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Page 1
Discovery of tertiary sulfonamides as potent liver X receptor antagonists.
Zuercher WJ, Buckholz RG, Campobasso N, Collins JL, Galardi CM, Gampe RT, Hyatt SM, Merrihew SL, Moore JT, Oplinger JA, Reid PR, Spearing PK, Stanley TB, Stewart EL, Willson TM. Zuercher WJ, et al. Among authors: gampe rt. J Med Chem. 2010 Apr 22;53(8):3412-6. doi: 10.1021/jm901797p. J Med Chem. 2010. PMID: 20345102
A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors.
Schulte CA, Deaton DN, Diaz E, Do Y, Gampe RT, Guss JH, Hancock AP, Hobbs H, Hodgson ST, Holt J, Jeune MR, Kahler KM, Kramer HF, Le J, Mortenson PN, Musetti C, Nolte RT, Orband-Miller LA, Peckham GE, Petrov KG, Pietrak BL, Poole C, Price DJ, Saxty G, Shillings A, Smalley TL Jr, Somers DO, Stewart EL, Stuart JD, Thomson SA. Schulte CA, et al. Among authors: gampe rt. Bioorg Med Chem Lett. 2021 Sep 1;47:128113. doi: 10.1016/j.bmcl.2021.128113. Epub 2021 May 13. Bioorg Med Chem Lett. 2021. PMID: 33991628
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: gampe rt. J Med Chem. 2012 Aug 23;55(16):7193-207. doi: 10.1021/jm300713s. Epub 2012 Aug 8. J Med Chem. 2012. PMID: 22827572
Structure-based design of potent retinoid X receptor alpha agonists.
Haffner CD, Lenhard JM, Miller AB, McDougald DL, Dwornik K, Ittoop OR, Gampe RT Jr, Xu HE, Blanchard S, Montana VG, Consler TG, Bledsoe RK, Ayscue A, Croom D. Haffner CD, et al. Among authors: gampe rt jr. J Med Chem. 2004 Apr 8;47(8):2010-29. doi: 10.1021/jm030565g. J Med Chem. 2004. PMID: 15056000
Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
Axten JM, Romeril SP, Shu A, Ralph J, Medina JR, Feng Y, Li WH, Grant SW, Heerding DA, Minthorn E, Mencken T, Gaul N, Goetz A, Stanley T, Hassell AM, Gampe RT, Atkins C, Kumar R. Axten JM, et al. Among authors: gampe rt. ACS Med Chem Lett. 2013 Aug 12;4(10):964-8. doi: 10.1021/ml400228e. eCollection 2013 Oct 10. ACS Med Chem Lett. 2013. PMID: 24900593 Free PMC article.
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. Among authors: gampe rt jr. J Med Chem. 2001 Dec 6;44(25):4339-58. doi: 10.1021/jm010117d. J Med Chem. 2001. PMID: 11728181
30 results