Top ▲
Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
BACE1 (beta-secretase 1) Show summary »« Hide summary More detailed page
|
|||||||||||||||||||||||||||||||||||||||||||||||
BACE2 (beta-secretase 2) Show summary »« Hide summary More detailed page
|
|||||||||||||||||||||||||||||||||||||||||||||||
cathepsin D Show summary »« Hide summary More detailed page
|
|||||||||||||||||||||||||||||||||||||||||||||||
cathepsin E Show summary »« Hide summary More detailed page
|
|||||||||||||||||||||||||||||||||||||||||||||||
pepsinogen A5 Show summary »« Hide summary More detailed page
|
|||||||||||||||||||||||||||||||||||||||||||||||
progastricsin Show summary »« Hide summary More detailed page
|
|||||||||||||||||||||||||||||||||||||||||||||||
renin C Show summary »« Hide summary More detailed page
|
1. Banner D et.al. (2010) Dihydropyrimidinones for use as BACE2 inhibitors. Patent number: WO2010128058. Assignee: Roche. Priority date: 31/10/2014. Publication date: 11/11/2010.
2. Blass B. (2012) Compounds and Their Use as BACE Inhibitors: Patent Highlight. ACS Med Chem Lett, 3 (11): 875-6. [PMID:24900397]
3. Blass B. (2013) Cyclopropyl-Fused 1,3-Thiazepines as BACE1 and BACE2 Inhibitors. ACS Med Chem Lett, 4 (4): 379-80. [PMID:24900681]
4. Cheng Y, Brown J, Judd TC, Lopez P, Qian W, Powers TS, Chen JJ, Bartberger MD, Chen K, Dunn 2nd RT et al.. (2015) An Orally Available BACE1 Inhibitor That Affords Robust CNS Aβ Reduction without Cardiovascular Liabilities. ACS Med Chem Lett, 6 (2): 210-5. [PMID:25699151]
5. Dineen TA, Chen K, Cheng AC, Derakhchan K, Epstein O, Esmay J, Hickman D, Kreiman CE, Marx IE, Wahl RC et al.. (2014) Inhibitors of β-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, 57 (23): 9811-31. [PMID:25363711]
6. Eketjäll S, Janson J, Jeppsson F, Svanhagen A, Kolmodin K, Gustavsson S, Radesäter AC, Eliason K, Briem S, Appelkvist P et al.. (2013) 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, 33 (24): 10075-84. [PMID:23761903]
7. Esterházy D, Stützer I, Wang H, Rechsteiner MP, Beauchamp J, Döbeli H, Hilpert H, Matile H, Prummer M, Schmidt A et al.. (2011) Bace2 is a β cell-enriched protease that regulates pancreatic β cell function and mass. Cell Metab, 14 (3): 365-77. [PMID:21907142]
8. Fukumoto H, Takahashi H, Tarui N, Matsui J, Tomita T, Hirode M, Sagayama M, Maeda R, Kawamoto M, Hirai K et al.. (2010) A noncompetitive BACE1 inhibitor TAK-070 ameliorates Abeta pathology and behavioral deficits in a mouse model of Alzheimer's disease. J Neurosci, 30 (33): 11157-66. [PMID:20720123]
9. Ghosh AK, Reddy BS, Yen YC, Cardenas E, Rao KV, Downs D, Huang X, Tang J, Mesecar AD. (2016) Design of Potent and Highly Selective Inhibitors for Human β-Secretase 2 (Memapsin 1), a Target for Type 2 Diabetes. Chem Sci, 7: 3117-3122. [PMID:27347366]
10. Hilpert H, Guba W, Woltering TJ, Wostl W, Pinard E, Mauser H, Mayweg AV, Rogers-Evans M, Humm R, Krummenacher D et al.. (2013) β-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease. J Med Chem, 56 (10): 3980-95. [PMID:23590342]
11. Holenz J et al. (2011) 5h-pyrrolo[3,4- gbp >]pyrazin-7-amine derivatives inhibitors of beta-secretase. Patent number: WO2011002409. Assignee: AstraZeneca. Priority date: 03/07/2009. Publication date: 06/01/2011.
12. Jacobsen H, Ozmen L, Caruso A, Narquizian R, Hilpert H, Jacobsen B, Terwel D, Tanghe A, Bohrmann B. (2014) Combined treatment with a BACE inhibitor and anti-Aβ antibody gantenerumab enhances amyloid reduction in APPLondon mice. J Neurosci, 34 (35): 11621-30. [PMID:25164658]
13. Jeppsson F, Eketjäll S, Janson J, Karlström S, Gustavsson S, Olsson LL, Radesäter AC, Ploeger B, Cebers G, Kolmodin K et al.. (2012) Discovery of AZD3839, a potent and selective BACE1 inhibitor clinical candidate for the treatment of Alzheimer disease. J Biol Chem, 287 (49): 41245-57. [PMID:23048024]
14. Juichi, S et al.. (2009) Fused aminodihydrothiazine derivatives. Patent number: US20090209755. Assignee: Eisai. Priority date: 18/01/2008. Publication date: 20/08/2009.
