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.)

2026

Keller,M., Gallagher,C., Marengo,L., Bickenbach,K., Schmitt,U., Abukhalaf,M., Tholey,A., Kreiselmaier,S., Becker-Pauly,C., Mittmann,T. and Pietrzik,C.U. Meprin beta elevates hippocampal soluble Abeta in the APP/V717I mouse model Exp Neurol (2026) 397, 115600-115600. PubMed Europe PubMed DOI

2025

Barbosa,D.B., de Oliveira,L.M.G., Mendes,G.O., Costa Junior,D.B., de Oliveira,T.A., da Silva,M.P., Damazio,L.C.M., Maia,E.H.B., Falkoski,D.L., de S Marra, Valle,M.S., da Silva,A.M., Taranto,A.G., da Silva,V.D.A., de Carvalho,P.B. and Leite,F.H.A. Silodosin as a Novel Inhibitor of Acetylcholinesterase, Butyrylcholinesterase, and BETA-Secretase 1: In Vitro and In Silico Studies ACS Omega (2025) 10, 48887-48899. PubMed Europe PubMed DOI PMC EPMC
Bartolic,M. and Bosak,A. BACE1: Biological Functions and Involvement in the Pathophysiology of Alzheimer's Disease and Other Neurological Disorders Biofactors (2025) 51, e70071-e70071. PubMed Europe PubMed DOI
Ella,F.A., Tchamgoue,J., Ambamba,B.D.A., Mountessou,B.Y.G., Essouman,F.M., Essola,N.N., Wilhelm,A., Ngondi,J.L., Njayou,F.N. and Kouam,S.F. Anti-Alzheimer potential of biflavonoids from Allanblackia floribunda: Multi-target inhibition of monoamine oxidase, beta-secretase, and glycogen synthase kinase-3beta Fitoterapia (2025) 188, 106967-106967. PubMed Europe PubMed DOI

2024

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 Chem (2024) 266, 116131-116131. PubMed Europe PubMed DOI I
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 Dis (2024) 101, S53-S78. PubMed Europe PubMed DOI V
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 Neuropathol (2024) 147, 97-97. PubMed Europe PubMed DOI
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 Pharm (2024) 650, 123727-123727. PubMed Europe PubMed DOI
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) (2024) 29, 78-78. PubMed Europe PubMed DOI
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 Biol (2024) 46, 450-460. PubMed Europe PubMed DOI PMC EPMC K
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 Commun (2024) 698, 149538-149538. PubMed Europe PubMed DOI I
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 Invest (2024) 134, e170550-e170550. PubMed Europe PubMed DOI
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 Res (2024) 85, e22214-e22214. PubMed Europe PubMed DOI I
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 Neuropathol (2024) 148, 57-57. PubMed Europe PubMed DOI
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 Res (2024) 463, 114896-114896. PubMed Europe PubMed DOI
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 Talanta (2024) 266, 124904-124904. PubMed Europe PubMed DOI
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 Biol (2024) 31, 265-283. PubMed Europe PubMed DOI

2023

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 J (2023) 122, 3999-4010. PubMed Europe PubMed DOI PMC EPMC
Bao,H. and Shen,Y. Unmasking BACE1 in aging and age-related diseases Trends Mol Med (2023) 29, 99-111. PubMed Europe PubMed DOI V
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 Genet (2023) 32, 1193-1207. PubMed Europe PubMed DOI PMC EPMC
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 Molecules (2023) 28 PubMed Europe PubMed DOI PMC EPMC I
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 Sci (2023) 24 PubMed Europe PubMed DOI PMC EPMC I
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 Res (2023) 20, 131-148. PubMed Europe PubMed DOI V I
Munj,S.M. and Patil,P.B. Drug Discovery to Drug Development of BACE1 Inhibitor as Antialzheimer's: A Review Curr Top Med Chem (2023) 23, 77-97. PubMed Europe PubMed DOI V
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 Macromol (2023) 250, 126224-126224. PubMed Europe PubMed DOI
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 Sci (2023) 24 PubMed Europe PubMed DOI PMC EPMC I
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) (2023) 16 PubMed Europe PubMed DOI PMC EPMC

2022

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 Model (2022) 62, 914-926. PubMed Europe PubMed DOI PMC EPMC
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 Commun (2022) 626, 66-71. PubMed Europe PubMed DOI PMC EPMC
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 Dis (2022) 89, 877-891. PubMed Europe PubMed DOI
Ihara,M. Endothelial BACE1: Bridging the Gap Between Hypertension and Alzheimer's Disease Circ Res (2022) 130, 1342-1344. PubMed Europe PubMed DOI
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 Neurosci (2022) 14, 853180-853180. PubMed Europe PubMed DOI PMC EPMC
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 Adv (2022) 8, eabo1286-eabo1286. PubMed Europe PubMed DOI PMC EPMC
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 Lett (2022) 56, 128463-128463. PubMed Europe PubMed DOI I
Taylor,H.A., Przemylska,L., Clavane,E.M. and Meakin,P.J. BACE1: More than just a beta-secretase Obes Rev (2022) , e13430-e13430. PubMed Europe PubMed DOI V
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 Molecules (2022) 27 PubMed Europe PubMed DOI PMC EPMC
Yeap,Y.J., Kandiah,N., Nizetic,D. and Lim,K.L. BACE2: A Promising Neuroprotective Candidate for Alzheimer's Disease J Alzheimers Dis (2022) PubMed Europe PubMed DOI V

2021

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 Res (2021) , 119164-119164. PubMed Europe PubMed DOI
Bhakat,S. Pepsin-like aspartic proteases (PAPs) as model systems for combining biomolecular simulation with biophysical experiments RSC Adv (2021) 11, 11026-11047. PubMed Europe PubMed DOI PMC EPMC
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 (2021) PubMed Europe PubMed DOI
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 Chem (2021) , 100489-100489. PubMed Europe PubMed DOI V
Fissel,J.A. and Farah,M.H. The influence of BACE1 on macrophage recruitment and activity in the injured peripheral nerve J Neuroinflammation (2021) 18, 71-71. PubMed Europe PubMed DOI PMC EPMC V
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 Chem (2021) 64, 3075-3085. PubMed Europe PubMed DOI I
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 Chem (2021) , 100818-100818. PubMed Europe PubMed DOI
Koriyama,Y., Hori,A., Ito,H., Yonezawa,S., Baba,Y., Tanimoto,N., Ueno,T., Yamamoto,S., Yamamoto,T., Asada,N., Morimoto,K., Einaru,S., Sakai,K., Kanazu,T., Matsuda,A., Yamaguchi,Y., Oguma,T., Timmers,M., Tritsmans,L., Kusakabe,K.I., Kato,A. and Sakaguchi,G. Discovery of Atabecestat (JNJ-54861911): A Thiazine-Based beta-Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor Advanced to the Phase 2b/3 EARLY Clinical Trial J Med Chem (2021) 64, 1873-1888. PubMed Europe PubMed DOI I
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 Chem (2021) 93, 15124-15132. PubMed Europe PubMed DOI
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 Chem (2021) 64, 8076-8100. PubMed Europe PubMed DOI I
Miranda,A., Montiel,E., Ulrich,H. and Paz,C. Selective Secretase Targeting for Alzheimer's Disease Therapy J Alzheimers Dis (2021) PubMed Europe PubMed DOI I
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 Drugs (2021) 19 PubMed Europe PubMed DOI PMC EPMC I
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 Chem (2021) 225, 113779-113779. PubMed Europe PubMed DOI
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 (2021) PubMed Europe PubMed DOI V
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 Pharmaceutics (2021) 13 PubMed Europe PubMed DOI PMC EPMC I
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 Neurobiol (2021) , 102113-102113. PubMed Europe PubMed DOI

2020

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 A (2020) 117, 28528-28530. PubMed Europe PubMed DOI
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 Int (2020) 2020, 8934289-8934289. PubMed Europe PubMed DOI PMC EPMC I
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 Imaging (2020) 47, 2429-2439. PubMed Europe PubMed DOI L
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 Dis (2020) 11, 98-98. PubMed Europe PubMed DOI PMC EPMC I
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 elife (2020) 9 PubMed Europe PubMed DOI PMC EPMC
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 (2020) PubMed Europe PubMed DOI
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 Chem (2020) 95, 103135-103135. PubMed Europe PubMed DOI I
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 (2020) PubMed Europe PubMed DOI I
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 (2020) PubMed Europe PubMed DOI
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 Res (2020) 31, 87-133. PubMed Europe PubMed DOI I
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 (2020) PubMed Europe PubMed DOI
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 Sci (2020) 21 PubMed Europe PubMed DOI I
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 Res (2020) 15, 1546-1553. PubMed Europe PubMed DOI I
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 Neuroscientist (2020) , 1073858420940943-1073858420940943. PubMed Europe PubMed DOI
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 iScience (2020) 23, 101887-101887. PubMed Europe PubMed DOI PMC EPMC
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 Lett (2020) , 126999-126999. PubMed Europe PubMed DOI I
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 Toxicol (2020) 146, 111829-111829. PubMed Europe PubMed DOI I
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 Pharmacol (2020) , 173522-173522. PubMed Europe PubMed DOI I
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 Res (2020) 34, 525-529. PubMed Europe PubMed DOI I
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 J (2020) 34, 2465-2482. PubMed Europe PubMed DOI P
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 Chem (2020) 295, 2175-2183. PubMed Europe PubMed DOI
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 Targets (2020) 19, 184-194. PubMed Europe PubMed DOI
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 Res (2020) 158, 47-55. PubMed Europe PubMed DOI I
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 Molecules (2020) 25 PubMed Europe PubMed DOI L
Wang,B. and Ng,H.L. Deep neural network affinity model for BACE inhibitors in D3R Grand Challenge 4 J Comput Aided Mol Des (2020) 34, 201-217. PubMed Europe PubMed DOI I
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 Cell (2020) , e13194-e13194. PubMed Europe PubMed DOI

