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67 results

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Page 1
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
Henne KR, Tran TB, VandenBrink BM, Rock DA, Aidasani DK, Subramanian R, Mason AK, Stresser DM, Teffera Y, Wong SG, Johnson MG, Chen X, Tonn GR, Wong BK. Henne KR, et al. Among authors: wong bk, wong sg. Drug Metab Dispos. 2012 Jul;40(7):1429-40. doi: 10.1124/dmd.112.045708. Epub 2012 Apr 19. Drug Metab Dispos. 2012. PMID: 22517972
An inhibitory metabolite leads to dose- and time-dependent pharmacokinetics of (R)-N-{1-[3-(4-ethoxy-phenyl)-4-oxo-3,4-dihydro-pyrido[2,3-d]pyrimidin-2-yl]-ethyl}-N-pyridin-3-yl-methyl-2-(4-trifluoromethoxy-phenyl)-acetamide (AMG 487) in human subjects after multiple dosing.
Tonn GR, Wong SG, Wong SC, Johnson MG, Ma J, Cho R, Floren LC, Kersey K, Berry K, Marcus AP, Wang X, Van Lengerich B, Medina JC, Pearson PG, Wong BK. Tonn GR, et al. Among authors: wong sc, wong bk, wong sg. Drug Metab Dispos. 2009 Mar;37(3):502-13. doi: 10.1124/dmd.108.021931. Epub 2008 Dec 16. Drug Metab Dispos. 2009. PMID: 19088267 Clinical Trial.
Bioactivation of a novel 2-methylindole-containing dual chemoattractant receptor-homologous molecule expressed on T-helper type-2 cells/D-prostanoid receptor antagonist leads to mechanism-based CYP3A inactivation: glutathione adduct characterization and prediction of in vivo drug-drug interaction.
Wong SG, Fan PW, Subramanian R, Tonn GR, Henne KR, Johnson MG, Tadano Lohr M, Wong BK. Wong SG, et al. Among authors: wong bk. Drug Metab Dispos. 2010 May;38(5):841-50. doi: 10.1124/dmd.109.031344. Epub 2010 Jan 25. Drug Metab Dispos. 2010. PMID: 20100816
Solving time-dependent CYP3A4 inhibition for a series of indole-phenylacetic acid dual antagonists of the PGD(2) receptors CRTH2 and DP.
Johnson MG, Liu JJ, Li AR, van Lengerich B, Wang S, Medina JC, Collins TL, Danao J, Seitz L, Willee A, D'Souza W, Budelsky AL, Fan PW, Wong SG. Johnson MG, et al. Among authors: wong sg. Bioorg Med Chem Lett. 2014 Jul 1;24(13):2877-80. doi: 10.1016/j.bmcl.2014.04.092. Epub 2014 May 4. Bioorg Med Chem Lett. 2014. PMID: 24825301
Synthesis and SAR study of potent and selective PI3Kδ inhibitors.
Bui M, Hao X, Shin Y, Cardozo M, He X, Henne K, Suchomel J, McCarter J, McGee LR, San Miguel T, Medina JC, Mohn D, Tran T, Wannberg S, Wong J, Wong S, Zalameda L, Metz D, Cushing TD. Bui M, et al. Bioorg Med Chem Lett. 2015 Mar 1;25(5):1104-9. doi: 10.1016/j.bmcl.2015.01.001. Epub 2015 Jan 17. Bioorg Med Chem Lett. 2015. PMID: 25666823
Discovery of the imidazole-derived GPR40 agonist AM-3189.
Ma Z, Lin DC, Sharma R, Liu J, Zhu L, Li AR, Kohn T, Wang Y, Liu JJ, Bartberger MD, Medina JC, Zhuang R, Li F, Zhang J, Luo J, Wong S, Tonn GR, Houze JB. Ma Z, et al. Bioorg Med Chem Lett. 2016 Jan 1;26(1):15-20. doi: 10.1016/j.bmcl.2015.11.050. Epub 2015 Nov 17. Bioorg Med Chem Lett. 2016. PMID: 26620255
Optimization of GPR40 Agonists for Type 2 Diabetes.
Liu JJ, Wang Y, Ma Z, Schmitt M, Zhu L, Brown SP, Dransfield PJ, Sun Y, Sharma R, Guo Q, Zhuang R, Zhang J, Luo J, Tonn GR, Wong S, Swaminath G, Medina JC, Lin DC, Houze JB. Liu JJ, et al. ACS Med Chem Lett. 2014 Feb 6;5(5):517-21. doi: 10.1021/ml400501x. eCollection 2014 May 8. ACS Med Chem Lett. 2014. PMID: 24900872 Free PMC article.
67 results