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Page 1
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: marquis rw. 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: marquis rw. PLoS One. 2013 Aug 1;8(8):e69619. doi: 10.1371/journal.pone.0069619. Print 2013. PLoS One. 2013. PMID: 23936340 Free PMC article.
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: marquis rw. 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.
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. Among authors: marquis rw. 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
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: marquis rw. 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
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: marquis rw. 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.
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: marquis rw. 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
The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase.
Haile PA, Votta BJ, Marquis RW, Bury MJ, Mehlmann JF, Singhaus R Jr, Charnley AK, Lakdawala AS, Convery MA, Lipshutz DB, Desai BM, Swift B, Capriotti CA, Berger SB, Mahajan MK, Reilly MA, Rivera EJ, Sun HH, Nagilla R, Beal AM, Finger JN, Cook MN, King BW, Ouellette MT, Totoritis RD, Pierdomenico M, Negroni A, Stronati L, Cucchiara S, Ziółkowski B, Vossenkämper A, MacDonald TT, Gough PJ, Bertin J, Casillas LN. Haile PA, et al. Among authors: marquis rw. J Med Chem. 2016 May 26;59(10):4867-80. doi: 10.1021/acs.jmedchem.6b00211. Epub 2016 May 4. J Med Chem. 2016. PMID: 27109867
Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel.
Haile PA, Casillas LN, Bury MJ, Mehlmann JF, Singhaus R Jr, Charnley AK, Hughes TV, DeMartino MP, Wang GZ, Romano JJ, Dong X, Plotnikov NV, Lakdawala AS, Convery MA, Votta BJ, Lipshutz DB, Desai BM, Swift B, Capriotti CA, Berger SB, Mahajan MK, Reilly MA, Rivera EJ, Sun HH, Nagilla R, LePage C, Ouellette MT, Totoritis RD, Donovan BT, Brown BS, Chaudhary KW, Gough PJ, Bertin J, Marquis RW. Haile PA, et al. Among authors: marquis rw. ACS Med Chem Lett. 2018 Sep 26;9(10):1039-1044. doi: 10.1021/acsmedchemlett.8b00344. eCollection 2018 Oct 11. ACS Med Chem Lett. 2018. PMID: 30344914 Free PMC article.
Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer.
Harris PA, Marinis JM, Lich JD, Berger SB, Chirala A, Cox JA, Eidam PM, Finger JN, Gough PJ, Jeong JU, Kang J, Kasparcova V, Leister LK, Mahajan MK, Miller G, Nagilla R, Ouellette MT, Reilly MA, Rendina AR, Rivera EJ, Sun HH, Thorpe JH, Totoritis RD, Wang W, Wu D, Zhang D, Bertin J, Marquis RW. Harris PA, et al. Among authors: marquis rw. ACS Med Chem Lett. 2019 May 9;10(6):857-862. doi: 10.1021/acsmedchemlett.9b00108. eCollection 2019 Jun 13. ACS Med Chem Lett. 2019. PMID: 31223438 Free PMC article.
45 results