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132 results

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Page 1
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: vacca jp. Anal Biochem. 2005 Jul 1;342(1):144-51. doi: 10.1016/j.ab.2005.04.019. Anal Biochem. 2005. PMID: 15958191
Methyl-substitution of an iminohydantoin spiropiperidine β-secretase (BACE-1) inhibitor has a profound effect on its potency.
Egbertson M, McGaughey GB, Pitzenberger SM, Stauffer SR, Coburn CA, Stachel SJ, Yang W, Barrow JC, Neilson LA, McWherter M, Perlow D, Fahr B, Munshi S, Allison TJ, Holloway K, Selnick HG, Yang Z, Swestock J, Simon AJ, Sankaranarayanan S, Colussi D, Tugusheva K, Lai MT, Pietrak B, Haugabook S, Jin L, Chen IW, Holahan M, Stranieri-Michener M, Cook JJ, Vacca J, Graham SL. Egbertson M, et al. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4812-4819. doi: 10.1016/j.bmcl.2015.06.082. Epub 2015 Jun 29. Bioorg Med Chem Lett. 2015. PMID: 26195137
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: vacca jp. 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: vacca jp. 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: vacca jp. J Med Chem. 2004 Dec 16;47(26):6447-50. doi: 10.1021/jm049379g. J Med Chem. 2004. PMID: 15588077
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: vacca jp. 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: vacca jp. 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
Macrocyclic inhibitors of beta-secretase: functional activity in an animal model.
Stachel SJ, Coburn CA, Sankaranarayanan S, Price EA, Wu G, Crouthamel M, Pietrak BL, Huang Q, Lineberger J, Espeseth AS, Jin L, Ellis J, Holloway MK, Munshi S, Allison T, Hazuda D, Simon AJ, Graham SL, Vacca JP. Stachel SJ, et al. Among authors: vacca jp. J Med Chem. 2006 Oct 19;49(21):6147-50. doi: 10.1021/jm060884i. J Med Chem. 2006. PMID: 17034118
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: vacca jp. J Med Chem. 2006 Dec 14;49(25):7270-3. doi: 10.1021/jm061046r. J Med Chem. 2006. PMID: 17149856
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: vacca jp. 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
132 results