beta production
    J Biol Chem276, 10879-10887. PubMed  Europe PubMed DOI
  748. [YEAR:13-4-2001]Bodendorf,U., Fischer,F., Bodian,D., Multhaup,G. and Paganetti,P.
    A splice variant of beta-secretase deficient in the amyloidogenic processing of the amyloid precursor protein
    J Biol Chem276, 12019-12023. PubMed  Europe PubMed DOI
  749. Cai,H.B., Wang,Y.S., McCarthy,D., Wen,H.J., Borchelt,D.R., Price,D.L. and Wong,P.C.
    BACE1 is the major beta-secretase for generation of Abeta peptides by neurons
    Nat Neurosci4, 233-234. PubMed  Europe PubMed DOI
  750. Charlwood,J., Dingwall,C., Matico,R., Hussain,I., Johanson,K., Moore,S., Powell,D.J., Skehel,J.M., Ratcliffe,S., Clarke,B., Trill,J., Sweitzer,S. and Camilleri,P.
    Characterization of the glycosylation profiles of Alzheimer's beta-secretase protein Asp-2 expressed in a variety of cell lines
    J Biol Chem276, 16739-16748. PubMed  Europe PubMed DOI
  751. [YEAR:9-2-2001]Creemers,J.W., Ines Dominguez,D., Plets,E., Serneels,L., Taylor,N.A., Multhaup,G., Craessaerts,K., Annaert,W. and De Strooper,B.
    Processing of beta-secretase by furin and other members of the proprotein convertase family
    J Biol Chem276, 4211-4217. PubMed  Europe PubMed DOI
  752. [YEAR:2-11-2001]Cruts,M., Dermaut,B., Rademakers,R., Roks,G., Van den Broeck,M., Munteanu,G., van Duijn,C.M. and Van Broeckhoven,C.V.
    Amyloid beta secretase gene (BACE) is neither mutated in nor associated with early-onset Alzheimer's disease
    Neurosci Lett313, 105-107. PubMed  Europe PubMed DOI
  753. Dominguez,D.I., De Strooper,B. and Annaert,W.
    Secretases as therapeutic targets for the treatment of Alzheimer's disease
    Amyloid8, 124-142. PubMed  Europe PubMed
  754. [YEAR:24-8-2001]Esler,W.P. and Wolfe,M.S.
    A portrait of Alzheimer secretases - new features and familiar faces
    Science293, 1449-1454. PubMed  Europe PubMed DOI
  755. [YEAR:30-8-2001]Ghosh,A.K., Bilcer,G., Harwood,C., Kawahama,R., Shin,D., Hussain,K.A., Hong,L., Loy,J.A., Nguyen,C., Koelsch,G., Ermolieff,J. and Tang,J.
    Structure-based design: potent inhibitors of human brain memapsin 2 (beta-secretase)
    J Med Chem44, 2865-2868. PubMed  Europe PubMed DOI  I
  756. Jhee,S., Shiovitz,T., Crawford,A.W. and Cutler,N.R.
    beta-amyloid therapies in Alzheimer's disease
    Expert Opin Investig Drugs10, 593-605. PubMed  Europe PubMed DOI
  757. Kitazume,S., Tachida,Y., Oka,R., Shirotani,K., Saido,T.C. and Hashimoto,Y.
    Alzheimer's beta-secretase, beta-site amyloid precursor protein-cleaving enzyme, is responsible for cleavage secretion of a Golgi-resident sialyltransferase
    Proc Natl Acad Sci U S A98, 13554-13559. PubMed  Europe PubMed DOI
  758. Luo,Y., Bolon,B., Kahn,S., Bennett,B.D., Babu-Khan,S., Denis,P., Fan,W., Kha,H., Zhang,J., Gong,Y., Martin,L., Louis,J.C., Yan,Q., Richards,W.G., Citron,M. and Vassar,R.
