Target intelligence / Profile preview

UDP-glucuronosyltransferase 1A8 (UGT1A8)

Target
UGT1A8
Molecular classification
Enzyme, UDP-glycosyltransferase, Membrane-bound protein
01

Overview

UDP-glucuronosyltransferase 1A8 (UGT1A8) is a membrane-bound phase II metabolic enzyme primarily expressed in extrahepatic tissues, particularly in the gastrointestinal tract[1][3][7]. It catalyzes the transfer of glucuronic acid from UDP-glucuronic acid to a variety of small lipophilic molecules—including steroids, bilirubin, hormones, phenols, flavones, anthraquinones, coumarins, drugs, and some opioids—transforming them into more polar, water-soluble metabolites for excretion in bile or urine[1][3][5][7]. UGT1A8 is part of the UGT1A subfamily produced from a complex locus with variable first exons regulating substrate specificity; its specific substrates and polymorphisms may influence the detoxification of dietary or environmental xenobiotics and impact disease risk, drug response, and toxicity[1][2][3]. Altered expression or function (due to polymorphisms or inhibitor interactions) is associated with diseases such as drug-induced toxicities, bilirubin disorders, and possibly cancer susceptibility via modulated hormone and carcinogen metabolism[2][3][5][7].

Other names
UGT1A8UDP glucuronosyltransferase family 1 member A8UDP-glucuronosyltransferase 1A8GNT1UGT1UDPGT 1-8UGT1*8UGT1-08UGT1.8UGT-1HUGT1HUDP-glucuronosyltransferase 1-8UDP-glucuronosyltransferase 1-HUDP-glucuronosyltransferase 1 family, polypeptide A8UDP glycosyltransferase 1 family, polypeptide A8
02

Mechanism of action

Catalyzes glucuronidation, enhancing drug/metabolite excretion by increasing water solubility; Involved in inactivation and detoxification of drugs and endogenous molecules

03

Biological functions

Glucuronidation (phase II metabolism)Drug metabolismSteroid hormone metabolismDetoxification of xenobioticsRegulation of endogenous and exogenous molecule solubility
04

Disease associations

CancerDisorders of drug metabolismBilirubin metabolic disorderCrigler-Najjar syndrome (as part of UGT1A family)
05

Safety considerations

Genetic polymorphisms can lead to reduced or altered enzyme activity, affecting drug efficacy or toxicityDrug interactions due to competition for glucuronidationPossible reduced clearance of drugs, leading to toxicity
06

Interacting drugs

Mycophenolate

3 more in the full profile.

07

Biomarkers

Polymorphisms in UGT1A8 may indicate altered drug metabolism capacityExpression level may serve as a potential biomarker for cancer prognosis or drug clearance efficiency

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