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Page 1
Extended pharmacodynamic responses observed upon PROTAC-mediated degradation of RIPK2.
Mares A, Miah AH, Smith IED, Rackham M, Thawani AR, Cryan J, Haile PA, Votta BJ, Beal AM, Capriotti C, Reilly MA, Fisher DT, Zinn N, Bantscheff M, MacDonald TT, Vossenkamper A, Dace P, Churcher I, Benowitz AB, Watt G, Denyer J, Scott-Stevens P, Harling JD. Mares A, et al. Among authors: votta bj. Commun Biol. 2020 Mar 20;3(1):140. doi: 10.1038/s42003-020-0868-6. Commun Biol. 2020. PMID: 32198438 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: votta bj. 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
Catalytic in vivo protein knockdown by small-molecule PROTACs.
Bondeson DP, Mares A, Smith IE, Ko E, Campos S, Miah AH, Mulholland KE, Routly N, Buckley DL, Gustafson JL, Zinn N, Grandi P, Shimamura S, Bergamini G, Faelth-Savitski M, Bantscheff M, Cox C, Gordon DA, Willard RR, Flanagan JJ, Casillas LN, Votta BJ, den Besten W, Famm K, Kruidenier L, Carter PS, Harling JD, Churcher I, Crews CM. Bondeson DP, et al. Among authors: votta bj. Nat Chem Biol. 2015 Aug;11(8):611-7. doi: 10.1038/nchembio.1858. Epub 2015 Jun 10. Nat Chem Biol. 2015. PMID: 26075522 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. Among authors: votta bj. 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
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: votta bj. 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
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: votta bj. 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
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: votta bj. 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. Among authors: votta bj. 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.
Randomized clinical study of safety, pharmacokinetics, and pharmacodynamics of RIPK1 inhibitor GSK2982772 in healthy volunteers.
Weisel K, Scott NE, Tompson DJ, Votta BJ, Madhavan S, Povey K, Wolstenholme A, Simeoni M, Rudo T, Richards-Peterson L, Sahota T, Wang JG, Lich J, Finger J, Verticelli A, Reilly M, Gough PJ, Harris PA, Bertin J, Wang ML. Weisel K, et al. Among authors: votta bj. Pharmacol Res Perspect. 2017 Dec;5(6):e00365. doi: 10.1002/prp2.365. Pharmacol Res Perspect. 2017. PMID: 29226626 Free PMC article. Clinical Trial.
Preclinical evaluation of EPHX2 inhibition as a novel treatment for inflammatory bowel disease.
Reisdorf WC, Xie Q, Zeng X, Xie W, Rajpal N, Hoang B, Burgert ME, Kumar V, Hurle MR, Rajpal DK, O'Donnell S, MacDonald TT, Vossenkämper A, Wang L, Reilly M, Votta BJ, Sanchez Y, Agarwal P. Reisdorf WC, et al. Among authors: votta bj. PLoS One. 2019 Apr 19;14(4):e0215033. doi: 10.1371/journal.pone.0215033. eCollection 2019. PLoS One. 2019. PMID: 31002701 Free PMC article.
48 results