    Mice deficient in BACE1, the Alzheimer's beta-secretase, have normal phenotype and abolished beta-amyloid generation
    Nat Neurosci4, 231-232. PubMed  Europe PubMed DOI
  759. Mallender,W.D., Yager,D., Onstead,L., Nichols,M.R., Eckman,C., Sambamurti,K., Kopcho,L.M., Marcinkeviciene,J., Copeland,R.A. and Rosenberry,T.L.
    Characterization of recombinant, soluble beta-secretase from an insect cell expression system
    Mol Pharmacol59, 619-626. PubMed  Europe PubMed  E
  760. [YEAR:29-6-2001]Marcinkeviciene,J., Luo,Y., Graciani,N.R., Combs,A.P. and Copeland,R.A.
    Mechanism of inhibition of beta-site amyloid precursor protein-cleaving enzyme (BACE) by a statine-based peptide
    J Biol Chem276, 23790-23794. PubMed  Europe PubMed DOI
  761. [YEAR:5-3-2001]Murphy,T., Yip,A., Brayne,C., Easton,D., Evans,J.G., Xuereb,J., Cairns,N., Esiri,M.M. and Rubinsztein,D.C.
    The BACE gene: genomic structure and candidate gene study in late-onset Alzheimer's disease
    Neuroreport12, 631-634. PubMed  Europe PubMed  M
  762. [YEAR:3-7-2001]Nowotny,P., Kwon,J.M., Chakraverty,S., Nowotny,V., Morris,J.C. and Goate,A.M.
    Association studies using novel polymorphisms in BACE1 and BACE2
    Neuroreport12, 1799-1802. PubMed  Europe PubMed  M
  763. Pinnix,I., Council,J.E., Roseberry,B., Onstead,L., Mallender,W., Sucic,J. and Sambamurti,K.
    Convertases other than furin cleave beta-secretase to its mature form
    FASEB J15, 1810-1812. PubMed  Europe PubMed  I
  764. [YEAR:1-6-2001]Roberds,S.L., Anderson,J., Basi,G., Bienkowski,M.J., Branstetter,D.G., Chen,K.S., Freedman,S.B., Frigon,N.L., Games,D., Hu,K., Johnson-Wood,K., Kappenman,K.E., Kawabe,T.T., Kola,I., Kuehn,R., Lee,M., Liu,W., Motter,R., Nichols,N.F., Power,M., Robertson,D.W., Schenk,D., Schoor,M., Shopp,G.M., Shuck,M.E., Sinha,S., Svensson,K.A., Tatsuno,G., Tintrup,H., Wijsman,J., Wright,S. and McConlogue,L.
    BACE knockout mice are healthy despite lacking the primary beta-secretase activity in brain: implications for Alzheimer's disease therapeutics
    Hum Mol Genet10, 1317-1324. PubMed  Europe PubMed  K
  765. [YEAR:1-6-2001]Rossner,S., Apelt,J., Schliebs,R., Perez-Polo,J.R. and Bigl,V.
    Neuronal and glial beta-secretase (BACE) protein expression in transgenic Tg2576 mice with amyloid plaque pathology
    J Neurosci Res64, 437-446. PubMed  Europe PubMed DOI
  766. [YEAR:30-3-2001]Shi,X.P., Chen,E., Yin,K.C., Na,S., Garsky,V.M., Lai,M.T., Li,Y.M., Platchek,M., Register,R.B., Sardana,M.K., Tang,M.J., Thiebeau,J., Wood,T., Shafer,J.A. and Gardell,S.J.
    The Pro domain of beta-secretase does not confer strict zymogen-like properties but does assist proper folding of the protease domain
    J Biol Chem276, 10366-10373. PubMed  Europe PubMed
  767. [YEAR:28-8-2001]Turner,R.T., III, Koelsch,G., Hong,L., Castenheira,P., Ghosh,A. and Tang,J.
    Subsite specificity of memapsin 2 (beta-secretase): implications for inhibitor design
    Biochemistry40, 10001-10006. PubMed  Europe PubMed DOI  I
  768. Vassar,R.
    The beta-secretase, BACE: a prime drug target for Alzheimer's disease
    J Mol Neurosci17, 157-170. PubMed  Europe PubMed DOI
  769. Walter,J., Fluhrer,R., Hartung,B., Willem,M., Kaether,C., Capell,A., Lammich,S., Multhaup,G. and Haass,C.
    Phosphorylation regulates intracellular trafficking of beta-secretase
    J Biol Chem276, 14634-14641. PubMed  Europe PubMed DOI
  770. [YEAR:21-6-2001]Wolfe,M.S.
