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Page 1
DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors.
Harris PA, King BW, Bandyopadhyay D, Berger SB, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X, Finger JN, Grady LC, Hoffman SJ, Jeong JU, Kang J, Kasparcova V, Lakdawala AS, Lehr R, McNulty DE, Nagilla R, Ouellette MT, Pao CS, Rendina AR, Schaeffer MC, Summerfield JD, Swift BA, Totoritis RD, Ward P, Zhang A, Zhang D, Marquis RW, Bertin J, Gough PJ. Harris PA, et al. Among authors: hoffman sj. J Med Chem. 2016 Mar 10;59(5):2163-78. doi: 10.1021/acs.jmedchem.5b01898. Epub 2016 Feb 23. J Med Chem. 2016. PMID: 26854747
High throughput screening identifies ATP-competitive inhibitors of the NLRP1 inflammasome.
Harris PA, Duraiswami C, Fisher DT, Fornwald J, Hoffman SJ, Hofmann G, Jiang M, Lehr R, McCormick PM, Nickels L, Schwartz B, Wu Z, Zhang G, Marquis RW, Bertin J, Gough PJ. Harris PA, et al. Bioorg Med Chem Lett. 2015 Jul 15;25(14):2739-43. doi: 10.1016/j.bmcl.2015.05.032. Epub 2015 May 19. Bioorg Med Chem Lett. 2015. PMID: 26022841
Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis.
Harris PA, Bandyopadhyay D, Berger SB, Campobasso N, Capriotti CA, Cox JA, Dare L, Finger JN, Hoffman SJ, Kahler KM, Lehr R, Lich JD, Nagilla R, Nolte RT, Ouellette MT, Pao CS, Schaeffer MC, Smallwood A, Sun HH, Swift BA, Totoritis RD, Ward P, Marquis RW, Bertin J, Gough PJ. Harris PA, et al. Among authors: hoffman sj. ACS Med Chem Lett. 2013 Nov 4;4(12):1238-43. doi: 10.1021/ml400382p. eCollection 2013 Dec 12. ACS Med Chem Lett. 2013. PMID: 24900635 Free PMC article.
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: hoffman bl, hoffman sj. 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: hoffman sj. 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
Systemic activation of the transient receptor potential vanilloid subtype 4 channel causes endothelial failure and circulatory collapse: Part 2.
Willette RN, Bao W, Nerurkar S, Yue TL, Doe CP, Stankus G, Turner GH, Ju H, Thomas H, Fishman CE, Sulpizio A, Behm DJ, Hoffman S, Lin Z, Lozinskaya I, Casillas LN, Lin M, Trout RE, Votta BJ, Thorneloe K, Lashinger ES, Figueroa DJ, Marquis R, Xu X. Willette RN, et al. Among authors: hoffman s. J Pharmacol Exp Ther. 2008 Aug;326(2):443-52. doi: 10.1124/jpet.107.134551. Epub 2008 May 22. J Pharmacol Exp Ther. 2008. PMID: 18499744
Characterization of GSK'963: a structurally distinct, potent and selective inhibitor of RIP1 kinase.
Berger SB, Harris P, Nagilla R, Kasparcova V, Hoffman S, Swift B, Dare L, Schaeffer M, Capriotti C, Ouellette M, King BW, Wisnoski D, Cox J, Reilly M, Marquis RW, Bertin J, Gough PJ. Berger SB, et al. Among authors: hoffman s. Cell Death Discov. 2015 Jul 27;1:15009. doi: 10.1038/cddiscovery.2015.9. eCollection 2015. Cell Death Discov. 2015. PMID: 27551444 Free PMC article.
Cutting Edge: RIP1 kinase activity is dispensable for normal development but is a key regulator of inflammation in SHARPIN-deficient mice.
Berger SB, Kasparcova V, Hoffman S, Swift B, Dare L, Schaeffer M, Capriotti C, Cook M, Finger J, Hughes-Earle A, Harris PA, Kaiser WJ, Mocarski ES, Bertin J, Gough PJ. Berger SB, et al. Among authors: hoffman s. J Immunol. 2014 Jun 15;192(12):5476-80. doi: 10.4049/jimmunol.1400499. Epub 2014 May 12. J Immunol. 2014. PMID: 24821972 Free PMC article.
MALT1 Protease Activity Is Required for Innate and Adaptive Immune Responses.
Yu JW, Hoffman S, Beal AM, Dykon A, Ringenberg MA, Hughes AC, Dare L, Anderson AD, Finger J, Kasparcova V, Rickard D, Berger SB, Ramanjulu J, Emery JG, Gough PJ, Bertin J, Foley KP. Yu JW, et al. Among authors: hoffman s. PLoS One. 2015 May 12;10(5):e0127083. doi: 10.1371/journal.pone.0127083. eCollection 2015. PLoS One. 2015. PMID: 25965667 Free PMC article.
1,936 results