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Drug Metabolism and Pharmacokinetics, 2007 The interaction between cytochrome P450s (CYP, P450) and UDP-glucuronosyltransferases (UGTs) was studied by co-immunoprecipitation. P450 isoform-selective antibody was used as a probe to co-precipitate UGTs with the P450s from solubilized rat liver microsomes.
Peter I Mackenzie +2 more
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Inhibition of aflatoxins on UDP-glucuronosyltransferases (UGTs)
Toxicology in Vitro, 2023Aflatoxins have been recognized as the most harmful mycotoxins leading to various toxic effects. The present study aims to determine the inhibition behavior of aflatoxins on the activity of the important phase II metabolizing enzymes, UDP-glucuronosyltransferases (UGTs), based on in vitro incubation system of recombinant human UGTs-catalyzed ...
Zuo, Du, Zhen-Zhong, Liu
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Pharmacogenetics, 2003
UDP-glucuronosyltransferases (UGTs) belong to a superfamily of microsomal enzymes responsible for glucuronidation of numerous endogenous and exogenous compounds including bilirubin, hormones, various drugs as well as environmental carcinogens. Glucuronidation predominantly serves as a pathway for elimination of the different glucuronidated compounds ...
Apurva A, Desai +2 more
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UDP-glucuronosyltransferases (UGTs) belong to a superfamily of microsomal enzymes responsible for glucuronidation of numerous endogenous and exogenous compounds including bilirubin, hormones, various drugs as well as environmental carcinogens. Glucuronidation predominantly serves as a pathway for elimination of the different glucuronidated compounds ...
Apurva A, Desai +2 more
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Drug Metabolism and Disposition, 2012
We have suggested that adenine-related compounds are allosteric inhibitors of UGT in rat liver microsomes (RLM) treated with detergent. To clarify whether the same occurs with a pore-forming peptide, alamethicin, the effects of adenine-related compounds on 4-metylumbelliferone (4-MU) glucuronidation were examined using RLM and human liver microsomes ...
Yuji, Ishii +3 more
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We have suggested that adenine-related compounds are allosteric inhibitors of UGT in rat liver microsomes (RLM) treated with detergent. To clarify whether the same occurs with a pore-forming peptide, alamethicin, the effects of adenine-related compounds on 4-metylumbelliferone (4-MU) glucuronidation were examined using RLM and human liver microsomes ...
Yuji, Ishii +3 more
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Assessment of UGT Polymorphisms and Neonatal Jaundice
Seminars in Perinatology, 2011Elevation of the serum bilirubin level is a common, if not universal, finding during the first week of life. This can be a transient phenomenon that resolves spontaneously or can signify a serious or even life-threatening condition. There are many causes of hyperbilirubinemia and related therapeutic and prognostic implications.
Mark G, Bartlett, Glenn R, Gourley
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Drug Metabolism and Disposition, 2007
5-(4'-Hydroxyphenyl)-5-phenylhydantoin (4'-HPPH), a major metabolite of phenytoin in human, is exclusively metabolized to a glucuronide. 4'-HPPH has a chiral center. (S)-4'-HPPH is a predominant form produced from phenytoin in humans, and (R)-4'-HPPH is an extremely toxic form with respect to gingival hyperplasia.
Miki, Nakajima +4 more
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5-(4'-Hydroxyphenyl)-5-phenylhydantoin (4'-HPPH), a major metabolite of phenytoin in human, is exclusively metabolized to a glucuronide. 4'-HPPH has a chiral center. (S)-4'-HPPH is a predominant form produced from phenytoin in humans, and (R)-4'-HPPH is an extremely toxic form with respect to gingival hyperplasia.
Miki, Nakajima +4 more
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The inhibition of UDP-glucuronosyltransferases (UGTs) by vitamin A
Xenobiotica, 20161. The exposed level of vitamin A in plasma might be exceeded due to the both inadvertent and clinical utilization. The adverse effects of vitamin A have been frequently reported, however, the mechanism remains unclear. The inhibition of vitamin A on the activity of UDP-glucuronosyltransferases (UGTs) was determined using in vitro incubation system to ...
Xin, Liu +9 more
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Drug Metabolism and Disposition, 2008
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.
Ryoichi, Fujiwara +4 more
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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.
Ryoichi, Fujiwara +4 more
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Inhibition of UDP-glucuronosyltransferases (UGTs) by bromophenols (BPs)
Chemosphere, 2020Bromophenols (BPs) are important organic compounds which have become dominant pollutants during these years. Our present study investigated the potential inhibition behaviour of BPs on the activity of one of the most important phase II drug-metabolizing enzymes (DMEs), UDP-glucuronosyltransferases (UGTs). Recombinant UDP-glucuronosyltransferases (UGTs)-
Feige, Wang +6 more
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Enzyme Kinetics of Uridine Diphosphate Glucuronosyltransferases (UGTs)
2021Glucuronidation, catalyzed by uridine diphosphate glucuronosyltransferases (UGTs), is an important process for the metabolism and clearance of many lipophilic chemicals, including drugs, environmental chemicals, and endogenous compounds. Glucuronidation is a bisubstrate reaction that requires the aglycone and the cofactor, UDP-GlcUA.
Jin, Zhou +2 more
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