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Page 1
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: haile pa. 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: haile pa. 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 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. 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 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: haile pa. PLoS One. 2013 Aug 1;8(8):e69619. doi: 10.1371/journal.pone.0069619. Print 2013. PLoS One. 2013. PMID: 23936340 Free PMC article.
Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inflammatory Diseases.
Haile PA, Casillas LN, Votta BJ, Wang GZ, Charnley AK, Dong X, Bury MJ, Romano JJ, Mehlmann JF, King BW, Erhard KF, Hanning CR, Lipshutz DB, Desai BM, Capriotti CA, Schaeffer MC, Berger SB, Mahajan MK, Reilly MA, Nagilla R, Rivera EJ, Sun HH, Kenna JK, Beal AM, Ouellette MT, Kelly M, Stemp G, Convery MA, Vossenkämper A, MacDonald TT, Gough PJ, Bertin J, Marquis RW. Haile PA, et al. J Med Chem. 2019 Jul 25;62(14):6482-6494. doi: 10.1021/acs.jmedchem.9b00575. Epub 2019 Jul 2. J Med Chem. 2019. PMID: 31265286
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: haile pa. 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 Pyrazolocarboxamides as Potent and Selective Receptor Interacting Protein 2 (RIP2) Kinase Inhibitors.
Haffner CD, Charnley AK, Aquino CJ, Casillas L, Convery MA, Cox JA, Elban MA, Goodwin NC, Gough PJ, Haile PA, Hughes TV, Knapp-Reed B, Kreatsoulas C, Lakdawala AS, Li H, Lian Y, Lipshutz D, Mehlmann JF, Ouellette M, Romano J, Shewchuk L, Shu A, Votta BJ, Zhou H, Bertin J, Marquis RW. Haffner CD, et al. Among authors: haile pa. ACS Med Chem Lett. 2019 Oct 11;10(11):1518-1523. doi: 10.1021/acsmedchemlett.9b00141. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 31749904 Free PMC article.
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. 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
Correction to 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, Duraiswami C, 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. ACS Med Chem Lett. 2020 Jun 2;11(6):1353. doi: 10.1021/acsmedchemlett.0c00260. eCollection 2020 Jun 11. ACS Med Chem Lett. 2020. PMID: 32551024 Free PMC article.
Optimization of a Series of RIPK2 PROTACs.
Miah AH, Smith IED, Rackham M, Mares A, Thawani AR, Nagilla R, Haile PA, Votta BJ, Gordon LJ, Watt G, Denyer J, Fisher DT, Dace P, Giffen P, Goncalves A, Churcher I, Scott-Stevens P, Harling JD. Miah AH, et al. Among authors: haile pa. J Med Chem. 2021 Sep 9;64(17):12978-13003. doi: 10.1021/acs.jmedchem.1c01118. Epub 2021 Aug 25. J Med Chem. 2021. PMID: 34432979
17 results