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11β-hydroxysteroid dehydrogenase type 1 gene knockout attenuates atherosclerosis and in vivo foam cell formation in hyperlipidemic apoE⁻/⁻ mice.
García RA, Search DJ, Lupisella JA, Ostrowski J, Guan B, Chen J, Yang WP, Truong A, He A, Zhang R, Yan M, Hellings SE, Gargalovic PS, Ryan CS, Watson LM, Langish RA, Shipkova PA, Carson NL, Taylor JR, Yang R, Psaltis GC, Harrity TW, Robl JA, Gordon DA. García RA, et al. Among authors: harrity tw. PLoS One. 2013;8(2):e53192. doi: 10.1371/journal.pone.0053192. Epub 2013 Feb 1. PLoS One. 2013. PMID: 23383297 Free PMC article.
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: harrity t. 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. 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 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: harrity t. 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
The Guinea pig as a preclinical model for demonstrating the efficacy and safety of statins.
Madsen CS, Janovitz E, Zhang R, Nguyen-Tran V, Ryan CS, Yin X, Monshizadegan H, Chang M, D'Arienzo C, Scheer S, Setters R, Search D, Chen X, Zhuang S, Kunselman L, Peters A, Harrity T, Apedo A, Huang C, Cuff CA, Kowala MC, Blanar MA, Sun CQ, Robl JA, Stein PD. Madsen CS, et al. J Pharmacol Exp Ther. 2008 Feb;324(2):576-86. doi: 10.1124/jpet.107.131615. Epub 2007 Nov 6. J Pharmacol Exp Ther. 2008. PMID: 17986646
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: harrity t. 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
(3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(methyl(1-methyl-1h-1,2,4-triazol-5-yl)amino)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic acid (BMS-644950): a rationally designed orally efficacious 3-hydroxy-3-methylglutaryl coenzyme-a reductase inhibitor with reduced myotoxicity potential.
Ahmad S, Madsen CS, Stein PD, Janovitz E, Huang C, Ngu K, Bisaha S, Kennedy LJ, Chen BC, Zhao R, Sitkoff D, Monshizadegan H, Yin X, Ryan CS, Zhang R, Giancarli M, Bird E, Chang M, Chen X, Setters R, Search D, Zhuang S, Nguyen-Tran V, Cuff CA, Harrity T, Darienzo CJ, Li T, Reeves RA, Blanar MA, Barrish JC, Zahler R, Robl JA. Ahmad S, et al. J Med Chem. 2008 May 8;51(9):2722-33. doi: 10.1021/jm800001n. Epub 2008 Apr 15. J Med Chem. 2008. PMID: 18412317
5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP.
Sulsky R, Robl JA, Biller SA, Harrity TW, Wetterau J, Connolly F, Jolibois K, Kunselman L. Sulsky R, et al. Among authors: harrity tw. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5067-70. doi: 10.1016/j.bmcl.2004.07.069. Bioorg Med Chem Lett. 2004. PMID: 15380200
An MTP inhibitor that normalizes atherogenic lipoprotein levels in WHHL rabbits.
Wetterau JR, Gregg RE, Harrity TW, Arbeeny C, Cap M, Connolly F, Chu CH, George RJ, Gordon DA, Jamil H, Jolibois KG, Kunselman LK, Lan SJ, Maccagnan TJ, Ricci B, Yan M, Young D, Chen Y, Fryszman OM, Logan JV, Musial CL, Poss MA, Robl JA, Simpkins LM, Slusarchyk WA, Sulsky R, Taunk P, Magnin DR, Tino JA, Lawrence RM, Dickson JK Jr, Biller SA. Wetterau JR, et al. Among authors: harrity tw. Science. 1998 Oct 23;282(5389):751-4. doi: 10.1126/science.282.5389.751. Science. 1998. PMID: 9784135
39 results