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Page 1
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: sehon ca. 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
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: sehon ca. 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
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. Among authors: sehon ca. 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.
CCR2 receptor antagonists: optimization of biaryl sulfonamides to increase activity in whole blood.
Wang GZ, Haile PA, Daniel T, Belot B, Viet AQ, Goodman KB, Sha D, Dowdell SE, Varga N, Hong X, Chakravorty S, Webb C, Cornejo C, Olzinski A, Bernard R, Evans C, Emmons A, Briand J, Chung CW, Quek R, Lee D, Gough PJ, Sehon CA. Wang GZ, et al. Among authors: sehon ca. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7291-4. doi: 10.1016/j.bmcl.2011.10.038. Epub 2011 Oct 19. Bioorg Med Chem Lett. 2011. PMID: 22047688
Identification of selective small molecule inhibitors of the nucleotide-binding oligomerization domain 1 (NOD1) signaling pathway.
Rickard DJ, Sehon CA, Kasparcova V, Kallal LA, Haile PA, Zeng X, Montoute MN, Poore DD, Li H, Wu Z, Eidam PM, Emery JG, Marquis RW, Gough PJ, Bertin J. Rickard DJ, et al. Among authors: sehon ca. PLoS One. 2014 May 7;9(5):e96737. doi: 10.1371/journal.pone.0096737. eCollection 2014. PLoS One. 2014. PMID: 24806487 Free PMC article.
Identification of benzimidazole diamides as selective inhibitors of the nucleotide-binding oligomerization domain 2 (NOD2) signaling pathway.
Rickard DJ, Sehon CA, Kasparcova V, Kallal LA, Zeng X, Montoute MN, Chordia T, Poore DD, Li H, Wu Z, Eidam PM, Haile PA, Yu J, Emery JG, Marquis RW, Gough PJ, Bertin J. Rickard DJ, et al. Among authors: sehon ca. PLoS One. 2013 Aug 1;8(8):e69619. doi: 10.1371/journal.pone.0069619. Print 2013. PLoS One. 2013. PMID: 23936340 Free PMC article.
Development of potent and selective small-molecule human Urotensin-II antagonists.
McAtee JJ, Dodson JW, Dowdell SE, Girard GR, Goodman KB, Hilfiker MA, Sehon CA, Sha D, Wang GZ, Wang N, Viet AQ, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Yuan CC, Douglas SA, Neeb MJ. McAtee JJ, et al. Among authors: sehon ca. Bioorg Med Chem Lett. 2008 Jun 15;18(12):3500-3. doi: 10.1016/j.bmcl.2008.05.027. Epub 2008 May 10. Bioorg Med Chem Lett. 2008. PMID: 18502123
Toll-like receptor 3-mediated necrosis via TRIF, RIP3, and MLKL.
Kaiser WJ, Sridharan H, Huang C, Mandal P, Upton JW, Gough PJ, Sehon CA, Marquis RW, Bertin J, Mocarski ES. Kaiser WJ, et al. Among authors: sehon ca. J Biol Chem. 2013 Oct 25;288(43):31268-79. doi: 10.1074/jbc.M113.462341. Epub 2013 Sep 9. J Biol Chem. 2013. PMID: 24019532 Free PMC article.
Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.
McAtee JJ, Dodson JW, Dowdell SE, Erhard K, Girard GR, Goodman KB, Hilfiker MA, Jin J, Sehon CA, Sha D, Shi D, Wang F, Wang GZ, Wang N, Wang Y, Viet AQ, Yuan CC, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Douglas SA, Neeb MJ. McAtee JJ, et al. Among authors: sehon ca. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3716-9. doi: 10.1016/j.bmcl.2008.05.058. Epub 2008 May 20. Bioorg Med Chem Lett. 2008. PMID: 18524591
Potent, selective and orally bioavailable dihydropyrimidine inhibitors of Rho kinase (ROCK1) as potential therapeutic agents for cardiovascular diseases.
Sehon CA, Wang GZ, Viet AQ, Goodman KB, Dowdell SE, Elkins PA, Semus SF, Evans C, Jolivette LJ, Kirkpatrick RB, Dul E, Khandekar SS, Yi T, Wright LL, Smith GK, Behm DJ, Bentley R, Doe CP, Hu E, Lee D. Sehon CA, et al. J Med Chem. 2008 Nov 13;51(21):6631-4. doi: 10.1021/jm8005096. Epub 2008 Oct 9. J Med Chem. 2008. PMID: 18842034
24 results