Kinetic and inhibitor studies of 4-methylumbelliferone and 1-naphthol glucuronidation in human liver microsomes
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A broad-spectrum substrate for the human UDP-glucuronosyltransferases and its use for investigating glucuronidation inhibitors
2021, International Journal of Biological MacromoleculesCitation Excerpt :By contrast, the approaches for assessing drug interaction potentials mediated by human UGTs are rarely reported, owing to the lack of a good substrate(s) for the entire panel of important human UGTs [32–34]. Currently, 4-methylumbelliferone (4-MU), a non-specific UGT substrate, is frequently used as the broad-spectrum substrate of human UGTs for evaluating UGT-mediated drug interaction potentials [35]. However, UGT1A4 and 2B10 do not catalyze 4-MU glucuronidation, while UGT2B4 and 2B17 catalyze this reaction at very low rates.
Application of NMR Spectroscopy in Plant Polyphenols Associated with Human Health
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2015, Applications of NMR Spectroscopy: Volume 2Glucuronidation of fenamates: Kinetic studies using human kidney cortical microsomes and recombinant UDP-glucuronosyltransferase (UGT) 1A9 and 2B7
2007, Biochemical PharmacologyCitation Excerpt :Quantitative densitometry of glucuronides was based on a UDP-[U-14C]glucuronic acid standard curve (0.6 pmol to 6 pmol) using a scanning laser PhosphorImager and associated ImageQuant software (Molecular Dynamics Inc., CA, USA). The fluorescence assay of Miners et al. [35], with modifications [32], was used for quantification of 4-MU glucuronide formation by HKCM, UGT1A9 and UGT2B7. Preliminary studies established linearity of the reaction with respect to time and protein concentration, and less than 10% substrate consumption occurred during the course of the incubation.
Functional characterization of human and cynomolgus monkey UDP-glucuronosyltransferase 1A6 enzymes
2006, Chemico-Biological InteractionsCitation Excerpt :Several genetic polymorphisms with functional changes have been reported for the UGT1A6 gene. Ciotti et al. [26] originally identified two nonsynonymous single nucleotide polymorphisms (SNPs), UGT1A6*5 (541A > G, Thr181Ala) and UGT1A6*9 (552A > C, Arg184Ser), both of which were in high (but not complete) linkage disequilibrium with each other. These variations are located in the putative endoplasmic reticulum-localization signal [31].