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Page 1
Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase.
Barrow JC, Stauffer SR, Rittle KE, Ngo PL, Yang Z, Selnick HG, Graham SL, Munshi S, McGaughey GB, Holloway MK, Simon AJ, Price EA, Sankaranarayanan S, Colussi D, Tugusheva K, Lai MT, Espeseth AS, Xu M, Huang Q, Wolfe A, Pietrak B, Zuck P, Levorse DA, Hazuda D, Vacca JP. Barrow JC, et al. Among authors: lai mt. J Med Chem. 2008 Oct 23;51(20):6259-62. doi: 10.1021/jm800914n. Epub 2008 Sep 24. J Med Chem. 2008. PMID: 18811140
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: lai mt. 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: lai mt. 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: lai mt. 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: lai mt. 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.
Conformationally biased P3 amide replacements of beta-secretase inhibitors.
Stachel SJ, Coburn CA, Steele TG, Crouthamel MC, Pietrak BL, Lai MT, Holloway MK, Munshi SK, Graham SL, Vacca JP. Stachel SJ, et al. Among authors: lai mt. Bioorg Med Chem Lett. 2006 Feb;16(3):641-4. doi: 10.1016/j.bmcl.2005.10.032. Epub 2005 Nov 2. Bioorg Med Chem Lett. 2006. PMID: 16263281
BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres.
Coburn CA, Stachel SJ, Jones KG, Steele TG, Rush DM, DiMuzio J, Pietrak BL, Lai MT, Huang Q, Lineberger J, Jin L, Munshi S, Katharine Holloway M, Espeseth A, Simon A, Hazuda D, Graham SL, Vacca JP. Coburn CA, et al. Among authors: lai mt. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3635-8. doi: 10.1016/j.bmcl.2006.04.076. Epub 2006 May 11. Bioorg Med Chem Lett. 2006. PMID: 16690314
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: lai mt. 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: lai mt. J Med Chem. 2006 Dec 14;49(25):7270-3. doi: 10.1021/jm061046r. J Med Chem. 2006. PMID: 17149856
172 results