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Page 1
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
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
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.
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
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
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Lindsley SR, Moore KP, Rajapakse HA, Selnick HG, Young MB, Zhu H, Munshi S, Kuo L, McGaughey GB, Colussi D, Crouthamel MC, Lai MT, Pietrak B, Price EA, Sankaranarayanan S, Simon AJ, Seabrook GR, Hazuda DJ, Pudvah NT, Hochman JH, Graham SL, Vacca JP, Nantermet PG. Lindsley SR, et al. Among authors: crouthamel mc. Bioorg Med Chem Lett. 2007 Jul 15;17(14):4057-61. doi: 10.1016/j.bmcl.2007.04.072. Epub 2007 Apr 27. Bioorg Med Chem Lett. 2007. PMID: 17482814
SAR of tertiary carbinamine derived BACE1 inhibitors: role of aspartate ligand amine pKa in enzyme inhibition.
Rajapakse HA, Nantermet PG, Selnick HG, Barrow JC, McGaughey GB, Munshi S, Lindsley SR, Young MB, Ngo PL, Holloway MK, 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. Bioorg Med Chem Lett. 2010 Mar 15;20(6):1885-9. doi: 10.1016/j.bmcl.2010.01.137. Epub 2010 Feb 4. Bioorg Med Chem Lett. 2010. PMID: 20176482
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.
20 results