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497 results

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Page 1
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: allison t. 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. 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
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
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: allison t. J Med Chem. 2006 Oct 19;49(21):6147-50. doi: 10.1021/jm060884i. J Med Chem. 2006. PMID: 17034118
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: allison t. 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
Fragment-based discovery of nonpeptidic BACE-1 inhibitors using tethering.
Yang W, Fucini RV, Fahr BT, Randal M, Lind KE, Lam MB, Lu W, Lu Y, Cary DR, Romanowski MJ, Colussi D, Pietrak B, Allison TJ, Munshi SK, Penny DM, Pham P, Sun J, Thomas AE, Wilkinson JM, Jacobs JW, McDowell RS, Ballinger MD. Yang W, et al. Among authors: allison tj. Biochemistry. 2009 Jun 2;48(21):4488-96. doi: 10.1021/bi900017q. Biochemistry. 2009. PMID: 19284778
Structural basis for selective small molecule kinase inhibition of activated c-Met.
Rickert KW, Patel SB, Allison TJ, Byrne NJ, Darke PL, Ford RE, Guerin DJ, Hall DL, Kornienko M, Lu J, Munshi SK, Reid JC, Shipman JM, Stanton EF, Wilson KJ, Young JR, Soisson SM, Lumb KJ. Rickert KW, et al. J Biol Chem. 2011 Apr 1;286(13):11218-25. doi: 10.1074/jbc.M110.204404. Epub 2011 Jan 18. J Biol Chem. 2011. PMID: 21247903 Free PMC article.
Genetic and pharmacological inhibition of PDK1 in cancer cells: characterization of a selective allosteric kinase inhibitor.
Nagashima K, Shumway SD, Sathyanarayanan S, Chen AH, Dolinski B, Xu Y, Keilhack H, Nguyen T, Wiznerowicz M, Li L, Lutterbach BA, Chi A, Paweletz C, Allison T, Yan Y, Munshi SK, Klippel A, Kraus M, Bobkova EV, Deshmukh S, Xu Z, Mueller U, Szewczak AA, Pan BS, Richon V, Pollock R, Blume-Jensen P, Northrup A, Andersen JN. Nagashima K, et al. Among authors: allison t. J Biol Chem. 2011 Feb 25;286(8):6433-48. doi: 10.1074/jbc.M110.156463. Epub 2010 Nov 30. J Biol Chem. 2011. PMID: 21118801 Free PMC article.
497 results