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GLUCURONIDATION AND THE UDP-GLUCURONOSYLTRANSFERASES IN HEALTH AND DISEASE

Drug Metabolism and Disposition, 2004
This article is an updated report of a symposium held at the June 2000 annual meeting of the American Society for Pharmacology and Experimental Therapeutics in Boston. The symposium was sponsored by the ASPET Divisions for Drug Metabolism and Molecular Pharmacology.
Wells, Peter G   +10 more
openaire   +4 more sources

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

STRUCTURE AND FUNCTION OF URIDINE DIPHOSPHATE GLUCURONOSYLTRANSFERASES

Clinical and Experimental Pharmacology and Physiology, 1997
SUMMARY1. The uridine diphosphate (UDP)‐glucuronosyltransferases (UGT) are a family of enzymes that catalyse the covalent addition of glucuronic acid to a wide range of lipophilic chemicals. They play a major role in the detoxification of many exogenous and endogenous compounds by generating products that are more polar and, thus, more readily excreted
Robyn Meech, Peter I. Mackenzie
openaire   +3 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 ...
Jean-Pierre Raufman   +6 more
openaire   +3 more sources

UDP glucuronosyltransferase in the cirrhotic rat liver

Journal of Gastroenterology and Hepatology, 1996
AbstractIn patients with cirrhosis, the elimination of drugs metabolized by glucuronidation is relatively preserved, in comparison with the metabolism of drugs by oxidation. This study explores this phenomenon at a molecular level. In cirrhotic rat livers the content of UDP‐glucuronosyltransferase (UGT) was examined by immunohistochemistry and ...
Thomas R. Tephly   +7 more
openaire   +3 more sources

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).
Sylvie Fournel-Gigleux   +3 more
openaire   +2 more sources

Coffee and Gastrointestinal Glucuronosyltransferases

2015
Abstract The beneficial health effects of coffee have, among other mechanisms, been linked to the activation of phase II enzymes, including UDP-glucuronosyltransferases (UGTs). UGTs catalyze the detoxification of many xenobiotic compounds, including human carcinogens and reactive oxygen species.
Christian P. Strassburg, Sandra Kalthoff
openaire   +2 more sources

Cloning and Characterization of a Canine UDP-Glucuronosyltransferase

Archives of Biochemistry and Biophysics, 2001
UDP-glucuronosyltransferases (UGTs) are a major family of enzymes catalyzing the transfer of glucuronic acid to a range of endogenous compounds and xenobiotics facilitating their elimination in either urine or bile. Although the dog is commonly used in drug metabolism studies, relatively little is known about the expression and activity of UGTs in this
D.J. Smith   +3 more
openaire   +3 more sources

Isolation and purification of UDP-glucuronosyltransferases

Chemical Research in Toxicology, 1990
UDPGTs are members of a class of enzymes located in the endoplasmic reticulum and are encoded by a multigene family. These proteins are responsible for the glucuronidation of hundreds of xenobiotics of many chemical classes and many endogenous substances such as steroid hormones, bile acids, and bilirubin.
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

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