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Nomenclature update for the mammalian UDP glycosyltransferase (UGT) gene superfamily.
TLDR
The UGT nomenclature is updated to include new genes identified in the human, mouse and rat genomes and in other mammalian species to prevent confusion when the same gene is given different names.
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Specificity of substrate and inhibitor probes for human cytochromes P450 1A1 and 1A2.
TLDR
The results indicate that the majority of human CYP 1A xenobiotic inhibitor and substrate probes are nonspecific in their recognition of CYP1A1 and CYp1A2, although selectivity is apparent for some compounds.
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Cytochrome P4502C9: an enzyme of major importance in human drug metabolism.
TLDR
Consistent with the modulation of enzyme activity by genetic and other factors, wide interindividual variability occurs in the elimination and/or dosage requirements of prototypic CYP2C9 substrates.
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SELECTIVITY OF SUBSTRATE (TRIFLUOPERAZINE) AND INHIBITOR (AMITRIPTYLINE, ANDROSTERONE, CANRENOIC ACID, HECOGENIN, PHENYLBUTAZONE, QUINIDINE, QUININE, AND SULFINPYRAZONE) “PROBES” FOR HUMAN…
TLDR
TFP and hecogenin represent selective substrate and inhibitor probes for UGT1A4, although the extensive nonselective binding of the former should be taken into account in kinetic studies.
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Human udp-glucuronosyltransferases: isoform selectivity and kinetics of 4-methylumbelliferone and 1-naphthol glucuronidation, effects of organic solvents, and inhibition by diclofenac and probenecid.
TLDR
Diclofenac and probenecid inhibited all isoforms, precluding the use of these compounds for the reaction phenotyping of xenobiotic glucuronidation pathways in human tissues.
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Quantitative prediction of in vivo inhibitory interactions involving glucuronidated drugs from in vitro data: the effect of fluconazole on zidovudine glucuronidation.
TLDR
K(i) values determined under certain experimental conditions may quantitatively predict inhibition of UGT catalysed drug glucuronidation in vivo.
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The role of the CYP2C9-Leu359 allelic variant in the tolbutamide polymorphism.
TLDR
The present data suggest that the incidence of the Leu359 allelic variant of CYP2C9 may account for the occurrence of poor metabolizers of tolbutamide.
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Binding of Inhibitory Fatty Acids Is Responsible for the Enhancement of UDP-Glucuronosyltransferase 2B7 Activity by Albumin: Implications for in Vitro-in Vivo Extrapolation
TLDR
It is postulated that BSA and HSA-FAF sequester inhibitory fatty acids released during incubations, and the apparent high Km values observed for UGT2B7 substrates arise from the presence of these endogenous inhibitors.
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Genetic polymorphism of UDP-glucuronosyltransferase 2B7 (UGT2B7) at amino acid 268: ethnic diversity of alleles and potential clinical significance.
TLDR
Although the UGT2B7 polymorphism characterized here is probably not associated with altered enzyme activity, the results highlight the need to consider ethnic variability in assessing the consequences of UGT polymorphisms.
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The UDP-glucuronosyltransferases: their role in drug metabolism and detoxification.
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