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Page 1
Discovery of pyrrolidine-based β-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency.
Stachel SJ, Steele TG, Petrocchi A, Haugabook SJ, McGaughey G, Katharine Holloway M, Allison T, Munshi S, Zuck P, Colussi D, Tugasheva K, Wolfe A, Graham SL, Vacca JP. Stachel SJ, et al. Among authors: munshi s. Bioorg Med Chem Lett. 2012 Jan 1;22(1):240-4. doi: 10.1016/j.bmcl.2011.11.024. Epub 2011 Nov 12. Bioorg Med Chem Lett. 2012. PMID: 22130130
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. 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
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. 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 and SAR of isonicotinamide BACE-1 inhibitors that bind beta-secretase in a N-terminal 10s-loop down conformation.
Stauffer SR, Stanton MG, Gregro AR, Steinbeiser MA, Shaffer JR, Nantermet PG, Barrow JC, Rittle KE, Collusi D, Espeseth AS, Lai MT, Pietrak BL, Holloway MK, McGaughey GB, Munshi SK, Hochman JH, Simon AJ, Selnick HG, Graham SL, Vacca JP. Stauffer SR, et al. Among authors: munshi sk. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1788-92. doi: 10.1016/j.bmcl.2006.12.051. Epub 2006 Dec 21. Bioorg Med Chem Lett. 2007. PMID: 17257835
Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Moore KP, Zhu H, Rajapakse HA, McGaughey GB, Colussi D, Price EA, Sankaranarayanan S, Simon AJ, Pudvah NT, Hochman JH, Allison T, Munshi SK, Graham SL, Vacca JP, Nantermet PG. Moore KP, et al. Among authors: munshi sk. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5831-5. doi: 10.1016/j.bmcl.2007.08.040. Epub 2007 Aug 23. Bioorg Med Chem Lett. 2007. PMID: 17827011
Discovery of aminoheterocycles as a novel beta-secretase inhibitor class: pH dependence on binding activity part 1.
Stachel SJ, Coburn CA, Rush D, Jones KL, Zhu H, Rajapakse H, Graham SL, Simon A, Katharine Holloway M, Allison TJ, Munshi SK, Espeseth AS, Zuck P, Colussi D, Wolfe A, Pietrak BL, Lai MT, Vacca JP. Stachel SJ, et al. Among authors: munshi sk. Bioorg Med Chem Lett. 2009 Jun 1;19(11):2977-80. doi: 10.1016/j.bmcl.2009.04.033. Epub 2009 Apr 18. Bioorg Med Chem Lett. 2009. PMID: 19409780
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: munshi s. 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: munshi s. J Med Chem. 2004 Dec 16;47(26):6447-50. doi: 10.1021/jm049379g. J Med Chem. 2004. PMID: 15588077
338 results