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Page 1
Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases.
Harris PA, Berger SB, Jeong JU, Nagilla R, Bandyopadhyay D, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X, Eidam PM, Finger JN, Hoffman SJ, Kang J, Kasparcova V, King BW, Lehr R, Lan Y, Leister LK, Lich JD, MacDonald TT, Miller NA, Ouellette MT, Pao CS, Rahman A, Reilly MA, Rendina AR, Rivera EJ, Schaeffer MC, Sehon CA, Singhaus RR, Sun HH, Swift BA, Totoritis RD, Vossenkämper A, Ward P, Wisnoski DD, Zhang D, Marquis RW, Gough PJ, Bertin J. Harris PA, et al. Among authors: wisnoski dd. J Med Chem. 2017 Feb 23;60(4):1247-1261. doi: 10.1021/acs.jmedchem.6b01751. Epub 2017 Feb 10. J Med Chem. 2017. PMID: 28151659
Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.
Harris PA, Faucher N, George N, Eidam PM, King BW, White GV, Anderson NA, Bandyopadhyay D, Beal AM, Beneton V, Berger SB, Campobasso N, Campos S, Capriotti CA, Cox JA, Daugan A, Donche F, Fouchet MH, Finger JN, Geddes B, Gough PJ, Grondin P, Hoffman BL, Hoffman SJ, Hutchinson SE, Jeong JU, Jigorel E, Lamoureux P, Leister LK, Lich JD, Mahajan MK, Meslamani J, Mosley JE, Nagilla R, Nassau PM, Ng SL, Ouellette MT, Pasikanti KK, Potvain F, Reilly MA, Rivera EJ, Sautet S, Schaeffer MC, Sehon CA, Sun H, Thorpe JH, Totoritis RD, Ward P, Wellaway N, Wisnoski DD, Woolven JM, Bertin J, Marquis RW. Harris PA, et al. Among authors: wisnoski dd. J Med Chem. 2019 May 23;62(10):5096-5110. doi: 10.1021/acs.jmedchem.9b00318. Epub 2019 May 2. J Med Chem. 2019. PMID: 31013427
Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity.
Charnley AK, Convery MA, Lakdawala Shah A, Jones E, Hardwicke P, Bridges A, Ouellette M, Totoritis R, Schwartz B, King BW, Wisnoski DD, Kang J, Eidam PM, Votta BJ, Gough PJ, Marquis RW, Bertin J, Casillas L. Charnley AK, et al. Among authors: wisnoski dd. Bioorg Med Chem. 2015 Nov 1;23(21):7000-6. doi: 10.1016/j.bmc.2015.09.038. Epub 2015 Sep 25. Bioorg Med Chem. 2015. PMID: 26455654
RIP3 induces apoptosis independent of pronecrotic kinase activity.
Mandal P, Berger SB, Pillay S, Moriwaki K, Huang C, Guo H, Lich JD, Finger J, Kasparcova V, Votta B, Ouellette M, King BW, Wisnoski D, Lakdawala AS, DeMartino MP, Casillas LN, Haile PA, Sehon CA, Marquis RW, Upton J, Daley-Bauer LP, Roback L, Ramia N, Dovey CM, Carette JE, Chan FK, Bertin J, Gough PJ, Mocarski ES, Kaiser WJ. Mandal P, et al. Mol Cell. 2014 Nov 20;56(4):481-95. doi: 10.1016/j.molcel.2014.10.021. Epub 2014 Nov 20. Mol Cell. 2014. PMID: 25459880 Free PMC article.
Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists.
Evans KA, Budzik BW, Ross SA, Wisnoski DD, Jin J, Rivero RA, Vimal M, Szewczyk GR, Jayawickreme C, Moncol DL, Rimele TJ, Armour SL, Weaver SP, Griffin RJ, Tadepalli SM, Jeune MR, Shearer TW, Chen ZB, Chen L, Anderson DL, Becherer JD, De Los Frailes M, Colilla FJ. Evans KA, et al. Among authors: wisnoski dd. J Med Chem. 2009 Dec 24;52(24):7962-5. doi: 10.1021/jm901434t. J Med Chem. 2009. PMID: 19902954
Discovery of GlyT1 inhibitors with improved pharmacokinetic properties.
Wolkenberg SE, Zhao Z, Wisnoski DD, Leister WH, O'Brien J, Lemaire W, Williams DL Jr, Jacobson MA, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Gibson C, Ma BK, Polsky-Fisher SL, Lindsley CW, Hartman GD. Wolkenberg SE, et al. Among authors: wisnoski dd. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1492-5. doi: 10.1016/j.bmcl.2009.01.015. Epub 2009 Jan 10. Bioorg Med Chem Lett. 2009. PMID: 19181525
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.
Lindsley CW, Wisnoski DD, Leister WH, O'brien JA, Lemaire W, Williams DL Jr, Burno M, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Duggan ME, Hartman GD, Conn PJ, Huff JR. Lindsley CW, et al. Among authors: wisnoski dd. J Med Chem. 2004 Nov 18;47(24):5825-8. doi: 10.1021/jm049400d. J Med Chem. 2004. PMID: 15537338
p38MAP kinase inhibitors. Part 1: design and development of a new class of potent and highly selective inhibitors based on 3,4-dihydropyrido[3,2-d]pyrimidone scaffold.
Natarajan SR, Wisnoski DD, Singh SB, Stelmach JE, O'Neill EA, Schwartz CD, Thompson CM, Fitzgerald CE, O'Keefe SJ, Kumar S, Hop CE, Zaller DM, Schmatz DM, Doherty JB. Natarajan SR, et al. Among authors: wisnoski dd. Bioorg Med Chem Lett. 2003 Jan 20;13(2):273-6. doi: 10.1016/s0960-894x(02)00876-4. Bioorg Med Chem Lett. 2003. PMID: 12482438
24 results