    Secretase targets for Alzheimer's disease: identification and therapeutic potential
    J Med Chem44, 2039-2060. PubMed  Europe PubMed DOI
  771. [YEAR:7-9-2001]Yan,R., Munzner,J.B., Shuck,M.E. and Bienkowski,M.J.
    BACE2 functions as an alternative alpha-secretase in cells
    J Biol Chem276, 34019-34027. PubMed  Europe PubMed DOI
  772. [YEAR:28-9-2001]Yan,R., Han,P., Miao,H., Greengard,P. and Xu,H.
    The transmembrane domain of the Alzheimer's beta-secretase (BACE1) determines its late Golgi localization and access to beta-amyloid precursor protein (APP) substrate
    J Biol Chem276, 36788-36796. PubMed  Europe PubMed DOI
  773. 2000
  774. [YEAR:1-12-2000]Bennett,B.D., Denis,P., Haniu,M., Teplow,D.B., Kahn,S., Louis,J.C., Citron,M. and Vassar,R.
    A furin-like convertase mediates propeptide cleavage of BACE, the Alzheimer's beta-secretase
    J Biol Chem275, 37712-37717. PubMed  Europe PubMed DOI
  775. [YEAR:6-10-2000]Capell,A., Steiner,H., Willem,M., Kaiser,H., Meyer,C., Walter,J., Lammich,S., Multhaup,G. and Haass,C.
    Maturation and pro-peptide cleavage of beta-secretase
    J Biol Chem275, 30849-30854. PubMed  Europe PubMed DOI  I
  776. [YEAR:10-10-2000]Ermolieff,J., Loy,J.A., Koelsch,G. and Tang,J.
    Proteolytic activation of recombinant pro-memapsin 2 (pro-beta-secretase) studied with new fluorogenic substrates
    Biochemistry39, 12450-12456. PubMed  Europe PubMed DOI  A  E
  777. [YEAR:26-12-2000]Ermolieff,J., Loy,J.A., Koelsch,G. and Tang,J.
    Erratum: Proteolytic activation of recombinant pro-memapsin 2 (pro-beta-secretase) studied with new fluorogenic substrates (Biochemistry (October 10, 2000) 39:40 (12450-12456))
    Biochemistry39, 16263-16263. PubMed  Europe PubMed
  778. [YEAR:12-4-2000]Ghosh,A.K., Shin,D.W., Downs,D., Koelsch,G., Lin,X.L., Ermolieff,J. and Tang,J.
    Design of potent inhibitors for human brain memapsin 2 (beta-secretase)
    J Am Chem Soc122, 3522-3523.  I
  779. [YEAR:14-7-2000]Haniu,M., Denis,P., Young,Y., Mendiaz,E.A., Fuller,J., Hui,J.O., Bennett,B.D., Kahn,S., Ross,S., Burgess,T., Katta,V., Rogers,G., Vassar,R. and Citron,M.
    Characterization of Alzheimer's beta-secretase protein BACE. A pepsin family member with unusual properties
    J Biol Chem275, 21099-21106. PubMed  Europe PubMed DOI
  780. [YEAR:6-10-2000]Hong,L., Koelsch,G., Lin,X.L., Wu,S.L., Terzyan,S., Ghosh,A.K., Zhang,X.C. and Tang,J.
    Structure of the protease domain of memapsin 2 (beta-secretase) complexed with inhibitor
    Science290, 150-153. PubMed  Europe PubMed DOI  S  I
  781. [YEAR:27-10-2000]Huse,J.T., Pijak,D.S., Leslie,G.J., Lee,V.M. and Doms,R.W.
