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Metabolism and excretion of (S)-6-(3-cyclopentyl-2-(4-trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid (PF-04991532), a hepatoselective glucokinase activator, in humans: confirmation of the MIST potential noted in first-in-Human metabolite scouting studies.
Sharma R, Bergman A, Litchfield J, Atkinson K, Kazierad DJ, Kalgutkar AS. Sharma R, et al. Xenobiotica. 2019 Dec;49(12):1447-1457. doi: 10.1080/00498254.2019.1581960. Epub 2019 Mar 7. Xenobiotica. 2019. PMID: 30747552 Clinical Trial.
Differences in CYP3A4 catalyzed bioactivation of 5-aminooxindole and 5-aminobenzsultam scaffolds in proline-rich tyrosine kinase 2 (PYK2) inhibitors: retrospective analysis by CYP3A4 molecular docking, quantum chemical calculations and glutathione adduct detection using linear ion trap/orbitrap mass spectrometry.
Sun H, Sharma R, Bauman J, Walker DP, Aspnes GE, Zawistoski MP, Kalgutkar AS. Sun H, et al. Among authors: sharma r. Bioorg Med Chem Lett. 2009 Jun 15;19(12):3177-82. doi: 10.1016/j.bmcl.2009.04.118. Epub 2009 May 3. Bioorg Med Chem Lett. 2009. PMID: 19433356
Pyridones as glucokinase activators: identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle.
Pfefferkorn JA, Lou J, Minich ML, Filipski KJ, He M, Zhou R, Ahmed S, Benbow J, Perez AG, Tu M, Litchfield J, Sharma R, Metzler K, Bourbonais F, Huang C, Beebe DA, Oates PJ. Pfefferkorn JA, et al. Among authors: sharma r. Bioorg Med Chem Lett. 2009 Jun 15;19(12):3247-52. doi: 10.1016/j.bmcl.2009.04.107. Epub 2009 May 3. Bioorg Med Chem Lett. 2009. PMID: 19435665
Intrinsic electrophilicity of the 4-methylsulfonyl-2-pyridone scaffold in glucokinase activators: role of glutathione-S-transferases and in vivo quantitation of a glutathione conjugate in rats.
Litchfield J, Sharma R, Atkinson K, Filipski KJ, Wright SW, Pfefferkorn JA, Tan B, Kosa RE, Stevens B, Tu M, Kalgutkar AS. Litchfield J, et al. Among authors: sharma r. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6262-7. doi: 10.1016/j.bmcl.2010.08.095. Epub 2010 Aug 21. Bioorg Med Chem Lett. 2010. PMID: 20829042
Intrinsic electrophilicity of a 4-substituted-5-cyano-6-(2-methylpyridin-3-yloxy)pyrimidine derivative: structural characterization of glutathione conjugates in vitro.
Kalgutkar AS, Mascitti V, Sharma R, Walker GW, Ryder T, McDonald TS, Chen Y, Preville C, Basak A, McClure KF, Kohrt JT, Robinson RP, Munchhof MJ, Cornelius P. Kalgutkar AS, et al. Among authors: sharma r. Chem Res Toxicol. 2011 Feb 18;24(2):269-78. doi: 10.1021/tx100429x. Epub 2011 Feb 3. Chem Res Toxicol. 2011. PMID: 21288051
Design and evaluation of a 2-(2,3,6-trifluorophenyl)acetamide derivative as an agonist of the GPR119 receptor.
Mascitti V, Stevens BD, Choi C, McClure KF, Guimarães CR, Farley KA, Munchhof MJ, Robinson RP, Futatsugi K, Lavergne SY, Lefker BA, Cornelius P, Bonin PD, Kalgutkar AS, Sharma R, Chen Y. Mascitti V, et al. Among authors: sharma r. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1306-9. doi: 10.1016/j.bmcl.2011.01.088. Epub 2011 Jan 25. Bioorg Med Chem Lett. 2011. PMID: 21310611
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