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Page 1
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. Among authors: crouthamel mc. 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.
Rational design and synthesis of selective BACE-1 inhibitors.
Brady SF, Singh S, Crouthamel MC, Holloway MK, Coburn CA, Garsky VM, Bogusky M, Pennington MW, Vacca JP, Hazuda D, Lai MT. Brady SF, et al. Among authors: crouthamel mc. Bioorg Med Chem Lett. 2004 Feb 9;14(3):601-4. doi: 10.1016/j.bmcl.2003.11.061. Bioorg Med Chem Lett. 2004. PMID: 14741251
Presenilin-1 and presenilin-2 exhibit distinct yet overlapping gamma-secretase activities.
Lai MT, Chen E, Crouthamel MC, DiMuzio-Mower J, Xu M, Huang Q, Price E, Register RB, Shi XP, Donoviel DB, Bernstein A, Hazuda D, Gardell SJ, Li YM. Lai MT, et al. Among authors: crouthamel mc. J Biol Chem. 2003 Jun 20;278(25):22475-81. doi: 10.1074/jbc.M300974200. Epub 2003 Apr 8. J Biol Chem. 2003. PMID: 12684521 Free article.
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: crouthamel mc. J Med Chem. 2004 Dec 2;47(25):6117-9. doi: 10.1021/jm049388p. J Med Chem. 2004. PMID: 15566281
Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1).
Stachel SJ, Coburn CA, Steele TG, Jones KG, Loutzenhiser EF, Gregro AR, Rajapakse HA, Lai MT, Crouthamel MC, Xu M, Tugusheva K, Lineberger JE, Pietrak BL, Espeseth AS, Shi XP, Chen-Dodson E, Holloway MK, Munshi S, Simon AJ, Kuo L, Vacca JP. Stachel SJ, et al. Among authors: crouthamel mc. J Med Chem. 2004 Dec 16;47(26):6447-50. doi: 10.1021/jm049379g. J Med Chem. 2004. PMID: 15588077
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. Among authors: crouthamel mc. J Alzheimers Dis. 2005 Apr;7(2):139-48; discussion 173-80. doi: 10.3233/jad-2005-7207. J Alzheimers Dis. 2005. PMID: 15851852
Biochemical and cell-based assays for characterization of BACE-1 inhibitors.
Pietrak BL, Crouthamel MC, Tugusheva K, Lineberger JE, Xu M, DiMuzio JM, Steele T, Espeseth AS, Stachel SJ, Coburn CA, Graham SL, Vacca JP, Shi XP, Simon AJ, Hazuda DJ, Lai MT. Pietrak BL, et al. Among authors: crouthamel mc. Anal Biochem. 2005 Jul 1;342(1):144-51. doi: 10.1016/j.ab.2005.04.019. Anal Biochem. 2005. PMID: 15958191
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: crouthamel mc. 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.
Evaluating scoring functions for docking and designing beta-secretase inhibitors.
Katharine Holloway M, McGaughey GB, Coburn CA, Stachel SJ, Jones KG, Stanton EL, Gregro AR, Lai MT, Crouthamel MC, Pietrak BL, Munshi SK. Katharine Holloway M, et al. Among authors: crouthamel mc. Bioorg Med Chem Lett. 2007 Feb 1;17(3):823-7. doi: 10.1016/j.bmcl.2006.10.051. Epub 2006 Oct 25. Bioorg Med Chem Lett. 2007. PMID: 17107793
Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1).
Rajapakse HA, Nantermet PG, Selnick HG, Munshi S, McGaughey GB, Lindsley SR, Young MB, Lai MT, Espeseth AS, Shi XP, Colussi D, Pietrak B, Crouthamel MC, Tugusheva K, Huang Q, Xu M, Simon AJ, Kuo L, Hazuda DJ, Graham S, Vacca JP. Rajapakse HA, et al. Among authors: crouthamel mc. J Med Chem. 2006 Dec 14;49(25):7270-3. doi: 10.1021/jm061046r. J Med Chem. 2006. PMID: 17149856
20 results