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Heterodimerization of Human UDP-Glucuronosyltransferase 1A9 and UDP-Glucuronosyltransferase 2B7 Alters Their Glucuronidation Activities

Drug Metabolism and Disposition, 2023
Human UDP-glucuronosyltransferases (UGTs) play a pivotal role as prominent phase II metabolic enzymes, mediating the glucuronidation of both endobiotics and xenobiotics. Dimerization greatly modulates the enzymatic activities of UGTs. In this study, we examined the influence of three mutations (H35A, H268Y, and N68A/N315A) and four truncations (signal ...
Jia Xue   +5 more
openaire   +2 more sources

Regulation of UDP Glucuronosyltransferase Genes

Current Drug Metabolism, 2003
The UDP glucuronosyltransferase (UGT) content of cells and tissues is a major determinant of our response to those chemicals that are primarily eliminated by conjugation with glucuronic acid. There are marked interindividual differences in the content of UGTs in the liver and other organs.
Nishiyama, Takahito   +7 more
openaire   +3 more sources

UDP-Glucuronosyltransferase in gilbert’s syndrome

Pathology, 1996
The diagnosis of Gilbert's syndrome, a condition characterised by mild jaundice related to chronic unconjugated hyperbilirubinemia, is often presumptive and the pathogenesis is incompletely understood. It would be of interest to develop an immunohistochemical staining method to confirm a diagnosis of Gilbert's syndrome.
H S, Debinski   +5 more
openaire   +2 more sources

Regulation of Mammalian UDP-Glucuronosyltransferases

Current Drug Metabolism, 2018
UDP-glucuronosyltransferases (UGTs) are a class of important phase II drug metabolizing enzymes (DMEs), playing essential roles in the homeostasis of endobiotics as well as the dispositional behavior of exogenous compounds. The expression and enzyme activity of UGTs are regulated by multiple dimensions of mechanisms and can be influenced by diverse ...
Hong, Wang   +3 more
openaire   +2 more sources

UDP-Glucuronosyltransferases*

2010
United ...
Mackenzie, Peter Ian   +2 more
openaire   +2 more sources

Inhibition of aflatoxins on UDP-glucuronosyltransferases (UGTs)

Toxicology in Vitro, 2023
Aflatoxins 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
openaire   +2 more sources

The UDP-Glucuronosyltransferases as Oligomeric Enzymes

Current Drug Metabolism, 2008
The UDP-glucuronosyltransferases (UGTs) are integral membrane proteins of the endoplasmic reticulum that play important roles in the defense against potentially hazardous xenobiotics. The UGTs also participate in the metabolism and homeostasis of many endogenous compounds, including bilirubin and steroid hormones.
Moshe, Finel, Mika, Kurkela
openaire   +2 more sources

UDP-glucuronosyltransferases in human intestinal mucosa

Biochimica et Biophysica Acta (BBA) - Lipids and Lipid Metabolism, 1998
While UDP-glucuronosyltransferases (UGTs) are known to be expressed at high levels in human liver, relatively little is known about extrahepatic expression. In the present study, UGT2B family isoforms involved in the glucuronidation of steroid hormones and bile acids have been characterized in microsomes prepared from jejunum, ileum and colon from six ...
A, Radominska-Pandya   +6 more
openaire   +2 more sources

Development of Human Liver UDP-Glucuronosyltransferases

Developmental Pharmacology and Therapeutics, 1989
The development of multiple UDPGT activities towards eight substrates has been studied in fetal term and adult post-mortem (less than 5 h after death) liver samples. Most fetal and term liver activities were less than 14% of adult values, except that towards 5-hydroxytryptamine which was present in fetal and term liver at adult levels.
B, Burchell   +6 more
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Structure of UDP‐Glucuronosyltransferases in Membranes

2005
This chapter presents the most recent experimental approaches to the investigation of UDP-glucuronosyltransferase (UGTs) in membranes. The first topic described is the subcellular localization of UGTs with special emphasis on the association of these proteins with the endoplasmic reticulum (ER).
Anna, Radominska-Pandya   +3 more
openaire   +2 more sources

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