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Page 1
Discovery of 3-hydroxy-4-cyano-isoquinolines as novel, potent, and selective inhibitors of human 11β-hydroxydehydrogenase 1 (11β-HSD1).
Wu SC, Yoon D, Chin J, van Kirk K, Seethala R, Golla R, He B, Harrity T, Kunselman LK, Morgan NN, Ponticiello RP, Taylor JR, Zebo R, Harper TW, Li W, Wang M, Zhang L, Sleczka BG, Nayeem A, Sheriff S, Camac DM, Morin PE, Everlof JG, Li YX, Ferraro CA, Kieltyka K, Shou W, Vath MB, Zvyaga TA, Gordon DA, Robl JA. Wu SC, et al. Among authors: zebo r. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6693-8. doi: 10.1016/j.bmcl.2011.09.058. Epub 2011 Sep 21. Bioorg Med Chem Lett. 2011. PMID: 21983444
Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.
Wang W, Devasthale P, Farrelly D, Gu L, Harrity T, Cap M, Chu C, Kunselman L, Morgan N, Ponticiello R, Zebo R, Zhang L, Locke K, Lippy J, O'Malley K, Hosagrahara V, Zhang L, Kadiyala P, Chang C, Muckelbauer J, Doweyko AM, Zahler R, Ryono D, Hariharan N, Cheng PT. Wang W, et al. Among authors: zebo r. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1939-44. doi: 10.1016/j.bmcl.2008.01.126. Epub 2008 Feb 7. Bioorg Med Chem Lett. 2008. PMID: 18291645
Discovery of Clinical Candidate 2-((2S,6S)-2-Phenyl-6-hydroxyadamantan-2-yl)-1-(3'-hydroxyazetidin-1-yl)ethanone [BMS-816336], an Orally Active Novel Selective 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor.
Ye XY, Chen SY, Wu S, Yoon DS, Wang H, Hong Z, O'Connor SP, Li J, Li JJ, Kennedy LJ, Walker SJ, Nayeem A, Sheriff S, Camac DM, Ramamurthy V, Morin PE, Zebo R, Taylor JR, Morgan NN, Ponticiello RP, Harrity T, Apedo A, Golla R, Seethala R, Wang M, Harper TW, Sleczka BG, He B, Kirby M, Leahy DK, Li J, Hanson RL, Guo Z, Li YX, DiMarco JD, Scaringe R, Maxwell B, Moulin F, Barrish JC, Gordon DA, Robl JA. Ye XY, et al. Among authors: zebo r. J Med Chem. 2017 Jun 22;60(12):4932-4948. doi: 10.1021/acs.jmedchem.7b00211. Epub 2017 Jun 5. J Med Chem. 2017. PMID: 28537398
Discovery of Clinical Candidate BMS-823778 as an Inhibitor of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1).
Li J, Kennedy LJ, Walker SJ, Wang H, Li JJ, Hong Z, O'Connor SP, Ye XY, Chen S, Wu S, Yoon DS, Nayeem A, Camac DM, Ramamurthy V, Morin PE, Sheriff S, Wang M, Harper TW, Golla R, Seethala R, Harrity T, Ponticiello RP, Morgan NN, Taylor JR, Zebo R, Maxwell B, Moulin F, Gordon DA, Robl JA. Li J, et al. Among authors: zebo r. ACS Med Chem Lett. 2018 Nov 13;9(12):1170-1174. doi: 10.1021/acsmedchemlett.8b00307. eCollection 2018 Dec 13. ACS Med Chem Lett. 2018. PMID: 30613321 Free PMC article.
Optimization of 1,2,4-Triazolopyridines as Inhibitors of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1).
Li J, Kennedy LJ, Wang H, Li JJ, Walker SJ, Hong Z, O'Connor SP, Nayeem A, Camac DM, Morin PE, Sheriff S, Wang M, Harper T, Golla R, Seethala R, Harrity T, Ponticiello RP, Morgan NN, Taylor JR, Zebo R, Gordon DA, Robl JA. Li J, et al. Among authors: zebo r. ACS Med Chem Lett. 2014 May 22;5(7):803-8. doi: 10.1021/ml500144h. eCollection 2014 Jul 10. ACS Med Chem Lett. 2014. PMID: 25050169 Free PMC article.
Discovery of 5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one (BMS-903452), an antidiabetic clinical candidate targeting GPR119.
Wacker DA, Wang Y, Broekema M, Rossi K, O'Connor S, Hong Z, Wu G, Malmstrom SE, Hung CP, LaMarre L, Chimalakonda A, Zhang L, Xin L, Cai H, Chu C, Boehm S, Zalaznick J, Ponticiello R, Sereda L, Han SP, Zebo R, Zinker B, Luk CE, Wong R, Everlof G, Li YX, Wu CK, Lee M, Griffen S, Miller KJ, Krupinski J, Robl JA. Wacker DA, et al. Among authors: zebo r. J Med Chem. 2014 Sep 25;57(18):7499-508. doi: 10.1021/jm501175v. Epub 2014 Sep 10. J Med Chem. 2014. PMID: 25208139
Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)-1H-pyrazol-1-yl)methyl)phosphonate (BMS-820132).
Shi Y, Wang Y, Meng W, Brigance RP, Ryono DE, Bolton S, Zhang H, Chen S, Smirk R, Tao S, Tino JA, Williams KN, Sulsky R, Nielsen L, Ellsworth B, Wong MKY, Sun JH, Leith LW, Sun D, Wu DR, Gupta A, Rampulla R, Mathur A, Chen BC, Wang A, Fuentes-Catanio HG, Kunselman L, Cap M, Zalaznick J, Ma X, Liu H, Taylor JR, Zebo R, Jones B, Kalinowski S, Swartz J, Staal A, O'Malley K, Kopcho L, Muckelbauer JK, Krystek SR Jr, Spronk SA, Marcinkeviciene J, Everlof G, Chen XQ, Xu C, Li YX, Langish RA, Yang Y, Wang Q, Behnia K, Fura A, Janovitz EB, Pannacciulli N, Griffen S, Zinker BA, Krupinski J, Kirby M, Whaley J, Zahler R, Barrish JC, Robl JA, Cheng PTW. Shi Y, et al. Among authors: zebo r. J Med Chem. 2022 Mar 10;65(5):4291-4317. doi: 10.1021/acs.jmedchem.1c02110. Epub 2022 Feb 18. J Med Chem. 2022. PMID: 35179904
The dual peroxisome proliferator-activated receptor alpha/gamma activator muraglitazar prevents the natural progression of diabetes in db/db mice.
Tozzo E, Ponticiello R, Swartz J, Farrelly D, Zebo R, Welzel G, Egan D, Kunselman L, Peters A, Gu L, French M, Chen S, Devasthale P, Janovitz E, Staal A, Harrity T, Belder R, Cheng PT, Whaley J, Taylor S, Hariharan N. Tozzo E, et al. Among authors: zebo r. J Pharmacol Exp Ther. 2007 Apr;321(1):107-15. doi: 10.1124/jpet.106.115337. Epub 2007 Jan 26. J Pharmacol Exp Ther. 2007. PMID: 17259449