15. Koriyama, Y. Discovery and synthesis of JNJ-54861911, a novel orally active BACE1 inhibitor. Accessed on 28/05/2018. Modified on 28/05/2018. CiteUlike, http://www.citeulike.org/user/cdsouthan/article/14595136
16. Mauser H etal. (2012) Bace inhibitors for use in the treatment of diabetes. Patent number: WO2012028563. Assignee: Roche. Priority date: 01/09/2009. Publication date: 08/03/2012.
17. May P, Boggs L, Brier R, Calligaro D, Citron M, Day T, Lin S, Lindstrom T, Mergott D, Monk S et al.. (2012) Preclinical characterizathion of LY2886721: A BACE1 inhibitor in clinical development for early Alzheimer's disease. Alzheimers Dement, 8 (4): 95.
18. May PC, Dean RA, Lowe SL, Martenyi F, Sheehan SM, Boggs LN, Monk SA, Mathes BM, Mergott DJ, Watson BM et al.. (2011) Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor. J Neurosci, 31 (46): 16507-16. [PMID:22090477]
19. Neumann U, Rueeger H, Machauer R, Veenstra SJ, Lueoend RM, Tintelnot-Blomley M, Laue G, Beltz K, Vogg B, Schmid P et al.. (2015) A novel BACE inhibitor NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in APP transgenic mice. Mol Neurodegener, 10: 44. [PMID:26336937]
20. O'Neill BT, Beck EM, Butler CR, Nolan CE, Gonzales C, Zhang L, Doran SD, Lapham K, Buzon LM, Dutra JK et al.. (2018) Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation. J Med Chem, 61 (10): 4476-4504. [PMID:29613789]
21. Ostermann N, Eder J, Eidhoff U, Zink F, Hassiepen U, Worpenberg S, Maibaum J, Simic O, Hommel U, Gerhartz B. (2006) Crystal structure of human BACE2 in complex with a hydroxyethylamine transition-state inhibitor. J Mol Biol, 355 (2): 249-61. [PMID:16305800]
22. Rueeger H et al.. (2012) Bace-2 inhibitors for the treatment of metabolic disorders. Patent number: WO2012095521. Assignee: Novartis. Priority date: 03/01/2011. Publication date: 19/07/2012.
23. Rueeger H, Lueoend R, Machauer R, Veenstra SJ, Jacobson LH, Staufenbiel M, Desrayaud S, Rondeau JM, Möbitz H, Neumann U. (2013) Discovery of cyclic sulfoxide hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure based design and in vivo reduction of amyloid β-peptides. Bioorg Med Chem Lett, 23 (19): 5300-6. [PMID:23981898]
24. Scott JD et al.. (2015) Iminothiadiazine dioxide compounds as BACE inhibitors, compositions, and their use. Patent number: US8940748. Assignee: Merck Sharp & Dohme. Priority date: 08/10/2009. Publication date: 27/01/2015.
25. Southan C. (2013) BACE2 as a new diabetes target: a patent review (2010 - 2012). Expert Opin Ther Pat, 23 (5): 649-63. [PMID:23506624]
26. Stamford AW, Scott JD, Li SW, Babu S, Tadesse D, Hunter R, Wu Y, Misiaszek J, Cumming JN, Gilbert EJ et al.. (2012) Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor that Affords Robust CNS Aβ Reduction. ACS Med Chem Lett, 3 (11): 897-902. [PMID:23412139]
27. Wood S, Wen PH, Zhang J, Zhu L, Luo Y, Babu-Khan S, Chen K, Pham R, Esmay J, Dineen TA et al.. (2012) Establishing the relationship between in vitro potency, pharmacokinetic, and pharmacodynamic parameters in a series of orally available, hydroxyethylamine-derived β-secretase inhibitors. J Pharmacol Exp Ther, 343 (2): 460-7. [PMID:22911925]
28. Wuerzner G, Azizi M. (2008) Renin inhibition with aliskiren. Clin Exp Pharmacol Physiol, 35 (4): 426-30. [PMID:18307734]
29. Zhang L, Chen L, Dutra JK, Beck EM, Nag S, Takano A, Amini N, Arakawa R, Brodney MA, Buzon LM et al.. (2018) Identification of a Novel Positron Emission Tomography (PET) Ligand for Imaging β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE-1) in Brain. J Med Chem, 61 (8): 3296-3308. [PMID:29356535]
Database page citation:
A1: Pepsin. Accessed on 04/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=726.
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Fabbro D, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Enzymes. Br J Pharmacol. 180 Suppl 2:S289-373.
This work is licensed under a Creative Commons Attribution-ShareAlike 4.0 International License