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Comparison of the circulating metabolite profile of PF-04991532, a hepatoselective glucokinase activator, across preclinical species and humans: potential implications in metabolites in safety testing assessment.
Sharma R, Litchfield J, Bergman A, Atkinson K, Kazierad D, Gustavson SM, Di L, Pfefferkorn JA, Kalgutkar AS. Sharma R, et al. Drug Metab Dispos. 2015 Feb;43(2):190-8. doi: 10.1124/dmd.114.061218. Epub 2014 Nov 10. Drug Metab Dispos. 2015. PMID: 25384899 Clinical Trial.
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.
De novo lipogenesis is essential for platelet production in humans.
Kelly KL, Reagan WJ, Sonnenberg GE, Clasquin M, Hales K, Asano S, Amor PA, Carvajal-Gonzalez S, Shirai N, Matthews MD, Li KW, Hellerstein MK, Vera NB, Ross TT, Cappon G, Bergman A, Buckeridge C, Sun Z, Qejvanaj EZ, Schmahai T, Beebe D, Pfefferkorn JA, Esler WP. Kelly KL, et al. Nat Metab. 2020 Oct;2(10):1163-1178. doi: 10.1038/s42255-020-00272-9. Epub 2020 Sep 14. Nat Metab. 2020. PMID: 32929234 Clinical Trial.
Pharmacologic inhibition of ketohexokinase prevents fructose-induced metabolic dysfunction.
Gutierrez JA, Liu W, Perez S, Xing G, Sonnenberg G, Kou K, Blatnik M, Allen R, Weng Y, Vera NB, Chidsey K, Bergman A, Somayaji V, Crowley C, Clasquin MF, Nigam A, Fulham MA, Erion DM, Ross TT, Esler WP, Magee TV, Pfefferkorn JA, Bence KK, Birnbaum MJ, Tesz GJ. Gutierrez JA, et al. Mol Metab. 2021 Jun;48:101196. doi: 10.1016/j.molmet.2021.101196. Epub 2021 Mar 3. Mol Metab. 2021. PMID: 33667726 Free PMC article. Clinical Trial.
74 results