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Page 1
Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).
Axten JM, Medina JR, Feng Y, Shu A, Romeril SP, Grant SW, Li WH, Heerding DA, Minthorn E, Mencken T, Atkins C, Liu Q, Rabindran S, Kumar R, Hong X, Goetz A, Stanley T, Taylor JD, Sigethy SD, Tomberlin GH, Hassell AM, Kahler KM, Shewchuk LM, Gampe RT. Axten JM, et al. Among authors: shewchuk lm. J Med Chem. 2012 Aug 23;55(16):7193-207. doi: 10.1021/jm300713s. Epub 2012 Aug 8. J Med Chem. 2012. PMID: 22827572
The formation of a covalent complex between a dipeptide ligand and the src SH2 domain.
Alligood KJ, Charifson PS, Crosby R, Consler TG, Feldman PL, Gampe RT Jr, Gilmer TM, Jordan SR, Milstead MW, Mohr C, Peel MR, Rocque W, Rodriguez M, Rusnak DW, Shewchuk LM, Sternbach DD. Alligood KJ, et al. Among authors: shewchuk lm. Bioorg Med Chem Lett. 1998 May 19;8(10):1189-94. doi: 10.1016/s0960-894x(98)00195-4. Bioorg Med Chem Lett. 1998. PMID: 9871733
Prevention of chemotherapy-induced alopecia in rats by CDK inhibitors.
Davis ST, Benson BG, Bramson HN, Chapman DE, Dickerson SH, Dold KM, Eberwein DJ, Edelstein M, Frye SV, Gampe RT Jr, Griffin RJ, Harris PA, Hassell AM, Holmes WD, Hunter RN, Knick VB, Lackey K, Lovejoy B, Luzzio MJ, Murray D, Parker P, Rocque WJ, Shewchuk L, Veal JM, Walker DH, Kuyper LF. Davis ST, et al. Science. 2001 Jan 5;291(5501):134-7. doi: 10.1126/science.291.5501.134. Science. 2001. Retraction in: Science. 2002 Dec 20;298(5602):2327. doi: 10.1126/science.298.5602.2327b PMID: 11141566 Retracted.
Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis.
Bramson HN, Corona J, Davis ST, Dickerson SH, Edelstein M, Frye SV, Gampe RT Jr, Harris PA, Hassell A, Holmes WD, Hunter RN, Lackey KE, Lovejoy B, Luzzio MJ, Montana V, Rocque WJ, Rusnak D, Shewchuk L, Veal JM, Walker DH, Kuyper LF. Bramson HN, et al. J Med Chem. 2001 Dec 6;44(25):4339-58. doi: 10.1021/jm010117d. J Med Chem. 2001. PMID: 11728181
Exploration of the P1 SAR of aldehyde cathepsin K inhibitors.
Catalano JG, Deaton DN, Furfine ES, Hassell AM, McFadyen RB, Miller AB, Miller LR, Shewchuk LM, Willard DH Jr, Wright LL. Catalano JG, et al. Among authors: shewchuk lm. Bioorg Med Chem Lett. 2004 Jan 5;14(1):275-8. doi: 10.1016/j.bmcl.2003.09.088. Bioorg Med Chem Lett. 2004. PMID: 14684342
Novel and potent cyclic cyanamide-based cathepsin K inhibitors.
Deaton DN, Hassell AM, McFadyen RB, Miller AB, Miller LR, Shewchuk LM, Tavares FX, Willard DH Jr, Wright LL. Deaton DN, et al. Among authors: shewchuk lm. Bioorg Med Chem Lett. 2005 Apr 1;15(7):1815-9. doi: 10.1016/j.bmcl.2005.02.033. Bioorg Med Chem Lett. 2005. PMID: 15780613
59 results