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Literature for peptidase A01.041: BACE2 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, I Inhibitor, U Therapeutic. To select only the references relevant to a single topic, click the link above. See explanation.)

    2025
  1. Beguin,A., Chasseriaud,M., Hollaender,G., Jacob,Y., Mousseau,G., Heidmann,T. and Heidmann,O.
    The human endogenous retroviral envelope HEMO protein interacts with BACE2: Novel partnership acquired in the primate lineage
    Proc Natl Acad Sci U S A (2025) 122, e2515527122-e2515527122. PubMed  Europe PubMed DOI  PMC  EPMC
    2. 2024
  2. Guan,D., Sun,S., Song,L., Zhao,P., Nie,Y., Huang,X., Zhou,W., Yan,L., Lei,Y., Hu,Y. and Wei,F.
    Taking a color photo: A homozygous 25-bp deletion in Bace2 may cause brown-and-white coat color in giant pandas
    Proc Natl Acad Sci U S A (2024) 121, e2317430121-e2317430121. PubMed  Europe PubMed DOI  PMC  EPMC
  3. 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
    4. 2023
  4. He,T., d'Uscio,L.V. and Katusic,Z.S.
    BACE2 deficiency impairs expression and function of endothelial nitric oxide synthase in brain endothelial cells
    J Neurochem (2023) 166, 928-942. PubMed  Europe PubMed DOI  PMC  EPMC
  5. Saez-Valero,J. and Perez-Gonzalez,R.
    BACE2 beyond beta-processing of APP, its neuroprotective role in cerebrovascular endothelium
    J Neurochem (2023) 166, 887-890. PubMed  Europe PubMed DOI
    6. 2021
  6. 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
  7. Yen,Y.C., Kammeyer,A.M., Tirlangi,J., Ghosh,A.K. and Mesecar,A.D.
    A Structure-Based Discovery Platform for BACE2 and the Development of Selective BACE Inhibitors
    ACS Chem Neurosci (2021) 12, 581-588. PubMed  Europe PubMed DOI
    8. 2019
  8. 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
  9. Wang,Z., Xu,Q., Cai,F., Liu,X., Wu,Y. and Song,W.
    BACE2, a conditional beta-secretase, contributes to Alzheimer's disease pathogenesis
    JCI Insight (2019) 4 PubMed  Europe PubMed DOI
    10. 2018
  10. 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
  11. Liu,F., Zhang,Y., Liang,Z., Sun,Q., Liu,H., Zhao,J., Xu,J., Zheng,J., Yun,Y., Yu,X., Song,W. and Sun,X.
    Cleavage of potassium channel Kv2.1 by BACE2 reduces neuronal apoptosis
    Mol Psychiatry (2018) 23, 1542-1554. PubMed  Europe PubMed DOI
    12. 2017
  12. Alcarraz-Vizan,G., Castano,C., Visa,M., Montane,J., Servitja,J.M. and Novials,A.
    BACE2 suppression promotes beta-cell survival and function in a model of type 2 diabetes induced by human islet amyloid polypeptide overexpression
    Cell Mol Life Sci (2017) 74, 2827-2838. PubMed  Europe PubMed DOI
  13. 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
    14. 2016
  14. Ghosh,A.K., Reddy,B.S., Yen,Y.C., Cardenas,E., Rao,K.V., Downs,D., Huang,X., Tang,J. and Mesecar,A.D.
    Design of potent and highly selective inhibitors for human beta-secretase 2 (memapsin 1), a target for type 2 diabetes
    Chem Sci (2016) 7, 3117-3122. PubMed  Europe PubMed DOI  PMC  EPMC  I
  15. 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
  16. Rulifson,I.C., Cao,P., Miao,L., Kopecky,D., Huang,L., White,R.D., Samayoa,K., Gardner,J., Wu,X., Chen,K., Tsuruda,T., Homann,O., Baribault,H., Yamane,H., Carlson,T., Wiltzius,J. and Li,Y.
    Identification of human islet amyloid polypeptide as a BACE2 substrate
    PLoS ONE (2016) 11, e0147254-e0147254. PubMed  Europe PubMed DOI  PMC  EPMC  U
  17. 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
    18. 2015
  18. Alcarraz-Vizan,G., Casini,P., Cadavez,L., Visa,M., Montane,J., Servitja,J.M. and Novials,A.
    Inhibition of BACE2 counteracts hIAPP-induced insulin secretory defects in pancreatic beta-cells
    FASEB J (2015) 29, 95-104. PubMed  Europe PubMed DOI
  19. 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
    20. 2014
  20. 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
  21. 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
    22. 2013
  22. Banner,D.W., Gsell,B., Benz,J., Bertschinger,J., Burger,D., Brack,S., Cuppuleri,S., Debulpaep,M., Gast,A., Grabulovski,D., Hennig,M., Hilpert,H., Huber,W., Kuglstatter,A., Kusznir,E., Laeremans,T., Matile,H., Miscenic,C., Rufer,A.C., Schlatter,D., Steyaert,J., Stihle,M., Thoma,R., Weber,M. and Ruf,A.
