Article
Phenotypic analysis of human CYP2C9 polymorphisms using fluorine-substituted tolbutamide.
Drug discoveries & therapeutics - 8 Sept 2020
Kitamura Yuki, Saeki Ken-Ichi
Abstract excerpt
To investigate the effect of fluorine substitution on tolbutamide (TB) hydroxylation catalyzed by CYP2C9, the hydroxylation of TB and its fluorinated derivative 3'-fluoro-tolbutamide (3'-F-TB) by recombinant human CYP2C9*1, CYP2C9*2, and CYP2C9*3 was analyzed. In general, fluorine substitution near the metabolic site may decrease enzymatic oxidation owing to its electron-withdrawing nature. Fluorine substitution...
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