2019

Aathi,M. and Piramanayagam,S. From EST to structure models for functional inference of APP, BACE1, PSEN1, PSEN2 genes Bioinformation (2019) 15, 760-771. PubMed Europe PubMed DOI PMC EPMC I
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 ChemMedChem (2019) 14, 1894-1910. PubMed Europe PubMed DOI I
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 Chem (2019) 84, 202-210. PubMed Europe PubMed DOI I
Blass,B.E. Tricyclic inhibitors of beta-secretase and their methods of use for the treatment of Alzheimer's disease ACS Med Chem Lett (2019) 10, 8-9. PubMed Europe PubMed DOI PMC EPMC I
Das,B. and Yan,R. A close look at BACE1 inhibitors for Alzheimer's disease treatment CNS Drugs (2019) 33, 251-263. PubMed Europe PubMed DOI I
Das,S., Chakraborty,S. and Basu,S. Hybrid approach to sieve out natural compounds against dual targets in Alzheimer's disease Sci Rep (2019) 9, 3714-3714. PubMed Europe PubMed DOI PMC EPMC I
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 Neurosci (2019) 39, 9013-9027. PubMed Europe PubMed DOI K I
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 Lett (2019) 29, 126772-126772. PubMed Europe PubMed DOI I
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 Chem (2019) 92, 103253-103253. PubMed Europe PubMed DOI I
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 PeerJ (2019) 7, e8219-e8219. PubMed Europe PubMed DOI PMC EPMC I
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 ChemMedChem (2019) 14, 545-560. PubMed Europe PubMed DOI S I
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 Dyn (2019) 37, 3674-3685. PubMed Europe PubMed DOI I
Islam,M.A. and Pillay,T.S. beta-Secretase inhibitors for Alzheimer's disease: identification using pharmacoinformatics J Biomol Struct Dyn (2019) 37, 503-522. PubMed Europe PubMed DOI I
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) (2019) 69, 451-457. PubMed Europe PubMed DOI I
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 Med (2019) 216, 279-293. PubMed Europe PubMed DOI
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 Polym (2019) 217, 232-239. PubMed Europe PubMed DOI I
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 Biol (2019) 218, 644-663. PubMed Europe PubMed DOI
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 Dement (2019) 15, 1183-1194. PubMed Europe PubMed DOI I
Maia,M.A. and Sousa,E. BACE-1 and gamma-secretase as therapeutic targets for Alzheimer's disease Pharmaceuticals (Basel) (2019) 12 PubMed Europe PubMed DOI I
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 Drugs (2019) 17 PubMed Europe PubMed DOI
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 Acids (2019) 51, 1593-1607. PubMed Europe PubMed DOI I
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 Lett (2019) 10, 1159-1165. PubMed Europe PubMed DOI PMC EPMC I
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 Chem (2019) 84, 4893-4897. PubMed Europe PubMed DOI I
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 Neurother (2019) 19, 599-602. PubMed Europe PubMed DOI I
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 Rep (2019) 9, 9102-9102. PubMed Europe PubMed DOI PMC EPMC I
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 Chem (2019) 87, 474-483. PubMed Europe PubMed DOI I
Selkoe,D. beta-Secretase inhibitors for Alzheimer's disease: heading in the wrong direction? Lancet Neurol (2019) 18, 624-626. PubMed Europe PubMed DOI I
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 Chem (2019) 62, 9331-9337. PubMed Europe PubMed DOI I
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 Med (2019) 60, 992-997. PubMed Europe PubMed DOI L
Yang,E.J., Lee,T. and Song,K.S. beta-Secretase inhibition by C-methylisoflavones from Abronia nana Nat Prod Res (2019) 33, 1705-1712. PubMed Europe PubMed DOI I
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 Brain (2019) 142, 176-192. PubMed Europe PubMed DOI I

2018

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 A (2018) 115, 3954-3959. PubMed Europe PubMed DOI
Bittner,H.J., Guixa-Gonzalez,R. and Hildebrand,P.W. Structural basis for the interaction of the beta-secretase with copper Biochim Biophys Acta (2018) 1860, 1105-1113. PubMed Europe PubMed DOI
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 Biol (2018) 430, 1566-1576. PubMed Europe PubMed DOI I
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 Chem (2018) 61, 5122-5137. PubMed Europe PubMed DOI I
Gabr,M.T. and Abdel-Raziq,M.S. Design and synthesis of donepezil analogues as dual AChE and BACE-1 inhibitors Bioorg Chem (2018) 80, 245-252. PubMed Europe PubMed DOI I
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 Lett (2018) 28, 2910-2913. PubMed Europe PubMed DOI I
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 Chembiochem (2018) 19, 754-763. PubMed Europe PubMed DOI I
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 Lett (2018) 28, 2605-2610. PubMed Europe PubMed DOI S I
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 Chem (2018) 61, 5292-5303. PubMed Europe PubMed DOI I
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 Model (2018) 85, 1-12. PubMed Europe PubMed DOI I
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 Dyn (2018) 36, 3557-3574. PubMed Europe PubMed DOI I
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 Des (2018) 24, 3972-3979. PubMed Europe PubMed DOI I
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 Chem (2018) 61, 3491-3502. PubMed Europe PubMed DOI I
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 Chem (2018) 61, 6121-6139. PubMed Europe PubMed DOI L
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 Acta (2018) 1022, 89-95. PubMed Europe PubMed DOI A
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 Lett (2018) 28, 1111-1115. PubMed Europe PubMed DOI I
Luque Ruiz,I. and Gomez-Nieto,M.A. QSAR classification and regression models for beta-secretase inhibitors using relative distance matrices SAR QSAR Environ Res (2018) 29, 355-383. PubMed Europe PubMed DOI I
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 Chem (2018) 410, 7441-7448. PubMed Europe PubMed DOI A
Mermelstein,D.J., McCammon,J.A. and Walker,R.C. pH-Dependent conformational dynamics of beta-secretase 1: a molecular dynamics study J Mol Recognit (2018) , e2765-e2765. PubMed Europe PubMed DOI
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 Neurosci (2018) 12, 121-121. PubMed Europe PubMed DOI PMC EPMC I
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 Chem (2018) 61, 5525-5546. PubMed Europe PubMed DOI I
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 Med (2018) 10, e9316-e9316. PubMed Europe PubMed DOI I
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 Neurother (2018) 18, 847-857. PubMed Europe PubMed DOI I
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 Chem (2018) 61, 619-637. PubMed Europe PubMed DOI I
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 Chem (2018) 77, 307-317. PubMed Europe PubMed DOI I
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 Neurosci (2018) 9, 1663-1679. PubMed Europe PubMed DOI I
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 Psychiatry (2018) 83, 447-455. PubMed Europe PubMed DOI
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 Lett (2018) 28, 2195-2200. PubMed Europe PubMed DOI I
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) (2018) 6 PubMed Europe PubMed DOI I
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 Chem (2018) 61, 3296-3308. PubMed Europe PubMed DOI L
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 Psychiatry (2018) 26, 586-603. PubMed Europe PubMed DOI
Zhu,K., Peters,F., Filser,S. and Herms,J. Consequences of pharmacological BACE inhibition on synaptic structure and function Biol Psychiatry (2018) 84, 478-487. PubMed Europe PubMed DOI I
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 Analyst (2018) 143, 4585-4591. PubMed Europe PubMed DOI A

2017

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 A (2017) 114, E9665-E9665. PubMed Europe PubMed DOI
Blass,B. C5-C6 Carbocyclic-fused iminothiadiazine dioxides as BACE inhibitors, their compositions, and their use ACS Med Chem Lett (2017) 8, 786-788. PubMed Europe PubMed DOI PMC EPMC I
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 Chem (2017) 60, 9807-9820. PubMed Europe PubMed DOI I
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 Chem (2017) 60, 386-402. PubMed Europe PubMed DOI I
Cheron,N. and Shakhnovich,E.I. Effect of sampling on BACE-1 ligands binding free energy predictions via MM-PBSA calculations J Comput Chem (2017) 38, 1941-1951. PubMed Europe PubMed DOI
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 ONE (2017) 12, e0177683-e0177683. PubMed Europe PubMed DOI I
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 Chem (2017) 38, 1260-1269. PubMed Europe PubMed DOI I
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 Lett (2017) 27, 2432-2438. PubMed Europe PubMed DOI S I
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 Model (2017) 76, 274-288. PubMed Europe PubMed DOI I
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 Lett (2017) , 4832-4837. PubMed Europe PubMed DOI I
Innocenti,R., Lenci,E., Menchi,G., Pupi,A. and Trabocchi,A. Design and synthesis of bicyclic acetals as beta secretase (BACE1) inhibitors Bioorg Med Chem (2017) 25, 5077-5083. PubMed Europe PubMed DOI I
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 Comput (2017) 13, 1439-1453. PubMed Europe PubMed DOI I
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 Model (2017) 23, 239-239. PubMed Europe PubMed DOI I
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 Chem (2017) 71, 1-9. PubMed Europe PubMed DOI I
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 Chem (2017) 292, 13258-13270. PubMed Europe PubMed DOI
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 Chem (2017) 409, 6635-6642. PubMed Europe PubMed DOI A I
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 MedChemComm (2017) 8, 1196-1206. PubMed Europe PubMed DOI PMC EPMC I
Marumoto,S., Okuno,Y. and Miyazawa,M. Inhibition of beta-secretase activity by monoterpenes, sesquiterpenes, and C13 norisoprenoids J Oleo Sci (2017) 66, 851-855. PubMed Europe PubMed DOI I
Palakurti,R. and Vadrevu,R. Pharmacophore based 3D-QSAR modeling, virtual screening and docking for identification of potential inhibitors of beta-secretase Comput Biol Chem (2017) 68, 107-117. PubMed Europe PubMed DOI I
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 PeerJ (2017) 5, e3086-e3086. PubMed Europe PubMed DOI PMC EPMC A L
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 A (2017) 1518, 89-96. PubMed Europe PubMed DOI A I
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 Omega (2017) 2, 685-697. PubMed Europe PubMed DOI PMC EPMC I
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 EBioMedicine (2017) 24, 76-92. PubMed Europe PubMed DOI I
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 Pharmacol (2017) 57, 1460-1471. PubMed Europe PubMed DOI I
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 A (2017) 1487, 235-241. PubMed Europe PubMed DOI A
Yan,R. Physiological functions of the beta-site amyloid precursor protein cleaving enzyme 1 and 2 Front Mol Neurosci (2017) 10, 97-97. PubMed Europe PubMed DOI PMC EPMC
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 Chem (2017) 67, 38-47. PubMed Europe PubMed DOI I