    Mapping the conformational space accessible to BACE2 using surface mutants and cocrystals with Fab fragments, Fynomers and Xaperones
    Acta Crystallogr D Biol Crystallogr (2013) 69, 1124-1137. PubMed  Europe PubMed DOI  S
  23. 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
  24. 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
  25. Southan,C.
    BACE2 as a new diabetes target: a patent review (2010 - 2012)
    Expert Opin Ther Pat (2013) 23, 649-663. PubMed  Europe PubMed DOI  I
  26. 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
    27. 2012
  27. Abdul-Hay,S.O., Sahara,T., McBride,M., Kang,D. and Leissring,M.A.
    Identification of BACE2 as an avid beta-amyloid degrading protease
    Mol Neurodegener (2012) 7, 46-46. PubMed  Europe PubMed DOI
  28. Tang,J. and Koelsch,G.
    Memapsin 1
    [ISSN:978-0-12-407744-7] (2012) 3, 85-87. DOI
    29. 2011
  29. Esterhazy,D., Stutzer,I., Wang,H., Rechsteiner,M.P., Beauchamp,J., Dobeli,H., Hilpert,H., Matile,H., Prummer,M., Schmidt,A., Lieske,N., Boehm,B., Marselli,L., Bosco,D., Kerr-Conte,J., Aebersold,R., Spinas,G.A., Moch,H., Migliorini,C. and Stoffel,M.
    Bace2 is a beta cell-enriched protease that regulates pancreatic beta cell function and mass
    Cell Metab (2011) 14, 365-377. PubMed  Europe PubMed DOI  K  T  I
    30. 2010
  30. Azkona,G., Levannon,D., Groner,Y. and Dierssen,M.
    In vivo effects of APP are not exacerbated by BACE2 co-overexpression: behavioural characterization of a double transgenic mouse model
    Amino Acids (2010) 39, 1571-1580. PubMed  Europe PubMed DOI
  31. Casas,S., Casini,P., Piquer,S., Altirriba,J., Soty,M., Cadavez,L., Gomis,R. and Novials,A.
    BACE2 plays a role in the insulin receptor trafficking in pancreatic beta-cells
    Am J Physiol Endocrinol Metab (2010) 299, E1087-E1095. PubMed  Europe PubMed DOI
    32. 2009
  32. Emmons,T.L., Mildner,A.M., Lull,J.M., Leone,J.W., Fischer,H.D., Heinrikson,R.L. and Tomasselli,A.G.
    Large scale refolding and purification of the catalytic domain of human BACE-2 produced in E. coli
    Protein Pept Lett (2009) 16, 121-131. PubMed  Europe PubMed DOI  E
    33. 2008
  33. Finzi,G., Franzi,F., Placidi,C., Acquati,F., Palumbo,E., Russo,A., Taramelli,R., Sessa,F. and La Rosa,S.
    BACE2 is stored in secretory granules of mouse and rat pancreatic beta cells
    Ultrastruct Pathol (2008) 32, 246-251. PubMed  Europe PubMed DOI
    34. 2006
  34. [YEAR:8-11-2006]Ostermann,N., Eder,J., Eidhoff,U., Zink,F., Hassiepen,U., Worpenberg,S., Maibaum,J., Simic,O., Hommel,U. and Gerhartz,B.
    Crystal structure of human BACE2 in complex with a hydroxyethylamine transition-state inhibitor
    J Mol Biol (8-11-2006) 355, 249-261. PubMed  Europe PubMed DOI  S  I
  35. Sun,X., He,G. and Song,W.
    BACE2, as a novel APP theta-secretase, is not responsible for the pathogenesis of Alzheimer's disease in Down syndrome
    FASEB J (2006) 20, 1369-1376. PubMed  Europe PubMed DOI
    36. 2004
  36. Chou,K.C.
    Insights from modeling the tertiary structure of human BACE2
    J Proteome Res (2004) 3, 1069-1072. PubMed  Europe PubMed DOI
  37. Tang,J. and Koelsch,G.
    Memapsin 1
    [ISSN:0-12-079610-4] (2004) 2, 64-66.  V
  38. Vassar,R.
    BACE1: the beta-secretase enzyme in Alzheimer's disease
    J Mol Neurosci (2004) 23, 105-114. PubMed  Europe PubMed DOI  K
    39. 2003
  39. [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
  40. Barbiero,L., Benussi,L., Ghidoni,R., Alberici,A., Russo,C., Schettini,G., Pagano,S.F., Parati,E.A., Mazzoli,F., Nicosia,F., Signorini,S., Feudatari,E. and Binetti,G.
