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Page 1
An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure.
Thorneloe KS, Cheung M, Bao W, Alsaid H, Lenhard S, Jian MY, Costell M, Maniscalco-Hauk K, Krawiec JA, Olzinski A, Gordon E, Lozinskaya I, Elefante L, Qin P, Matasic DS, James C, Tunstead J, Donovan B, Kallal L, Waszkiewicz A, Vaidya K, Davenport EA, Larkin J, Burgert M, Casillas LN, Marquis RW, Ye G, Eidam HS, Goodman KB, Toomey JR, Roethke TJ, Jucker BM, Schnackenberg CG, Townsley MI, Lepore JJ, Willette RN. Thorneloe KS, et al. Among authors: casillas ln. Sci Transl Med. 2012 Nov 7;4(159):159ra148. doi: 10.1126/scitranslmed.3004276. Sci Transl Med. 2012. PMID: 23136043
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: casillas ln. 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
N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I.
Thorneloe KS, Sulpizio AC, Lin Z, Figueroa DJ, Clouse AK, McCafferty GP, Chendrimada TP, Lashinger ES, Gordon E, Evans L, Misajet BA, Demarini DJ, Nation JH, Casillas LN, Marquis RW, Votta BJ, Sheardown SA, Xu X, Brooks DP, Laping NJ, Westfall TD. Thorneloe KS, et al. Among authors: casillas ln. J Pharmacol Exp Ther. 2008 Aug;326(2):432-42. doi: 10.1124/jpet.108.139295. Epub 2008 May 22. J Pharmacol Exp Ther. 2008. PMID: 18499743
Understanding Pharmacokinetic Disconnect in Preclinical Species for 4-Aminoquinolines: Consequences of Low Permeability and High P-glycoprotein Efflux Ratio on Rat and Dog Oral Pharmacokinetics.
Mahajan MK, Rivera EJ, Sun HH, Nagilla R, DeMartino MP, Haile PA, Casillas LN, Marquis RW, Votta BJ, Bertin J, Reilly MA. Mahajan MK, et al. Among authors: casillas ln. J Pharm Sci. 2020 Oct;109(10):3160-3171. doi: 10.1016/j.xphs.2020.06.013. Epub 2020 Jun 18. J Pharm Sci. 2020. PMID: 32565354
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. 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
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: casillas ln. 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.
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: casillas ln. 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.
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. 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.
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: casillas ln. 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
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: casillas ln. 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
17 results