2016

Araki,W. Post-translational regulation of the beta-secretase BACE1 Brain Res Bull (2016) 126, 170-177. PubMed Europe PubMed DOI V
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 Neurosci (2016) 39, 158-169. PubMed Europe PubMed DOI V
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 Rep (2016) 14, 2127-2141. PubMed Europe PubMed DOI P I
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 Funct (2016) 7, 3834-3842. PubMed Europe PubMed DOI I
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 Chem (2016) 291, 318-333. PubMed Europe PubMed DOI P
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 Model (2016) 66, 155-167. PubMed Europe PubMed DOI I
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 Model (2016) 70, 181-195. PubMed Europe PubMed DOI
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 Model (2016) 22, 58-58. PubMed Europe PubMed DOI
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 Lett (2016) 26, 33-37. PubMed Europe PubMed DOI I
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 Chem (2016) 24, 2567-2575. PubMed Europe PubMed DOI I
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 Chem (2016) 59, 3732-3749. PubMed Europe PubMed DOI I
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 Des (2016) 12, 73-82. PubMed Europe PubMed I
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 Med (2016) 8, 363ra150-363ra. PubMed Europe PubMed DOI I
Kumalo,H.M., Bhakat,S. and Soliman,M.E. Investigation of flap flexibility of beta-secretase using molecular dynamic simulations J Biomol Struct Dyn (2016) 34, 1008-1019. PubMed Europe PubMed DOI
Kumalo,H.M. and Soliman,M.E. A comparative molecular dynamics study on BACE1 and BACE2 flap flexibility J Recept Signal Transduct Res (2016) 36, 505-514. PubMed Europe PubMed DOI
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) (2016) 10, 365-378. PubMed Europe PubMed DOI V
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 Screen (2016) 19, 470-480. PubMed Europe PubMed I
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 Chem (2016) 59, 3231-3248. PubMed Europe PubMed DOI I
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 Neurosci (2016) 60, 305-315. PubMed Europe PubMed DOI I
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 Bioinformatics (2016) 2016, 9258578-9258578. PubMed Europe PubMed DOI PMC EPMC I
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 Phys (2016) 18, 24790-24801. PubMed Europe PubMed DOI
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 Neurodegener (2016) 11, 67-67. PubMed Europe PubMed DOI
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 Chem (2016) 88, 10559-10565. PubMed Europe PubMed DOI A
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 Model (2016) 68, 206-215. PubMed Europe PubMed DOI
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 Chem (2016) 59, 10435-10450. PubMed Europe PubMed DOI I
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 Rep (2016) 6, 21917-21917. PubMed Europe PubMed DOI PMC EPMC I
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 Targets (2016) 15, 935-944. PubMed Europe PubMed DOI I
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 Lett (2016) 7, 271-276. PubMed Europe PubMed DOI PMC EPMC I
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 Chem (2016) 59, 8593-8600. PubMed Europe PubMed DOI I
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 Lett (2016) 26, 5729-5731. PubMed Europe PubMed DOI I
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 Commun (2016) 7, 13042-13042. PubMed Europe PubMed DOI I

2015

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 Sci (2015) 28, 139-146. PubMed Europe PubMed I
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 Rep (2015) 12, 1367-1376. PubMed Europe PubMed DOI
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 Lett (2015) 25, 5040-5047. PubMed Europe PubMed DOI I
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 Chem (2015) 58, 2678-2702. PubMed Europe PubMed DOI I
Chakraborty,S. and Basu,S. Structural insight into the mechanism of amyloid precursor protein recognition by beta-secretase 1: A molecular dynamics study Biophys Chem (2015) 202, 1-12. PubMed Europe PubMed DOI
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 Lett (2015) 25, 767-774. PubMed Europe PubMed DOI I
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 Lett (2015) 6, 210-215. PubMed Europe PubMed DOI PMC EPMC I
Das,S., Chakraborty,S. and Basu,S. Fragment-based designing for the generation of novel leads against BACE1 Cent Nerv Syst Agents Med Chem (2015) 15, 52-64. PubMed Europe PubMed I
Devi,L. and Ohno,M. A combination Alzheimer's therapy targeting BACE1 and neprilysin in 5XFAD transgenic mice Mol Brain (2015) 8, 19- PubMed Europe PubMed DOI PMC EPMC
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 Proteomics (2015) 14, 2550-2563. PubMed Europe PubMed DOI
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 J (2015) 282, 3618-3631. PubMed Europe PubMed DOI
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) (2015) 348, 330-337. PubMed Europe PubMed DOI I
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 Lett (2015) 25, 4812-4819. PubMed Europe PubMed DOI I
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 Psychiatry (2015) 77, 729-739. PubMed Europe PubMed DOI I
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 Lett (2015) 25, 668-672. PubMed Europe PubMed DOI S I
Ghosh,A.K. and Tang,J. Prospects of beta-secretase inhibitors for the treatment of Alzheimer's disease ChemMedChem (2015) 10, 1463-1466. PubMed Europe PubMed DOI I
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 Chem (2015) 87, 4100-4103. PubMed Europe PubMed DOI
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 Chem (2015) 23, 5626-5640. PubMed Europe PubMed DOI I
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 ONE (2015) 10, e0115973-e0115973. PubMed Europe PubMed DOI I
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 Biol (2015) 11, e1004341-e1004341. PubMed Europe PubMed DOI I
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 Med (2015) 7, 175-189. PubMed Europe PubMed DOI
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 OA (2015) 1, FSO11-FSO11. PubMed Europe PubMed DOI PMC EPMC
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 Neurosci (2015) 35, 1199-1210. PubMed Europe PubMed DOI I
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 Res (2015) 38, 456-469. PubMed Europe PubMed DOI I
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 Neurodegener (2015) 10, 44-44. PubMed Europe PubMed DOI PMC EPMC I
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 Neurosci (2015) 6, 1665-1682. PubMed Europe PubMed DOI I
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 Engl (2015) 54, 1578-1582. PubMed Europe PubMed DOI I
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 Biol (2015) 9, 67-72. PubMed Europe PubMed DOI PMC EPMC I
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 Res (2015) 29, 1735-1738. PubMed Europe PubMed DOI I
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 Chem (2015) 58, 8216-8235. PubMed Europe PubMed DOI I
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 J (2015) 9, 13-26. PubMed Europe PubMed DOI PMC EPMC I
Semighini,E.P. In silico design of beta-secretase inhibitors in Alzheimer's disease Chem Biol Drug Des (2015) 86, 284-290. PubMed Europe PubMed DOI I
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 ONE (2015) 10, e0136950-e0136950. PubMed Europe PubMed DOI PMC EPMC
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 Pharmacokinet (2015) 40, 171-185. PubMed Europe PubMed DOI I
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 Sci (2015) 76, 138-148. PubMed Europe PubMed DOI I
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 Chem (2015) 155, 389-397. DOI I
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 Chem (2015) 58, 5408-5418. PubMed Europe PubMed DOI I
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 Chem (2015) 23, 3260-3268. PubMed Europe PubMed DOI I
Wolfe,M.S. Cutting in on a secretase pas de deux Cell Res (2015) 25, 1091-1092. PubMed Europe PubMed DOI
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 Biochem (2015) 408, 37-46. PubMed Europe PubMed DOI I

2014

The BACE race is on Nat Rev Drug Discov (2014) 13, 165-165. DOI I
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 Sci (2014) 15, 5128-5139. PubMed Europe PubMed DOI I
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) 2014, 598728-598728. PubMed Europe PubMed DOI PMC EPMC
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 Lett (2014) 24, 5455-5459. PubMed Europe PubMed DOI I
Cruz,D.S. and Castilho,M.S. 2D QSAR studies on series of human beta-secretase (BACE-1) inhibitors Med Chem (2014) 10, 162-173. PubMed Europe PubMed DOI I
Cully,M. Deal watch: Lilly buys back into the BACE race for Alzheimer's disease Nat Rev Drug Discov (2014) 13, 804-804. PubMed Europe PubMed DOI I
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 Sci (2014) 953-954, 108-114. PubMed Europe PubMed DOI A
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 Commun (2014) 443, 1054-1059. PubMed Europe PubMed DOI I
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 Chem (2014) 57, 9811-9831. PubMed Europe PubMed DOI I
Ghosh,A.K. and Osswald,H.L. BACE1 (beta-secretase) inhibitors for the treatment of Alzheimer's disease Chem Soc Rev (2014) 43, 6765-6813. PubMed Europe PubMed DOI I
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 Chem (2014) 57, 90-98. PubMed Europe PubMed DOI I
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 Chem (2014) 289, 20630-20637. PubMed Europe PubMed DOI
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 J (2014) 281, 2074-2087. PubMed Europe PubMed DOI
Kandalepas,P.C. and Vassar,R. The normal and pathologic roles of the Alzheimer's beta-secretase, BACE1 Curr Alzheimer Res (2014) 11, 441-449. PubMed Europe PubMed DOI
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 Soc (2014) 58, 553-559. DOI E
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 Chem (2014) 79, 413-421. PubMed Europe PubMed DOI I
Menting,K.W. and Claassen,J.A. beta-secretase inhibitor; a promising novel therapeutic drug in Alzheimer's disease Front Aging Neurosci (2014) 6, 165-165. PubMed Europe PubMed DOI PMC EPMC I
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 ScientificWorldJournal (2014) 2014, 482463-482463. PubMed Europe PubMed DOI PMC EPMC
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 Biol (2014) 41, 536-543. PubMed Europe PubMed DOI I
Polgar,T. and Keseru,G.M. Structure-based beta-secretase (BACE1) inhibitors Curr Pharm Des (2014) 20, 3373-3379. PubMed Europe PubMed DOI I
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 Model (2014) 54, 818-825. PubMed Europe PubMed DOI I
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 Chem (2014) 57, 878-902. PubMed Europe PubMed DOI I
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 Chem (2014) 57, 10112-10129. PubMed Europe PubMed DOI I
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 Neurochem (2014) 130, 4-28. PubMed Europe PubMed DOI K
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 Prod (2014) 77, 1275-1279. PubMed Europe PubMed DOI I
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 Lett (2014) 5, 440-445. PubMed Europe PubMed DOI I
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 Lett (2014) 24, 2477-2480. PubMed Europe PubMed DOI I
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 Chem (2014) 84, 1615-1621. DOI I
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 Med (2014) 14, 88-88. PubMed Europe PubMed DOI PMC EPMC I
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 Rep (2014) 2, 167-171. PubMed Europe PubMed DOI PMC EPMC V
Yan,R. and Vassar,R. Targeting the beta secretase BACE1 for Alzheimer's disease therapy Lancet Neurol (2014) 13, 319-329. PubMed Europe PubMed DOI I