    Maturation and endosomal targeting of beta-site amyloid precursor protein-cleaving enzyme. The Alzheimer's disease beta-secretase
    J Biol Chem275, 33729-33737. PubMed  Europe PubMed DOI
  782. [YEAR:15-2-2000]Lin,X., Koelsch,G., Wu,S., Downs,D., Dashti,A. and Tang,J.
    Human aspartic protease memapsin 2 cleaves the beta-secretase site of beta-amyloid precursor protein
    Proc Natl Acad Sci U S A97, 1456-1460. PubMed  Europe PubMed
  783. Potter,H. and Dressler,D.
    The potential of BACE inhibitors for Alzheimer's therapy
    Nat Biotechnol18, 125-126. PubMed  Europe PubMed DOI  I
  784. [YEAR:7-7-2000]Sauder,J.M., Arthur,J.W. and Dunbrack,R.L., Jr.
    Modeling of substrate specificity of the Alzheimer's disease amyloid precursor protein beta-secretase
    J Mol Biol300, 241-248. PubMed  Europe PubMed DOI
  785. [YEAR:28-1-2000]Skovronsky,D.M., Moore,D.B., Milla,M.E., Doms,R.W. and Lee,V.M.
    Protein kinase C-dependent alpha-secretase competes with beta-secretase for cleavage of amyloid-beta precursor protein in the trans-Golgi network
    J Biol Chem275, 2568-2575. PubMed  Europe PubMed DOI
  786. 1999
  787. Hussain,I., Powell,D., Howlett,D.R., Tew,D.G., Meek,T.D., Chapman,C., Gloger,I.S., Murphy,K.E., Southan,C.D., Ryan,D.M., Smith,T.S., Simmons,D.L., Walsh,F.S., Dingwall,C. and Christie,G.
    Identification of a novel aspartic protease (Asp 2) as beta-secretase
    Mol Cell Neurosci14, 419-427. PubMed  Europe PubMed DOI
  788. [YEAR:2-12-1999]Sinha,S., Anderson,J.P., Barbour,R., Basi,G.S., Caccavello,R., Davis,D., Doan,M., Dovey,H.F., Frigon,N., Hong,J., Jacobson-Croak,K., Jewett,N., Keim,P., Knops,J., Lieberburg,I., Power,M., Tan,H., Tatsuno,G., Tung,J., Schenk,D., Seubert,P., Suomensaari,S.M., Wang,S., Walker,D., Zhao,J., McConlogue,L. and John,V.
    Purification and cloning of amyloid precursor protein beta-secretase from human brain
    Nature402, 537-540. PubMed  Europe PubMed DOI
  789. [YEAR:22-10-1999]Vassar,R., Bennett,B.D., Babu-Khan,S., Kahn,S., Mendiaz,E.A., Denis,P., Teplow,D.B., Ross,S., Amarante,P., Loeloff,R., Luo,Y., Fisher,S., Fuller,J., Edenson,S., Lile,J., Jarosinski,M.A., Biere,A.L., Curran,E., Burgess,T., Louis,J.C., Collins,F., Treanor,J., Rogers,G. and Citron,M.
    Beta-secretase cleavage of Alzheimer's amyloid precursor protein by the transmembrane aspartic protease BACE
    Science286, 735-741. PubMed  Europe PubMed DOI
  790. [YEAR:2-12-1999]Yan,R., Bienkowski,M.J., Shuck,M.E., Miao,H., Tory,M.C., Pauley,A.M., Brashier,J.R., Stratman,N.C., Mathews,W.R., Buhl,A.E., Carter,D.B., Tomasselli,A.G., Parodi,L.A., Heinrikson,R.L. and Gurney,M.E.
    Membrane-anchored aspartyl protease with Alzheimer's disease beta-secretase activity
    Nature402, 533-537. PubMed  Europe PubMed DOI
  791. 1996
  792. Citron,M., Diehl,T.S., Gordon,G., Biere,A.L., Seubert,P. and Selkoe,D.J.
    Evidence that the 42- and 40-amino acid forms of amyloid beta protein are generated from the beta-amyloid precursor protein by different protease activities
    Proc Natl Acad Sci U S A93, 13170-13175. PubMed  Europe PubMed DOI