Overcoming Drug Resistance through the Development of Selective Inhibitors of UDP-Glucuronosyltransferase Enzymes
نویسندگان
چکیده
منابع مشابه
Inhibition of Human UDP-Glucuronosyltransferase Enzymes by Canagliflozin and Dapagliflozin: Implications for Drug-Drug Interactions.
Canagliflozin (CNF) and dapagliflozin (DPF) are the first sodium-glucose cotransporter 2 inhibitors to be approved for clinical use. Although available evidence excludes clinically significant inhibition of cytochromes P450, the effects of CNF and DPF on human UDP-glucuronosyltransferase (UGT) enzymes are unknown. Here, we report the inhibition of human recombinant UGTs by CNF and DPF, along wi...
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this study investigated the impact of explicit instruction of morphemic analysis and synthesis on the vocabulary development of the students. the participants were 90 junior high school students divided into two experimental groups and one control group. morphological awareness techniques (analysis/synthesis) and conventional techniques were used to teach vocabulary in the experimental groups a...
15 صفحه اولEffects of ketoconazole on glucuronidation by UDP-glucuronosyltransferase enzymes.
PURPOSE Ketoconazole has been shown to inhibit the glucuronidation of the UGT2B7 substrates zidovudine and lorazepam. Its effect on UGT1A substrates is unclear. A recent study found that coadministration of irinotecan and ketoconazole led to a significant increase in the formation of SN-38 (7-ethyl-10-hydroxycamptothecine), an UGT1A substrate. This study investigates whether ketoconazole contri...
متن کاملProduct inhibition of UDP-glucuronosyltransferase (UGT) enzymes by UDP obfuscates the inhibitory effects of UGT substrates.
Substrates that are specific for certain UDP-glucuronosyltransferase (UGT) isoforms are usually used as specific inhibitors to identify UGT isoforms responsible for the glucuronidation of drugs. 1-Naphthol and 4-nitrophenol are probe substrates for human UGT1A6. In the present study, we found that UGT1A1-catalyzed estradiol 3-O-glucuronide formation and UGT1A4-catalyzed imipramine N-glucuronide...
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ژورنال
عنوان ژورنال: Journal of Molecular Biology
سال: 2019
ISSN: 0022-2836
DOI: 10.1016/j.jmb.2018.11.007