2013

Abdel-Magid,A.F. beta-Secretase inhibitors for the treatment of Alzheimer's disease and Down's Syndrome ACS Med Chem Lett (2013) 4, 578-579. PubMed Europe PubMed DOI PMC EPMC I
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 Chem (2013) 28, 153-162. PubMed Europe PubMed DOI I
Barman,A. and Prabhakar,R. Elucidating the catalytic mechanism of beta-secretase (BACE1): A quantum mechanics/molecular mechanics (QM/MM) approach J Mol Graph Model (2013) 40, 1-9. PubMed Europe PubMed DOI
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 Lett (2013) 23, 2181-2186. PubMed Europe PubMed DOI I
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 Lett (2013) 23, 85-89. PubMed Europe PubMed DOI I
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 Chem (2013) 13, 1787-1807. PubMed Europe PubMed I
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 Dis (2013) 37, 823-834. PubMed Europe PubMed DOI I
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 J (2013) 32, 2015-2028. PubMed Europe PubMed DOI
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 Anal (2013) 73, 131-134. PubMed Europe PubMed DOI I
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 Chem (2013) 405, 827-835. PubMed Europe PubMed DOI I
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 Neurosci (2013) 37, 1962-1969. PubMed Europe PubMed DOI P
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 Dis (2013) 37, 343-355. PubMed Europe PubMed DOI I
Devi,L. and Ohno,M. Mechanisms that lessen benefits of beta-secretase reduction in a mouse model of Alzheimer's disease Transl Psychiatry (2013) 3, e284-e284. PubMed Europe PubMed DOI
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 Des (2013) 27, 403-417. PubMed Europe PubMed DOI I
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 Chem (2013) 21, 2396-2412. PubMed Europe PubMed DOI I
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 Neurosci (2013) 33, 10075-10084. PubMed Europe PubMed DOI I
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) ChemMedChem (2013) 8, 1041-1056. PubMed Europe PubMed DOI A I
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 Model (2013) 19, 2971-2979. PubMed Europe PubMed DOI I
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 Chem (2013) 56, 4181-4205. PubMed Europe PubMed DOI I
Hamada,Y. [Significance of quantum chemical interactions for medicinal science and design of beta-secretase inhibitors] Yakugaku Zasshi (2013) 133, 1113-1120. PubMed Europe PubMed DOI I
Hamada,Y. and Kiso,Y. Advances in the identification of beta-secretase inhibitors Expert Opin Drug Discov (2013) 8, 709-731. PubMed Europe PubMed DOI I
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 Chem (2013) 56, 3980-3995. PubMed Europe PubMed DOI I
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 Proteomics (2013) 13, 1519-1527. PubMed Europe PubMed DOI K P
Holsinger,R.M., Goense,N., Bohorquez,J. and Strappe,P. Splice variants of the Alzheimer's disease beta-secretase, BACE1 Neurogenetics (2013) 14, 1-9. PubMed Europe PubMed DOI M
Hu,X., Schlanger,R., He,W., Macklin,W.B. and Yan,R. Reversing hypomyelination in BACE1-null mice with Akt-DD overexpression FASEB J (2013) 27, 1868-1873. PubMed Europe PubMed DOI K
Hu,X., He,W., Luo,X., Tsubota,K.E. and Yan,R. BACE1 regulates hippocampal astrogenesis via the Jagged1-Notch pathway Cell Rep (2013) 4, 40-49. PubMed Europe PubMed DOI
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 Model (2013) 45, 65-83. PubMed Europe PubMed DOI I
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 Chem (2013) 56, 3379-3403. PubMed Europe PubMed DOI
Kashima,Y. and Miyazawa,M. Structure-activity relationships for bergenin analogues as beta-secretase (BACE1) inhibitors J Oleo Sci (2013) 62, 391-401. PubMed Europe PubMed DOI I
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 Chem (2013) 78, 2661-2669. PubMed Europe PubMed DOI I
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) (2013) 45, 613-621. PubMed Europe PubMed DOI P
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 Dispos (2013) 41, 1134-1147. PubMed Europe PubMed DOI I
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 Res (2013) 8, 3095-3106. PubMed Europe PubMed DOI K
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 Commun (2013) 441, 291-296. PubMed Europe PubMed DOI I
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 ONE (2013) 8, e55774-e55774. PubMed Europe PubMed DOI PMC EPMC
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 Soc (2013) 135, 19354-19361. PubMed Europe PubMed DOI
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 Sci (2013) 5, 119-126. PubMed Europe PubMed DOI I
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 Lett (2013) 23, 4674-4679. PubMed Europe PubMed DOI I
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 Inform (2013) 32, 385-398. PubMed Europe PubMed DOI I
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 Discov (2013) 10, 253-265. I
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 Lett (2013) 23, 4459-4464. PubMed Europe PubMed DOI I
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 Res (2013) 12, 423-436. PubMed Europe PubMed PMC EPMC I
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 Chem (2013) 21, 6893-6909. PubMed Europe PubMed DOI I
Rosse,G. Dihydrooxazines as inhibitors of BACE-1 or BACE-2 ACS Med Chem Lett (2013) 4, 433-434. PubMed Europe PubMed DOI PMC EPMC I
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 Lett (2013) 23, 5300-5306. PubMed Europe PubMed DOI I
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 J (2013) 27, 2458-2467. PubMed Europe PubMed DOI
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 Pharm (2013) 7, 558-566. I
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 J (2013) 7, 1-15. PubMed Europe PubMed DOI PMC EPMC I
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 Screen (2013) 18, 277-285. PubMed Europe PubMed DOI A
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 Molecules (2013) 18, 3577-3594. PubMed Europe PubMed DOI I
Southan,C. and Hancock,J.M. A tale of two drug targets: the evolutionary history of BACE1 and BACE2 Front Genet (2013) 4, 293-293. PubMed Europe PubMed DOI PMC EPMC
Stamford,A. and Strickland,C. Inhibitors of BACE for treating Alzheimer's disease: a fragment-based drug discovery story Curr Opin Chem Biol (2013) 17, 320-328. PubMed Europe PubMed DOI I
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 Chem (2013) 288, 10536-10547. PubMed Europe PubMed DOI P
Wang,H., Li,R. and Shen,Y. beta-Secretase: its biology as a therapeutic target in diseases Trends Pharmacol Sci (2013) 34, 215-225. PubMed Europe PubMed DOI V T
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 Lett (2013) 23, 4239-4243. PubMed Europe PubMed DOI I
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 Lett (2013) 23, 3075-3080. PubMed Europe PubMed DOI I
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 Chem (2013) 21, 6506-6522. PubMed Europe PubMed DOI I
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 Molecules (2013) 18, 5706-5722. PubMed Europe PubMed DOI I

2012

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 Model (2012) 52, 1275-1287. PubMed Europe PubMed DOI I
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 Chem (2012) 55, 9224-9239. PubMed Europe PubMed DOI I
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 Med (2012) 4, 980-991. PubMed Europe PubMed DOI K I
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 Rep (2012) 2, 231-231. PubMed Europe PubMed DOI PMC EPMC
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 Lett (2012) 22, 1408-1414. PubMed Europe PubMed DOI
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 Chem (2012) 48, 206-213. PubMed Europe PubMed DOI I
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 Lett (2012) 22, 2444-2449. PubMed Europe PubMed DOI I
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 Dis (2012) 45, 417-424. PubMed Europe PubMed DOI
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 Chem (2012) 55, 9025-9044. PubMed Europe PubMed DOI I
Dislich,B. and Lichtenthaler,S.F. The membrane-bound aspartyl protease BACE1: molecular and functional properties in Alzheimer's disease and beyond Front Physiol (2012) 3, 8-8. PubMed Europe PubMed DOI PMC EPMC V
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 Chem (2012) 55, 9069-9088. PubMed Europe PubMed DOI I
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 Chem (2012) 393, 473-484. PubMed Europe PubMed DOI
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 Neurochem (2012) 121, 763-773. PubMed Europe PubMed DOI R
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 Engl (2012) 51, 10795-10799. PubMed Europe PubMed DOI L
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 Chem (2012) 55, 9208-9223. PubMed Europe PubMed DOI S I
Ghosh,A.K., Brindisi,M. and Tang,J. Developing beta-secretase inhibitors for treatment of Alzheimer's disease J Neurochem (2012) 120 Suppl 1, 71-83. PubMed Europe PubMed DOI V I
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 Lett (2012) 22, 5460-5465. PubMed Europe PubMed DOI I
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 Chem (2012) 55, 9195-9207. PubMed Europe PubMed DOI S I
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 Chem (2012) 55, 9297-9311. PubMed Europe PubMed DOI I
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 Chem (2012) 287, 38408-38425. PubMed Europe PubMed DOI K
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 Chem (2012) 55, 9156-9169. PubMed Europe PubMed DOI I
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 Chem (2012) 287, 41245-41257. PubMed Europe PubMed DOI PMC EPMC I
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 Model (2012) 52, 1079-1085. PubMed Europe PubMed DOI I
Kacker,P., Bottegoni,G. and Cavalli,A. Computational methods in the discovery and design of BACE-1 inhibitors Curr Med Chem (2012) 19, 6095-6111. PubMed Europe PubMed I
Kandalepas,P.C. and Vassar,R. Identification and biology of beta-secretase J Neurochem (2012) 120 Suppl 1, 55-61. PubMed Europe PubMed DOI V
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 Molecules (2012) 18, 140-153. PubMed Europe PubMed DOI I
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 Purif (2012) 82, 125-131. PubMed Europe PubMed DOI E
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 Lett (2012) 22, 4740-4744. PubMed Europe PubMed DOI I
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 Chem (2012) 55, 10749-10765. PubMed Europe PubMed DOI I
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 Sin (2012) 33, 1459-1468. PubMed Europe PubMed DOI I
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 Chem (2012) 55, 9331-9345. PubMed Europe PubMed DOI I
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 Lett (2012) 22, 3607-3611. PubMed Europe PubMed DOI I
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 Des (2012) 79, 972-980. PubMed Europe PubMed DOI I
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 Model (2012) 18, 4567-4576. PubMed Europe PubMed DOI I
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 Chem (2012) 55, 3364-3386. PubMed Europe PubMed DOI I
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 Chem (2012) 20, 4377-4389. PubMed Europe PubMed DOI I
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 Heterocycles (2012) 85, 2749-2756. DOI I
Sathya,M., Premkumar,P., Karthick,C., Moorthi,P., Jayachandran,K.S. and Anusuyadevi,M. BACE1 in Alzheimer's disease Clin Chim Acta (2012) 414, 171-178. PubMed Europe PubMed DOI V
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 J (2012) 279, 1291-1305. PubMed Europe PubMed DOI
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 Lett (2012) 3, 897-902. PubMed Europe PubMed DOI PMC EPMC I
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 Lett (2012) 22, 6721-6727. PubMed Europe PubMed DOI I
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 Lett (2012) 22, 1854-1859. PubMed Europe PubMed DOI S I
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 Chem (2012) 55, 9346-9361. PubMed Europe PubMed DOI I
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 Neurodegener (2012) 7 Suppl 1, L9-L9. PMC EPMC
Tang,J. and Koelsch,G. Memapsin 2 [ISSN:978-0-12-407744-7] (2012) 3, 87-93. DOI
Vassar,R. BACE1, the Alzheimer's beta-secretase enzyme, in health and disease Mol Neurodegener (2012) 7 Suppl 1, L3-L3. DOI PMC EPMC V
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 Glia (2012) 60, 203-217. PubMed Europe PubMed DOI
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 Chem (2012) 55, 9009-9024. PubMed Europe PubMed DOI I
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 Chem (2012) 317, 83-114. PubMed Europe PubMed DOI I
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 Crystallogr (2012) 68, 13-25. PubMed Europe PubMed DOI
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 Chem (2012) 55, 8838-8858. PubMed Europe PubMed DOI I
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 Chem (2012) 287, 25927-25940. PubMed Europe PubMed DOI
Zhu,Z. Iminoheterocycle as a druggable motif: BACE1 inhibitors and beyond Trends Pharmacol Sci (2012) 33, 233-240. PubMed Europe PubMed DOI I

