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214 results

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Discovery and Preclinical Pharmacology of an Oral Bromodomain and Extra-Terminal (BET) Inhibitor Using Scaffold-Hopping and Structure-Guided Drug Design.
Gavai AV, Norris D, Delucca G, Tortolani D, Tokarski JS, Dodd D, O'Malley D, Zhao Y, Quesnelle C, Gill P, Vaccaro W, Huynh T, Ahuja V, Han WC, Mussari C, Harikrishnan L, Kamau M, Poss M, Sheriff S, Yan C, Marsilio F, Menard K, Wen ML, Rampulla R, Wu DR, Li J, Zhang H, Li P, Sun D, Yip H, Traeger SC, Zhang Y, Mathur A, Zhang H, Huang C, Yang Z, Ranasinghe A, Everlof G, Raghavan N, Tye CK, Wee S, Hunt JT, Vite G, Westhouse R, Lee FY. Gavai AV, et al. Among authors: raghavan n. J Med Chem. 2021 Oct 14;64(19):14247-14265. doi: 10.1021/acs.jmedchem.1c00625. Epub 2021 Sep 20. J Med Chem. 2021. PMID: 34543572
Development of BET Inhibitors as Potential Treatments for Cancer: Optimization of Pharmacokinetic Properties.
Hill MD, Fang H, Norris D, Delucca GV, Huang H, DeBenedetto M, Quesnelle C, Schmitz WD, Tokarski JS, Sheriff S, Yan C, Fanslau C, Haarhoff Z, Huang C, Kramer M, Madari S, Menard K, Monereau L, Morrison J, Raghavan N, Shields EE, Simmermacher-Mayer J, Sinz M, Tye CK, Westhouse R, Xie C, Zhang H, Zhang L, Zvyaga T, Lee F, Gavai AV, Degnan AP. Hill MD, et al. Among authors: raghavan n. ACS Med Chem Lett. 2022 Jul 5;13(7):1165-1171. doi: 10.1021/acsmedchemlett.2c00219. eCollection 2022 Jul 14. ACS Med Chem Lett. 2022. PMID: 35859878 Free PMC article.
Cytochrome P450 11A1 bioactivation of a kinase inhibitor in rats: use of radioprofiling, modulation of metabolism, and adrenocortical cell lines to evaluate adrenal toxicity.
Zhang D, Flint O, Wang L, Gupta A, Westhouse RA, Zhao W, Raghavan N, Caceres-Cortes J, Marathe P, Shen G, Zhang Y, Allentoff A, Josephs J, Gan J, Borzilleri R, Humphreys WG. Zhang D, et al. Among authors: raghavan n. Chem Res Toxicol. 2012 Mar 19;25(3):556-71. doi: 10.1021/tx200524d. Epub 2012 Mar 2. Chem Res Toxicol. 2012. PMID: 22295996
Plasma stability-dependent circulation of acyl glucuronide metabolites in humans: how circulating metabolite profiles of muraglitazar and peliglitazar can lead to misleading risk assessment.
Zhang D, Raghavan N, Wang L, Xue Y, Obermeier M, Chen S, Tao S, Zhang H, Cheng PT, Li W, Ramanathan R, Yang Z, Humphreys WG. Zhang D, et al. Among authors: raghavan n. Drug Metab Dispos. 2011 Jan;39(1):123-31. doi: 10.1124/dmd.110.035048. Epub 2010 Sep 28. Drug Metab Dispos. 2011. PMID: 20876787
Comparative metabolism of radiolabeled muraglitazar in animals and humans by quantitative and qualitative metabolite profiling.
Zhang D, Wang L, Raghavan N, Zhang H, Li W, Cheng PT, Yao M, Zhang L, Zhu M, Bonacorsi S, Yeola S, Mitroka J, Hariharan N, Hosagrahara V, Chandrasena G, Shyu WC, Humphreys WG. Zhang D, et al. Among authors: raghavan n. Drug Metab Dispos. 2007 Jan;35(1):150-67. doi: 10.1124/dmd.106.012450. Epub 2006 Oct 24. Drug Metab Dispos. 2007. PMID: 17062777 Clinical Trial.
214 results