The UDP-glycosyltransferase (UGT) superfamily: new members, new functions, and novel paradigms

R Meech, DG Hu, RA McKinnon… - Physiological …, 2019 - journals.physiology.org
UDP-glycosyltransferases (UGTs) catalyze the covalent addition of sugars to a broad range
of lipophilic molecules. This biotransformation plays a critical role in elimination of a broad …

Role of bile acids and bile acid receptors in metabolic regulation

P Lefebvre, B Cariou, F Lien, F Kuipers… - Physiological …, 2009 - journals.physiology.org
The incidence of the metabolic syndrome has taken epidemic proportions in the past
decades, contributing to an increased risk of cardiovascular disease and diabetes. The …

Bile acid metabolism and signaling in cholestasis, inflammation, and cancer

T Li, U Apte - Advances in pharmacology, 2015 - Elsevier
Bile acids are synthesized from cholesterol in the liver. Some cytochrome P450 (CYP)
enzymes play key roles in bile acid synthesis. Bile acids are physiological detergent …

A comprehensive review of UDP-glucuronosyltransferase and esterases for drug development

S Oda, T Fukami, T Yokoi, M Nakajima - Drug metabolism and …, 2015 - Elsevier
UDP-glucuronosyltransferase (UGT) and esterases are recognized as the most important
non-P450 enzymes because of their high contribution to drug metabolism. UGTs catalyze …

Roles of glucuronidation and UDP-glucuronosyltransferases in xenobiotic bioactivation reactions

JK Ritter - Chemico-biological interactions, 2000 - Elsevier
Glucuronide conjugates represent one of the major types of naturally occurring phase 2
metabolites of xenobiotics and endobiotics. The process underlying their formation …

Role of nuclear receptors in the adaptive response to bile acids and cholestasis: pathogenetic and therapeutic considerations

G Zollner, HU Marschall, M Wagner… - Molecular …, 2006 - ACS Publications
Cholestasis results in intrahepatic accumulation of cytotoxic bile acids which cause liver
injury ultimately leading to biliary fibrosis and cirrhosis. Cholestatic liver damage is …

Genetic susceptibility to diclofenac-induced hepatotoxicity: contribution of UGT2B7, CYP2C8, and ABCC2 genotypes

AK Daly, GP Aithal, JBS Leathart, RA Swainsbury… - Gastroenterology, 2007 - Elsevier
Background & Aims: Diclofenac is a widely used nonsteroidal anti-inflammatory drug and is
among the most common drugs causing idiosyncratic hepatotoxicity in several recent series …

Drug bioactivation covalent binding to target proteins and toxicity relevance

S Zhou, E Chan, W Duan, M Huang… - Drug metabolism …, 2005 - Taylor & Francis
A number of therapeutic drugs with different structures and mechanisms of action have been
reported to undergo metabolic activation by Phase I or Phase II drug-metabolizing enzymes …

Mechanisms of cholestasis

G Zollner, M Trauner - Clinics in liver disease, 2008 - Elsevier
This article gives an overview of the molecular and cellular mechanisms of cholestasis.
Topics reviewed include the pathomechanisms of hereditary cholestasis syndromes, such …

[HTML][HTML] Polymorphic gene regulation and interindividual variation of UDP-glucuronosyltransferase activity in human small intestine

CP Strassburg, S Kneip, J Topp… - Journal of Biological …, 2000 - ASBMB
UDP-glucuronosyltransferases (UGTs) convert dietary constituents, drugs, and
environmental mutagens to inactive hydrophilic glucuronides. Recent studies have shown …