2011

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 Chem (2011) 54, 8373-8385. PubMed Europe PubMed DOI I
Barman,A., Schurer,S. and Prabhakar,R. Computational modeling of substrate specificity and catalysis of the beta-secretase (BACE1) enzyme Biochemistry (2011) 50, 4337-4349. PubMed Europe PubMed DOI
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 Lett (2011) 21, 6916-6924. PubMed Europe PubMed DOI I
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 Int (2011) 58, 914-923. PubMed Europe PubMed DOI S I
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 J (2011) 25, 775-784. PubMed Europe PubMed DOI I
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 Chem (2011) 54, 5836-5857. PubMed Europe PubMed DOI I
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 Discov (2011) 6, 91-106. PubMed Europe PubMed DOI V I
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 Neurosci (2011) 31, 5744-5754. PubMed Europe PubMed DOI K
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 Des (2011) 25, 583-597. PubMed Europe PubMed DOI I
Halima,S.B. and Rajendran,L. Membrane anchored and lipid raft targeted beta-secretase inhibitors for Alzheimer's disease therapy J Alzheimers Dis (2011) 24 Suppl 2, 143-152. PubMed Europe PubMed DOI I
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 ONE (2011) 6, e21337-e21337. PubMed Europe PubMed DOI PMC EPMC P
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 Bioinformatics (2011) 12 Suppl 1, S28-S28. PubMed Europe PubMed DOI PMC EPMC I
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 Aging (2011) 32, 541-543. PubMed Europe PubMed DOI M
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 Chem (2011) 26, 643-648. PubMed Europe PubMed DOI I
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 Lett (2011) 21, 5164-5170. PubMed Europe PubMed DOI I
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 Chem (2011) 400, 1979-1996. PubMed Europe PubMed DOI I
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 Lett (2011) 21, 537-541. PubMed Europe PubMed DOI I
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 Neurosci (2011) 31, 16507-16516. PubMed Europe PubMed DOI I
Mishra,S. and Caflisch,A. Dynamics in the active site of beta-secretase: a network analysis of atomistic simulations Biochemistry (2011) 50, 9328-9339. PubMed Europe PubMed DOI
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 Des (2011) 7, 263-275. PubMed Europe PubMed V I
Prado-Prado,F., Escobar-Cubiella,M. and Garcia-Mera,X. Review of bioinformatics and QSAR studies of beta-secretase inhibitors Curr Bioinform (2011) 6, 3-15. V I
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 Neurodegener (2011) 6, 88-88. PubMed Europe PubMed DOI K
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 Lett (2011) 21, 1942-1947. PubMed Europe PubMed DOI I
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 Chem (2011) 392, 555-569. PubMed Europe PubMed DOI
Sorribas,A., Jimenez,J.I., Yoshida,W.Y. and Williams,P.G. Daedalols A-C, fungal-derived BACE1 inhibitors Bioorg Med Chem (2011) 19, 6581-6586. PubMed Europe PubMed DOI I
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 Chem (2011) 54, 3081-3085. PubMed Europe PubMed DOI I
Takahashi,T. and Miyazawa,M. Serotonin derivatives as inhibitors of beta-secretase (BACE 1) Pharmazie (2011) 66, 301-305. PubMed Europe PubMed DOI I
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 Lett (2011) 21, 6909-6915. PubMed Europe PubMed DOI I
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 Lett (2011) 21, 7255-7260. PubMed Europe PubMed DOI I
Vassar,R. and Kandalepas,P.C. The beta-secretase enzyme BACE1 as a therapeutic target for Alzheimer's disease Alzheimers Res Ther (2011) 3, 20-20. PubMed Europe PubMed DOI V T
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 Bao (2011) 27, 1655-1666. PubMed Europe PubMed E
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 Chem (2011) 19, 145-155. PubMed Europe PubMed DOI I
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 Res (2011) 36, 2083-2090. PubMed Europe PubMed DOI
Zhi,P., Chia,C. and Gleeson,P.A. Intracellular trafficking of the beta-secretase and processing of amyloid precursor protein IUBMB Life (2011) 63, 721-729. PubMed Europe PubMed DOI
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 Chem (2011) 286, 8677-8687. PubMed Europe PubMed DOI

2010

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 Chem (2010) 18, 3088-3115. PubMed Europe PubMed DOI I
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 Discov (2010) 7, 507-515. DOI I
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 Chem (2010) 18, 1711-1723. PubMed Europe PubMed DOI I
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 Chem (2010) 53, 1458-1464. PubMed Europe PubMed DOI I
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 Chem (2010) 45, 2578-2590. PubMed Europe PubMed DOI I
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 Lett (2010) 20, 4639-4644. PubMed Europe PubMed DOI I
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 Lett (2010) 20, 2837-2842. PubMed Europe PubMed DOI S I
De Strooper,B., Vassar,R. and Golde,T. The secretases: enzymes with therapeutic potential in Alzheimer disease Nat Rev Neurol (2010) 6, 99-107. PubMed Europe PubMed DOI I
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 Biochemistry (2010) 49, 7255-7263. PubMed Europe PubMed DOI I
Evin,G., Barakat,A. and Masters,C.L. BACE: therapeutic target and potential biomarker for Alzheimer's disease Int J Biochem Cell Biol (2010) 42, 1923-1926. PubMed Europe PubMed DOI K V T
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 Neurosci (2010) 30, 11157-11166. PubMed Europe PubMed DOI I
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 Lett (2010) 20, 1924-1927. PubMed Europe PubMed DOI S I
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 Chem (2010) 18, 5610-5615. PubMed Europe PubMed DOI I
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 Lett (2010) 20, 3158-3160. PubMed Europe PubMed DOI I
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 A (2010) 107, 1630-1635. PubMed Europe PubMed DOI
Jiaranaikulwanitch,J., Boonyarat,C., Fokin,V.V. and Vajragupta,O. Triazolyl tryptoline derivatives as beta-secretase inhibitors Bioorg Med Chem Lett (2010) 20, 6572-6576. PubMed Europe PubMed DOI I
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 Commun (2010) 393, 21-27. PubMed Europe PubMed DOI
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 Commun (2010) 393, 728-733. PubMed Europe PubMed DOI P
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 Neurochem (2010) 112, 1552-1561. PubMed Europe PubMed DOI
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 Chem (2010) 391, 849-859. PubMed Europe PubMed DOI I
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 Lett (2010) 20, 603-607. PubMed Europe PubMed DOI I
Li,X., Bo,H., Zhang,X.C., Hartsuck,J.A. and Tang,J. Predicting memapsin 2 (beta-secretase) hydrolytic activity Protein Sci (2010) 19, 2175-2185. PubMed Europe PubMed DOI P
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 Res (2010) 5, 572-578. DOI
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 Lett (2010) 20, 6533-6537. PubMed Europe PubMed DOI S I
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 Lett (2010) 20, 5329-5333. PubMed Europe PubMed DOI I
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 Chem (2010) 18, 630-639. PubMed Europe PubMed DOI I
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 Chem (2010) 53, 1146-1158. PubMed Europe PubMed DOI I
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 Lett (2010) 20, 2068-2073. PubMed Europe PubMed DOI I
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 Lett (2010) 20, 6597-6605. PubMed Europe PubMed DOI I
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 Chem (2010) 45, 542-554. PubMed Europe PubMed DOI I
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 Chem (2010) 45, 2089-2094. PubMed Europe PubMed DOI I
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 Lett (2010) 20, 632-635. PubMed Europe PubMed DOI I
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 Divers (2010) 14, 39-49. PubMed Europe PubMed DOI I
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 Lett (2010) 20, 6034-6039. PubMed Europe PubMed DOI I
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 J (2010) 277, 1503-1518. PubMed Europe PubMed DOI
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 Des (2010) 24, 803-817. PubMed Europe PubMed DOI I
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 Lett (2010) 20, 4558-4560. PubMed Europe PubMed DOI I
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 Chemistry (2010) 16, 14412-14423. PubMed Europe PubMed DOI I
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 Res (2010) 20, 138-153. PubMed Europe PubMed DOI
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 Lett (2010) 20, 4789-4794. PubMed Europe PubMed DOI I
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 Lett (2010) 20, 6231-6236. PubMed Europe PubMed DOI I
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 Chem (2010) 53, 942-950. PubMed Europe PubMed DOI I
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 Chem (2010) 45, 870-882. PubMed Europe PubMed DOI I
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 Lett (2010) 20, 5763-5766. PubMed Europe PubMed DOI I
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 Lett (2010) 20, 6203-6207. PubMed Europe PubMed DOI I
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 Chem (2010) 285, 1634-1642. PubMed Europe PubMed DOI I
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 Lett (2010) 20, 2326-2329. PubMed Europe PubMed DOI I
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 Lett (2010) 20, 1779-1782. PubMed Europe PubMed DOI I
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 Chem (2010) 53, 951-965. PubMed Europe PubMed DOI S I

