Inhibition of Human Liver Aldehyde Oxidase: Implications for Potential Drug-Drug Interactions
نویسندگان
چکیده
منابع مشابه
Inhibition of human liver aldehyde oxidase: implications for potential drug-drug interactions.
During the course of our research efforts to understand the kinetics of human aldehyde oxidase as a xenobiotic-clearing enzyme, we investigated the effect of eight different inhibitors on the oxidation of the probe substrate phthalazine. Saturation kinetic parameters for phthalazine oxidation in human liver cytosol were found to be the following: K(m) = 8.0 ± 0.4 μM and V(max) = 4.3 ± 0.1 nmol ...
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The selective estrogen receptor modulator, raloxifene, has been demonstrated as a potent uncompetitive inhibitor of human liver aldehyde oxidase-catalyzed oxidation of phthalazine, vanillin, and nicotine-Delta1'(5')-iminium ion, with K(i) values of 0.87 to 1.4 nM. Inhibition was not time-dependent. Raloxifene has also been shown to be a noncompetitive inhibitor of an aldehyde oxidase-catalyzed ...
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ژورنال
عنوان ژورنال: Drug Metabolism and Disposition
سال: 2011
ISSN: 0090-9556,1521-009X
DOI: 10.1124/dmd.111.041806