    BACE-2 is overexpressed in Down's syndrome
    Exp Neurol (2003) 182, 335-345. PubMed  Europe PubMed DOI
  41. 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
  42. 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
    43. 2002
  43. Fluhrer,R., Capell,A., Westmeyer,G., Willem,M., Hartung,B., Condron,M.M., Teplow,D.B., Haass,C. and Walter,J.
    A non-amyloidogenic function of BACE-2 in the secretory pathway
    J Neurochem (2002) 81, 1011-1020. PubMed  Europe PubMed DOI
  44. Kim,Y.T., Downs,D., Wu,S., Dashti,A., Pan,Y., Zhai,P., Wang,X., Zhang,X.C. and Lin,X.
    Enzymic properties of recombinant BACE2
    Eur J Biochem (2002) 269, 5668-5677. PubMed  Europe PubMed DOI
  45. [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
    46. 2001
  46. [YEAR:29-6-2001]Hussain,I., Christie,G., Schneider,K., Moore,S. and Dingwall,C.
    Prodomain processing of Asp1 (BACE2) is autocatalytic
    J Biol Chem (29-6-2001) 276, 23322-23328. PubMed  Europe PubMed DOI
  47. [YEAR:3-7-2001]Nowotny,P., Kwon,J.M., Chakraverty,S., Nowotny,V., Morris,J.C. and Goate,A.M.
    Association studies using novel polymorphisms in BACE1 and BACE2
    Neuroreport (3-7-2001) 12, 1799-1802. PubMed  Europe PubMed  M
    48. 2000
  48. [YEAR:18-2-2000]Acquati,F., Accarino,M., Nucci,C., Fumagalli,P., Jovine,L., Ottolenghi,S. and Taramelli,R.
    The gene encoding DRAP (BACE2), a glycosylated transmembrane protein of the aspartic protease family, maps to the Down critical region
    FEBS Lett (18-2-2000) 468, 59-64. PubMed  Europe PubMed DOI
  49. [YEAR:7-7-2000]Bennett,B.D., Babu-Khan,S., Loeloff,R., Louis,J.C., Curran,E., Citron,M. and Vassar,R.
    Expression analysis of BACE2 in brain and peripheral tissues
    J Biol Chem (7-7-2000) 275, 20647-20651. PubMed  Europe PubMed DOI
  50. [YEAR:15-8-2000]Farzan,M., Schnitzler,C.E., Vasilieva,N., Leung,D. and Choe,H.
    BACE2, a beta-secretase homolog, cleaves at the beta site and within the amyloid-beta region of the amyloid-beta precursor protein
    Proc Natl Acad Sci U S A (15-8-2000) 97, 9712-9717. PubMed  Europe PubMed DOI  PMC  EPMC
  51. Hussain,I., Powell,D.J., Howlett,D.R., Chapman,G.A., Gilmour,L., Murdock,P.R., Tew,D.G., Meek,T.D., Chapman,C., Schneider,K., Ratcliffe,S.J., Tattersall,D., Testa,T.T., Southan,C., Ryan,D.M., Simmons,D.L., Walsh,F.S., Dingwall,C. and Christie,G.
    ASP1 (BACE2) cleaves the amyloid precursor protein at the beta-secretase site
    Mol Cell Neurosci (2000) 16, 609-619. PubMed  Europe PubMed DOI
  52. [YEAR:15-2-2000]Lin,X., Koelsch,G., Wu,S., Downs,D., Dashti,A. and Tang,J.
    Human aspartic protease memapsin 2 cleaves the beta-secretase site of beta-amyloid precursor protein
    Proc Natl Acad Sci U S A (15-2-2000) 97, 1456-1460. PubMed  Europe PubMed  PMC  EPMC
  53. Solans,A., Estivill,X. and de La Luna,S.
    A new aspartyl protease on 21q22.3, BACE2, is highly similar to Alzheimer's amyloid precursor protein beta-secretase
    Cytogenet Cell Genet (2000) 89, 177-184. PubMed  Europe PubMed
  54. Xin,H., Stephans,J.C., Duan,X., Harrowe,G., Kim,E., Grieshammer,U., Kingsley,C. and Giese,K.
    Identification of a novel aspartic-like protease differentially expressed in human breast cancer cell lines
    Biochim Biophys Acta (2000) 1501, 125-137. PubMed  Europe PubMed DOI
    55. 1999
  55. Saunders,A.J., Kim,T. and Tanzi,R.E.
    BACE2, a homolog of BACE, in the Down syndrome region of chromosome 21
    Science (1999) 286, 1255-1255.

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