2009

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 Chem (2009) 52, 6484-6488. PubMed Europe PubMed DOI I
Albert,J.S. Progress in the development of beta-secretase inhibitors for Alzheimer's disease Prog Med Chem (2009) 48, 133-161. PubMed Europe PubMed DOI I
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 Commun (2009) 388, 434-438. PubMed Europe PubMed DOI R
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 Lett (2009) 583, 3221-3224. PubMed Europe PubMed DOI PMC EPMC
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 Lett (2009) 19, 3674-3678. PubMed Europe PubMed DOI I
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 Lett (2009) 19, 3664-3668. PubMed Europe PubMed DOI I
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 Lett (2009) 19, 3669-3673. PubMed Europe PubMed DOI I
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 Med (2009) 75, 537-540. PubMed Europe PubMed DOI I
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 Biochemistry (2009) 48, 10743-10751. PubMed Europe PubMed DOI I
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 Acta (2009) 1788, 1933-1938. PubMed Europe PubMed DOI
Hemming,M.L., Elias,J.E., Gygi,S.P. and Selkoe,D.J. Identification of beta-secretase (BACE1) substrates using quantitative proteomics PLoS ONE (2009) 4, e8477-e8477. PubMed Europe PubMed DOI PMC EPMC P
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 Lett (2009) 19, 4993-4995. PubMed Europe PubMed DOI I
Holloway,M.K., Hunt,P. and McGaughey,G.B. Structure and modeling in the design of beta- and gamma-secretase inhibitors Drug Dev Res (2009) 70, 70-93. DOI I
Huang,W.H., Sheng,R. and Hu,Y.Z. Progress in the development of nonpeptidomimetic BACE 1 inhibitors for Alzheimer's disease Curr Med Chem (2009) 16, 1806-1820. PubMed Europe PubMed DOI I
Hunt,C.E. and Turner,A.J. Cell biology, regulation and inhibition of beta-secretase (BACE-1) FEBS J (2009) 276, 1845-1859. PubMed Europe PubMed DOI V I
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 Res (2009) 87, 2963-2972. PubMed Europe PubMed DOI
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 Chem (2009) 24, 181-187. PubMed Europe PubMed DOI I
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 Cells (2009) 27, 651-656. PubMed Europe PubMed DOI
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 Lett (2009) 19, 1361-1365. PubMed Europe PubMed DOI S I
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 Lett (2009) 19, 1366-1370. PubMed Europe PubMed DOI I
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 Chem (2009) 52, 6314-6323. PubMed Europe PubMed DOI I
Mowrer,K.R. and Wolfe,M.S. Identification of a cis-acting element involved in the regulation of BACE1 mRNA alternative splicing J Neurochem (2009) 109, 1008-1016. PubMed Europe PubMed DOI R
Regina,G.L., Piscitelli,F. and Silvestri,R. Synthetic strategies of nonpeptidic beta-secretase (BACE1) inhibitors J Heterocycl Chem (2009) 46, 10-17. DOI I
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 Lett (2009) 16, 86-90. PubMed Europe PubMed DOI I
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 Lett (2009) 19, 6386-6391. PubMed Europe PubMed DOI
Silvestri,R. Boom in the development of non-peptidic beta-secretase (BACE1) inhibitors for the treatment of Alzheimer's disease Med Res Rev (2009) 29, 295-338. PubMed Europe PubMed DOI V I
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 B (2009) 113, 2990-2999. PubMed Europe PubMed DOI
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 Lett (2009) 19, 2977-2980. PubMed Europe PubMed DOI I
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 Lett (2009) 19, 17-20. PubMed Europe PubMed DOI I
Tomita,T. Secretase inhibitors and modulators for Alzheimer's disease treatment Expert Rev Neurother (2009) 9, 661-679. PubMed Europe PubMed DOI V
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 Neurosci (2009) 29, 12787-12794. PubMed Europe PubMed DOI V
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 Chem (2009) 284, 3793-3803. PubMed Europe PubMed DOI PMC EPMC
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 Model (2009) 49, 647-657. PubMed Europe PubMed DOI I
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 Biochem (2009) 387, 208-220. PubMed Europe PubMed DOI A
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 Lett (2009) 19, 4711-4714. PubMed Europe PubMed DOI I
Willem,M., Lammich,S. and Haass,C. Function, regulation and therapeutic properties of beta-secretase (BACE1) Semin Cell Dev Biol (2009) 20, 175-182. PubMed Europe PubMed DOI
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 Lett (2009) 19, 3188-3192. PubMed Europe PubMed DOI I
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 Biochemistry (2009) 48, 4488-4496. PubMed Europe PubMed DOI S I
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 Lett (2009) 19, 6770-6774. PubMed Europe PubMed DOI I
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 Chem (2009) 17, 1600-1613. PubMed Europe PubMed DOI I
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 Sin (2009) 30, 259-269. PubMed Europe PubMed DOI I

2008

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 Chem (2008) 16, 9471-9486. PubMed Europe PubMed DOI I
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 Chem (2008) 51, 6259-6262. PubMed Europe PubMed DOI S I
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 Lett (2008) 18, 1022-1026. PubMed Europe PubMed DOI I
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 Chem (2008) 51, 3313-3317. PubMed Europe PubMed DOI I
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 Med (2008) 74, 1405-1408. PubMed Europe PubMed DOI I
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 Lett (2008) 18, 1011-1016. PubMed Europe PubMed DOI I
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 Lett (2008) 18, 1017-1021. PubMed Europe PubMed DOI I
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 Lett (2008) 18, 1063-1066. PubMed Europe PubMed DOI I
Cole,S.L. and Vassar,R. BACE1 structure and function in health and Alzheimer's disease Curr Alzheimer Res (2008) 5, 100-120. PubMed Europe PubMed DOI K
Cole,S.L. and Vassar,R. The role of amyloid precursor protein processing by BACE1, the beta-secretase, in Alzheimer disease pathophysiology J Biol Chem (2008) 283, 29621-29625. PubMed Europe PubMed DOI PMC EPMC K V T
Dunn,B.M. Editorial. BACE or beta-secretase - a target for drug discovery for treatment of Alzheimer's disease Protein Pept Lett (2008) 15, 118-118. PubMed Europe PubMed
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 Lett (2008) 15, 119-130. PubMed Europe PubMed E
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 Med (2008) 14, 723-730. PubMed Europe PubMed DOI
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Ghosh,A.K., Kumaragurubaran,N., Hong,L., Koelsh,G. and Tang,J. Memapsin 2 (beta-secretase) inhibitors: drug development Curr Alzheimer Res (2008) 5, 121-131. PubMed Europe PubMed DOI T I
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 Lett (2008) 18, 1031-1036. PubMed Europe PubMed DOI PMC EPMC S I
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 Chem (2008) 283, 11302-11311. PubMed Europe PubMed DOI
Hoyos Flight,M. Neurodegenerative disease: inhibiting beta-secretase where it matters Nat Rev Neurosci (2008) 9, 414-415. DOI
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 Chem (2008) 16, 10190-10197. PubMed Europe PubMed DOI I
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 Lett (2008) 18, 414-417. PubMed Europe PubMed DOI I
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 Lett (2008) 18, 418-422. PubMed Europe PubMed DOI I
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 Lett (2008) 18, 767-771. PubMed Europe PubMed DOI I
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 Rep (2008) 9, 916-922. PubMed Europe PubMed DOI PMC EPMC
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 Lett (2008) 18, 1304-1307. PubMed Europe PubMed DOI I
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 Med (2008) 74, 540-545. PubMed Europe PubMed DOI I
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 Lett (2008) 18, 2900-2904. PubMed Europe PubMed DOI I
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 Science (2008) 320, 520-523. PubMed Europe PubMed DOI I
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 Ther (2008) 324, 957-969. PubMed Europe PubMed DOI I
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 Chem (2008) 389, 313-320. PubMed Europe PubMed DOI
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 Biol (2008) 28, 3663-3671. PubMed Europe PubMed DOI PMC EPMC S
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 Acta (2008) 1780, 819-825. PubMed Europe PubMed DOI I
Small,D.H., Klaver,D.W. and Beckman,M. Regulation of proBACE1 by glycosaminoglycans Neurodegener Dis (2008) 5, 206-208. PubMed Europe PubMed DOI
Stockley,J.H. and O'Neill,C. Understanding BACE1: essential protease for amyloid-beta production in Alzheimer's disease Cell Mol Life Sci (2008) 65, 3265-3289. PubMed Europe PubMed DOI V
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 Neurochem (2008) 104, 683-695. PubMed Europe PubMed DOI PMC EPMC
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 Med (2008) 10, 368-376. PubMed Europe PubMed DOI M
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 Lett (2008) 15, 131-143. PubMed Europe PubMed E
Wong,P.C. Translational control of BACE1 may go awry in Alzheimer's disease Neuron (2008) 60, 941-943. PubMed Europe PubMed DOI
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 Chem (2008) 283, 26364-26373. PubMed Europe PubMed DOI PMC EPMC

