Evidence for Substrate-Dependent Inhibition Profiles for Human Liver Aldehyde Oxidase
نویسندگان
چکیده
منابع مشابه
Evidence for substrate-dependent inhibition profiles for human liver aldehyde oxidase.
The goal of this study was to provide a reasonable assessment of how probe substrate selection may impact the results of in vitro aldehyde oxidase (AO) inhibition experiments. Here, we used a previously studied set of seven known AO inhibitors to probe the inhibition profile of a pharmacologically relevant substrate N-[(2-dimethylamino)ethyl]acridine-4-carboxamide (DACA). DACA oxidation in huma...
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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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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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HUMAN LIVER ALDEHYDE OXIDASE (ALDEHYDE: O(2) oxidoreductase, EC 1.2.3.1) has been purified 60-fold and some of its properties studied. Like aldehyde oxidase from other mammalian species, human liver aldehyde oxidase is an enzyme with dual substrate specificity, possessing the ability to catalyze not only the oxidation of aldehydes to the corresponding carboxylic acids, but also the hydroxylatio...
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The reduction of aldehyde oxidase (EC 1.2.3.1) by the substrate W-methylnicotinamide under anaerobic conditions is a biphasic reaction. In the present work we present evidence that this behavior is due to the presence, in standard preparations, of active and inactive enzyme, the former being responsible for the fast reaction and differing from the latter by the presence of a persulfide group. I...
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ژورنال
عنوان ژورنال: Drug Metabolism and Disposition
سال: 2012
ISSN: 0090-9556,1521-009X
DOI: 10.1124/dmd.112.048546