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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: gough pj. 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
In vivo activity of an azole series of CCR2 antagonists.
Smethurst CA, Bevan N, Brooks C, Emmons A, Gough PJ, Mookherjee C, Moores K, Peace S, Philp J, Piercy V, Watson SP, Zippoli M. Smethurst CA, et al. Among authors: gough pj. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7252-5. doi: 10.1016/j.bmcl.2012.09.020. Epub 2012 Sep 23. Bioorg Med Chem Lett. 2012. PMID: 23079519
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: gough pj. PLoS One. 2014 May 7;9(5):e96737. doi: 10.1371/journal.pone.0096737. eCollection 2014. PLoS One. 2014. PMID: 24806487 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. Among authors: gough pj. 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
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: gough pj. 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: gough pj. PLoS One. 2013 Aug 1;8(8):e69619. doi: 10.1371/journal.pone.0069619. Print 2013. PLoS One. 2013. PMID: 23936340 Free PMC article.
Pharmacological inhibition of C-C chemokine receptor 2 decreases macrophage infiltration in the aortic root of the human C-C chemokine receptor 2/apolipoprotein E-/- mouse: magnetic resonance imaging assessment.
Olzinski AR, Turner GH, Bernard RE, Karr H, Cornejo CA, Aravindhan K, Hoang B, Ringenberg MA, Qin P, Goodman KB, Willette RN, Macphee CH, Jucker BM, Sehon CA, Gough PJ. Olzinski AR, et al. Among authors: gough pj. Arterioscler Thromb Vasc Biol. 2010 Feb;30(2):253-9. doi: 10.1161/ATVBAHA.109.198812. Epub 2009 Dec 3. Arterioscler Thromb Vasc Biol. 2010. PMID: 19965779
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: gough pj. 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 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: gough pj. 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 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: gough pj. 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.
107 results