2007

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 Chembiochem (2007) 8, 2078-2091. PubMed Europe PubMed DOI I
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 ChemMedChem (2007) 2, 995-999. PubMed Europe PubMed DOI I
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 Chem (2007) 50, 4261-4264. PubMed Europe PubMed DOI S I
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 Lett (2007) 48, 7990-7993. DOI I
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 J (2007) 21, 3184-3196. PubMed Europe PubMed DOI
Cole,S.L. and Vassar,R. The Alzheimer's disease beta-secretase enzyme, BACE1 Mol Neurodegener (2007) 2, 22-22. PubMed Europe PubMed DOI PMC EPMC V
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 Chem (2007) 50, 1124-1132. PubMed Europe PubMed DOI I
Edwards,P. Tetramic and tetronic acids as beta-secretase inhibitors Drug Discov Today (2007) 12, 345-346. DOI I
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 Chem (2007) 50, 5912-5925. PubMed Europe PubMed DOI I
Evin,G. and Kenche,V.B. BACE inhibitors as potential therapeutics for Alzheimer's disease Recent Patents CNS Drug Discov (2007) 2, 188-199. PubMed Europe PubMed DOI V T I
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 Lett (2007) 17, 5353-5356. PubMed Europe PubMed DOI I
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 Lett (2007) 17, 78-81. PubMed Europe PubMed DOI I
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 Lett (2007) 17, 73-77. PubMed Europe PubMed DOI I
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 Chem (2007) 50, 5903-5911. PubMed Europe PubMed DOI I
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 Chem (2007) 50, 2399-2407. PubMed Europe PubMed DOI S I
Ghosh,A.K., Bilcer,G., Hong,L., Koelsch,G. and Tang,J. Memapsin 2 (beta-secretase) inhibitor drug, between fantasy and reality Curr Alzheimer Res (2007) 4, 418-422. PubMed Europe PubMed DOI
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 Dis (2007) 4, 127-135. PubMed Europe PubMed DOI
Hills,I.D. and Vacca,J.P. Progress toward a practical BACE-1 inhibitor Curr Opin Drug Discov Devel (2007) 10, 383-391. PubMed Europe PubMed I
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 Neurochem (2007) 100, 802-809. PubMed Europe PubMed DOI I
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 Lett (2007) 17, 3378-3383. PubMed Europe PubMed DOI I
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 Res (2007) 85, 153-165. PubMed Europe PubMed DOI
Lee,D.H., Lee,D.H. and Lee,J.S. Characterization of a new antidementia beta-secretase inhibitory peptide from Saccharomyces cerevisiae Enzyme Microb Technol (2007) 42, 83-88. DOI I
Lee,H.W., Seo,H.S., Ha,I. and Chung,S.H. Overexpression of BACE1 stimulates spontaneous basal secretion in PC12 cells Neurosci Lett (2007) 421, 178-183. PubMed Europe PubMed DOI
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 Lett (2007) 17, 4057-4061. PubMed Europe PubMed DOI I
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 Commun (2007) 362, 25-30. PubMed Europe PubMed DOI L
[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 Chem (22-2-2007) 50, 776-781. PubMed Europe PubMed DOI I
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 Chem (2007) 15, 4136-4143. PubMed Europe PubMed DOI I
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 Chem (2007) 282, 26326-26334. PubMed Europe PubMed DOI K
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 Lett (2007) 17, 1117-1121. PubMed Europe PubMed DOI I
McGaughey,G.B. and Holloway,M.K. Structure-guided design of beta-secretase (BACE-1) inhibitors Expert Opin Drug Discov (2007) 2, 1129-1138. PubMed Europe PubMed DOI V I
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 Lett (2007) 17, 5831-5835. PubMed Europe PubMed DOI I
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 Chem (2007) 50, 1116-1123. PubMed Europe PubMed DOI
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 Neurochem (2007) 101, 1583-1595. PubMed Europe PubMed DOI
Olson,R.E. and Marcin,L.R. Chapter 3 Secretase Inhibitors and Modulators for the Treatment of Alzheimer's Disease Annu Rep Med Chem (2007) 42, 27-47. DOI V I
Polgar,T., Magyar,C., Simon,I. and Keseru,G.M. Impact of ligand protonation on virtual screening against beta-secretase (BACE1) J Chem Inf Model (2007) 47, 2366-2373. PubMed Europe PubMed DOI
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 Chem (2007) 50, 3431-3433. PubMed Europe PubMed DOI I
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 Lett (2007) 17, 1788-1792. PubMed Europe PubMed DOI I
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 Chem (2007) 282, 34896-34903. PubMed Europe PubMed DOI
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 Lett (2007) 428, 103-108. PubMed Europe PubMed DOI R
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 Communications (2007) 37, 9-24. DOI I
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 Psychiatry (2007) 64, 718-726. PubMed Europe PubMed DOI
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 Chem (2007) 31, 186-195. PubMed Europe PubMed DOI

2006

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 Neurochem (2006) 96, 533-540. PubMed Europe PubMed DOI I
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 Inhib (2006) 2, 311-328. DOI
[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 Peptides (28-3-2006) 27, 1877-1885. PubMed Europe PubMed DOI I
[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 Lett (9-5-2006) 16, 3635-3638. PubMed Europe PubMed DOI I
[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 Chem (19-10-2006) 49, 6158-6161. PubMed Europe PubMed DOI I
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 Ban (2006) 37, 821-824. PubMed Europe PubMed
Durham,T.B. and Shepherd,T.A. Progress toward the discovery and development of efficacious BACE inhibitors Curr Opin Drug Discov Devel (2006) 9, 776-791. PubMed Europe PubMed I
[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 Lett (10-1-2006) 16, 1995-1999. PubMed Europe PubMed DOI I
[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 Chem (13-7-2006) 49, 4275-4285. PubMed Europe PubMed DOI I
[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 Soc (26-4-2006) 128, 5310-5311. PubMed Europe PubMed DOI PMC EPMC S I
Guo,T. and Hobbs,D.W. Development of BACE1 inhibitors for Alzheimer's disease Curr Med Chem (2006) 13, 1811-1829. PubMed Europe PubMed DOI V I
[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 Lett (3-6-2006) 16, 4354-4359. PubMed Europe PubMed DOI I
[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 Chem (27-7-2006) 49, 4544-4567. PubMed Europe PubMed DOI I
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 Ban (2006) 35, 622-629. PubMed Europe PubMed
John,V. Human beta-secretase (BACE) and BACE inhibitors: progress report Curr Top Med Chem (2006) 6, 569-578. PubMed Europe PubMed DOI V I
[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 Lett (13-2-2006) 16, 2380-2386. PubMed Europe PubMed DOI I
Larbig,G. and Schmidt,B. Synthesis of tetramic and tetronic acids as beta-secretase inhibitors J Comb Chem (2006) 8, 480-490. PubMed Europe PubMed DOI I
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 Neurosci (2006) 29, 81-99. PubMed Europe PubMed DOI
[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 Chem (5-10-2006) 49, 5885-5894. PubMed Europe PubMed DOI I
[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 Chem (14-12-2006) 49, 7270-7273. PubMed Europe PubMed DOI I
[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 Lett (21-10-2006) 16, 191-195. PubMed Europe PubMed DOI S I
Schmidt,B., Baumann,S., Braun,H.A. and Larbig,G. Inhibitors and modulators of beta- and gamma-secretase Curr Top Med Chem (2006) 6, 377-392. PubMed Europe PubMed DOI I
[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 Chem (19-10-2006) 49, 6147-6150. PubMed Europe PubMed DOI I
[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 Chem (13-4-2006) 52, 1168-1174. PubMed Europe PubMed DOI A
[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 Science (21-9-2006) 314, 664-666. PubMed Europe PubMed DOI K
[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 Chem (27-2-2006) 14, 4535-4551. PubMed Europe PubMed DOI I
[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 Chem (9-2-2006) 49, 839-842. PubMed Europe PubMed DOI S I
[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 Dis (8-2-2006) 22, 435-444. PubMed Europe PubMed DOI
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 Comput (2006) 2, 1057-1069. PubMed Europe PubMed DOI PMC EPMC S

2005

[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 Chem (18-2-2005) 280, 17930-17937. PubMed Europe PubMed DOI
[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 Polym (4-8-2005) 61, 198-202. I
[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 Biotechnol (6-4-2005) 116, 359-367. PubMed Europe PubMed DOI E
[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 Purif (13-9-2005) 44, 87-93. PubMed Europe PubMed DOI E
[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 Lett (3-1-2005) 15, 15-20. PubMed Europe PubMed DOI I
Ghosh,A.K., Kumaragurubaran,N. and Tang,J. Recent developments of structure based beta-secretase inhibitors for Alzheimer's disease Curr Top Med Chem (2005) 5, 1609-1622. PubMed Europe PubMed DOI V I
Gorfe,A.A. and Caflisch,A. Functional plasticity in the substrate binding site of beta-secretase Structure (2005) 13, 1487-1498. PubMed Europe PubMed DOI
[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 Chem (11-8-2005) 48, 5175-5190. PubMed Europe PubMed DOI I
[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 Chem (21-12-2005) 280, 11696-11703. PubMed Europe PubMed DOI
[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 Chem (11-8-2005) 48, 5108-5111. PubMed Europe PubMed DOI I
[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 Chem (22-8-2005) 280, 36815-36823. PubMed Europe PubMed DOI
[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 Lett (3-1-2005) 15, 211-215. PubMed Europe PubMed DOI I
[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 Chem (13-9-2005) 280, 8589-8595. PubMed Europe PubMed DOI
[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 Biochemistry (30-8-2005) 44, 11567-11573. PubMed Europe PubMed DOI
[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 Neurosci (14-12-2005) 25, 11693-11709. PubMed Europe PubMed DOI PMC EPMC K
[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 Biol (17-1-2005) 168, 291-302. PubMed Europe PubMed DOI PMC EPMC K
[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 Pharmacol (7-3-2005) 145, 228-235. PubMed Europe PubMed DOI PMC EPMC I
[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 Biochem (1-7-2005) 342, 144-151. PubMed Europe PubMed DOI A
[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 Chem (2-6-2005) 48, 3749-3755. PubMed Europe PubMed DOI I
Porcari,V., Magnoni,L., Terstappen,G.C. and Fecke,W. A continuous time-resolved fluorescence assay for identification of BACE1 inhibitors Assay Drug Dev Technol (2005) 3, 287-297. PubMed Europe PubMed DOI A
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 Neurochem (2005) 92, 226-234. PubMed Europe PubMed DOI
Tang,J., He,X., Huang,X. and Hong,L. Recent developments on the studies of human memapsin 2 (beta-secretase) Curr Alzheimer Res (2005) 2, 261-264. PubMed Europe PubMed DOI V
Thompson,L.A., Bronson,J.J. and Zusi,F.C. Progress in the discovery of BACE inhibitors Curr Pharm Des (2005) 11, 3383-3404. PubMed Europe PubMed DOI V I
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) (2005) 112, 455-469. PubMed Europe PubMed DOI
[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) Biochemistry (11-1-2005) 44, 105-112. PubMed Europe PubMed DOI
Vassar,R. beta-Secretase, APP and Abeta in Alzheimer's disease Subcell Biochem (2005) 38, 79-103. PubMed Europe PubMed
[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 Chem (4-3-2005) 280, 17777-17785. PubMed Europe PubMed DOI
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 Chem (2005) 280, 23009-23017. PubMed Europe PubMed DOI
[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 Chem (15-3-2005) 13, 2121-2131. PubMed Europe PubMed DOI I

