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Identification of a small molecule nonpeptide active site beta-secretase inhibitor that displays a nontraditional binding mode for aspartyl proteases.
Coburn CA, Stachel SJ, Li YM, Rush DM, Steele TG, Chen-Dodson E, Holloway MK, Xu M, Huang Q, Lai MT, DiMuzio J, Crouthamel MC, Shi XP, Sardana V, Chen Z, Munshi S, Kuo L, Makara GM, Annis DA, Tadikonda PK, Nash HM, Vacca JP, Wang T. Coburn CA, et al. Among authors: li ym. J Med Chem. 2004 Dec 2;47(25):6117-9. doi: 10.1021/jm049388p. J Med Chem. 2004. PMID: 15566281
Compounds that bind APP and inhibit Abeta processing in vitro suggest a novel approach to Alzheimer disease therapeutics.
Espeseth AS, Xu M, Huang Q, Coburn CA, Jones KL, Ferrer M, Zuck PD, Strulovici B, Price EA, Wu G, Wolfe AL, Lineberger JE, Sardana M, Tugusheva K, Pietrak BL, Crouthamel MC, Lai MT, Dodson EC, Bazzo R, Shi XP, Simon AJ, Li Y, Hazuda DJ. Espeseth AS, et al. J Biol Chem. 2005 May 6;280(18):17792-7. doi: 10.1074/jbc.M414331200. Epub 2005 Feb 25. J Biol Chem. 2005. PMID: 15737955 Free article.
A presenilin-independent aspartyl protease prefers the gamma-42 site cleavage.
Lai MT, Crouthamel MC, DiMuzio J, Pietrak BL, Donoviel DB, Bernstein A, Gardell SJ, Li YM, Hazuda D. Lai MT, et al. Among authors: li ym. J Neurochem. 2006 Jan;96(1):118-25. doi: 10.1111/j.1471-4159.2005.03528.x. Epub 2005 Nov 21. J Neurochem. 2006. PMID: 16300640 Free article.
Novel mutations introduced at the beta-site of amyloid beta protein precursor enhance the production of amyloid beta peptide by BACE1 in vitro and in cells.
Shi XP, Tugusheva K, Bruce JE, Lucka A, Chen-Dodson E, Hu B, Wu GX, Price E, Register RB, Lineberger J, Miller R, Tang MJ, Espeseth A, Kahana J, Wolfe A, Crouthamel MC, Sankaranarayanan S, Simon A, Chen L, Lai MT, Pietrak B, DiMuzio J, Li Y, Xu M, Huang Q, Garsky V, Sardana MK, Hazuda DJ. Shi XP, et al. J Alzheimers Dis. 2005 Apr;7(2):139-48; discussion 173-80. doi: 10.3233/jad-2005-7207. J Alzheimers Dis. 2005. PMID: 15851852
2,672 results