2004

[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 Lett (9-2-2004) 14, 601-604. PubMed Europe PubMed DOI I
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 Neurochem (2004) 89, 1409-1416. PubMed Europe PubMed DOI I
[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 Chem (27-9-2004) 279, 52535-52542. PubMed Europe PubMed DOI PMC EPMC
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 Biol (2004) 24, 865-874. PubMed Europe PubMed DOI PMC EPMC
Citron,M. Beta-secretase inhibition for the treatment of Alzheimer's disease - promise and challenge Trends Pharmacol Sci (2004) 25, 92-97. PubMed Europe PubMed DOI
[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 Chem (2-12-2004) 47, 6117-6119. PubMed Europe PubMed DOI I
Cumming,J.N., Iserloh,U. and Kennedy,M.E. Design and development of BACE-1 inhibitors Curr Opin Drug Discov Devel (2004) 7, 536-556. PubMed Europe PubMed I
Dominguez,D.I., Hartmann,D. and De Strooper,B. BACE1 and presenilin: two unusual aspartyl proteases involved in Alzheimer's disease Neurodegener Dis (2004) 1, 168-174. PubMed Europe PubMed DOI
[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 J (1-4-2004) 18, 1037-1039. PubMed Europe PubMed DOI
[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 Chem (1-1-2004) 47, 158-164. PubMed Europe PubMed DOI I
[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 Biochemistry (27-4-2004) 43, 4689-4695. PubMed Europe PubMed DOI S
[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 Lett (5-7-2004) 14, 3457-3460. PubMed Europe PubMed DOI I
Hussain,I. The potential for BACE1 inhibitors in the treatment of Alzheimer's disease IDrugs (2004) 7, 653-658. PubMed Europe PubMed I
[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 Lett (22-3-2004) 14, 1527-1531. PubMed Europe PubMed DOI I
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 J (2004) 21, 25-29. PubMed Europe PubMed DOI
Kitazume,S., Saido,T.C. and Hashimoto,Y. Alzheimer's beta-secretase cleaves a glycosyltransferase as a physiological substrate Glycoconj J (2004) 20, 59-62. PubMed Europe PubMed DOI
[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 Lett (5-1-2004) 14, 239-243. PubMed Europe PubMed DOI I
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 Rep (2004) 5, 620-625. PubMed Europe PubMed DOI PMC EPMC
[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 Chem (29-12-2004) 279, 10542-10550. PubMed Europe PubMed DOI
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 NMR (2004) 29, 425-426. PubMed Europe PubMed DOI
Mohajeri,M.H., Saini,K.D. and Nitsch,R.M. Transgenic BACE expression in mouse neurons accelerates amyloid plaque pathology J Neural Transm (2004) 111, 413-425. PubMed Europe PubMed DOI
[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 Neuron (8-1-2004) 41, 27-33. PubMed Europe PubMed DOI
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 Neurosci (2004) 25, 642-649. PubMed Europe PubMed DOI
[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 Biol (15-10-2004) 343, 407-416. PubMed Europe PubMed DOI S I
[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 Chem (10-9-2004) 279, 39010-39016. PubMed Europe PubMed DOI
Qing,H., Zhou,W., Christensen,M.A., Sun,X., Tong,Y. and Song,W. Degradation of BACE by the ubiquitin-proteasome pathway FASEB J (2004) 18, 1571-1573. PubMed Europe PubMed DOI
[YEAR:7-10-2004]Rajamani,R. and Reynolds,C.H. Modeling the protonation states of the catalytic aspartates in beta-secretase J Med Chem (7-10-2004) 47, 5159-5166. PubMed Europe PubMed DOI
[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 A (2-3-2004) 101, 2794-2799. PubMed Europe PubMed DOI PMC EPMC
[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 J (1-4-2004) 18, 1034-1036. PubMed Europe PubMed DOI
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 Purif (2004) 34, 190-196. PubMed Europe PubMed DOI
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 Traffic (2004) 5, 437-448. PubMed Europe PubMed DOI
[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 Chem (16-12-2004) 47, 6447-6450. PubMed Europe PubMed DOI I
Tang,J. and Koelsch,G. Memapsin 2 [ISSN:0-12-079610-4] (2004) 2, 66-69. V
Vassar,R. BACE1: the beta-secretase enzyme in Alzheimer's disease J Mol Neurosci (2004) 23, 105-114. PubMed Europe PubMed DOI K
[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 Sci (15-10-2004) 117, 5437-5445. PubMed Europe PubMed DOI
[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 Acta (6-5-2004) 1698, 255-259. PubMed Europe PubMed DOI
[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 Chem (12-10-2004) 279, 53205-53212. PubMed Europe PubMed DOI
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 Pathol (2004) 165, 1621-1631. PubMed Europe PubMed PMC EPMC K
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 Sin (2004) 25, 705-713. PubMed Europe PubMed
[YEAR:3-12-2004]Yamamoto,R., Yoneda,S. and Hara,H. Neuroprotective effects of beta-secretase inhibitors against rat retinal ganglion cell death Neurosci Lett (3-12-2004) 370, 61-64. PubMed Europe PubMed DOI I
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 Neurochem (2004) 91, 1249-1259. PubMed Europe PubMed DOI
Zhou,W., Qing,H., Tong,Y. and Song,W. BACE1 Gene Expression and Protein Degradation Ann N Y Acad Sci (2004) 1035, 49-67. PubMed Europe PubMed DOI

2003

[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 Chem (11-7-2003) 278, 25859-25866. PubMed Europe PubMed DOI A
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 Chem (2003) 278, 31512-31520. PubMed Europe PubMed DOI
[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 Genet (15-5-2003) 119B, 44-47. PubMed Europe PubMed DOI M
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 Neurosci (2003) 24, 646-655. PubMed Europe PubMed DOI
[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 Biochemistry (28-10-2003) 42, 12174-12180. PubMed Europe PubMed DOI
[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 Res (1-11-2003) 74, 393-405. PubMed Europe PubMed DOI
[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 Chem (9-5-2003) 278, 17141-17149. PubMed Europe PubMed DOI
[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 Chem (19-9-2003) 278, 36264-36268. PubMed Europe PubMed DOI
[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 Chem (23-10-2003) 46, 4625-4630. PubMed Europe PubMed DOI V I
[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 Biochem (1-8-2003) 319, 49-55. PubMed Europe PubMed DOI A I
[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 Neuroreport (1-7-2003) 14, 1243-1246. PubMed Europe PubMed DOI M
[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 Chem (25-4-2003) 278, 14865-14871. PubMed Europe PubMed DOI
[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 Res (1-7-2003) 73, 73-80. PubMed Europe PubMed DOI
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 Chem (2003) 278, 48713-48719. PubMed Europe PubMed DOI
Marlow,L., Cain,M., Pappolla,M.A. and Sambamurti,K. Beta-secretase processing of the Alzheimer's amyloid protein precursor (APP) J Mol Neurosci (2003) 20, 233-239. PubMed Europe PubMed DOI
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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 Dis (2003) 14, 291-301. PubMed Europe PubMed DOI
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 Neurosci (2003) 20, 299-304. PubMed Europe PubMed DOI I
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 Neurochem (2003) 84, 1006-1017. PubMed Europe PubMed DOI
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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 Neurol (2003) 179, 150-158. PubMed Europe PubMed DOI
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2002

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 Neurochem (2002) 80, 799-806. PubMed Europe PubMed DOI
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 Purif (2002) 26, 139-148. PubMed Europe PubMed DOI
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[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 Commun (26-4-2002) 293, 30-37. PubMed Europe PubMed DOI R
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 Neurochem (2002) 80, 1079-1088. PubMed Europe PubMed DOI
Ghosh,A.K., Hong,L. and Tang,J. beta-Secretase as a therapeutic target for inhibitor drugs Curr Med Chem (2002) 9, 1135-1144. PubMed Europe PubMed I
[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 Chem (15-2-2002) 277, 4687-4693. PubMed Europe PubMed DOI P I
[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 Lett (31-7-2002) 524, 183-187. PubMed Europe PubMed DOI
[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 Biochemistry (10-9-2002) 41, 10963-10967. PubMed Europe PubMed DOI S I
Hong,L., Turner,R.T., III, Koelsch,G., Ghosh,A.K. and Tang,J. Memapsin 2 (beta-secretase) as a therapeutic target Biochem Soc Trans (2002) 30, 530-534. PubMed Europe PubMed DOI I
[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 Biochemistry (5-3-2002) 41, 3128-3136. PubMed Europe PubMed DOI
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 Neurosci (2002) 19, 175-185. PubMed Europe PubMed DOI
[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 Chem (17-1-2002) 45, 259-262. PubMed Europe PubMed DOI I
[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 Biochemistry (9-7-2002) 41, 8742-8746. PubMed Europe PubMed DOI P I
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2001

[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 Chem (6-4-2001) 276, 10879-10887. PubMed Europe PubMed DOI
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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 Neurosci (2001) 4, 233-234. PubMed Europe PubMed DOI
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 Chem (2001) 276, 16739-16748. PubMed Europe PubMed DOI
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Jhee,S., Shiovitz,T., Crawford,A.W. and Cutler,N.R. beta-amyloid therapies in Alzheimer's disease Expert Opin Investig Drugs (2001) 10, 593-605. PubMed Europe PubMed DOI
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 A (2001) 98, 13554-13559. PubMed Europe PubMed DOI PMC EPMC
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 Neurosci (2001) 4, 231-232. PubMed Europe PubMed DOI
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 Pharmacol (2001) 59, 619-626. PubMed Europe PubMed E
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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 J (2001) 15, 1810-1812. PubMed Europe PubMed I
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Vassar,R. The beta-secretase, BACE: a prime drug target for Alzheimer's disease J Mol Neurosci (2001) 17, 157-170. PubMed Europe PubMed DOI
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 Chem (2001) 276, 14634-14641. PubMed Europe PubMed DOI
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2000

[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 Chem (1-12-2000) 275, 37712-37717. PubMed Europe PubMed DOI
[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 Chem (6-10-2000) 275, 30849-30854. PubMed Europe PubMed DOI I
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Potter,H. and Dressler,D. The potential of BACE inhibitors for Alzheimer's therapy Nat Biotechnol (2000) 18, 125-126. PubMed Europe PubMed DOI I
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1999

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 Neurosci (1999) 14, 419-427. PubMed Europe PubMed DOI
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1996

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 A (1996) 93, 13170-13175. PubMed Europe PubMed DOI PMC EPMC