Target intelligence / Profile preview

UDP-glucuronosyltransferase 1A5 (UGT1A5)

Target
UGT1A5
Molecular classification
Enzyme, Glycosyltransferase, Phase II drug-metabolizing enzyme
01

Overview

UDP-glucuronosyltransferase 1A5 (UGT1A5) is an enzyme involved in the glucuronidation pathway, a critical phase II metabolic process that attaches glucuronic acid to small lipophilic molecules such as drugs, steroids, bilirubin, and hormones, to render them more water-soluble for excretion via urine or bile[1][2][4][6][7]. UGT1A5 is one of several isoforms generated from a complex locus with multiple first exons spliced to common exons, each variant conferring different substrate specificity via its unique N-terminus[1][2]. This enzyme is essential for detoxification and elimination of various xenobiotics and endogenous compounds; alterations in its activity can impact drug metabolism and susceptibility to certain metabolic disorders—such as Crigler-Najjar syndrome and hyperbilirubinemia[1][2][6][7].

Other names
UDP-glucuronosyltransferase 1A5UGT1A5UDP glucuronosyltransferase 1 family, polypeptide A5UGT1*5UGT1-05UGT1.5UGT-1EUGT1EUDPGT 1-5UDP-glucuronosyltransferase 1 family polypeptide A5
02

Mechanism of action

Catalyzes the conjugation of glucuronic acid to a wide variety of endogenous and exogenous substances, aiding in their solubilization and excretion[1][7]

03

Biological functions

Glucuronidation (drug and xenobiotic detoxification)Metabolism of steroids, bilirubin, hormones, and other small lipophilic molecules
04

Disease associations

HyperbilirubinemiaCrigler-Najjar syndrome, type IOther metabolism-related disorders
05

Safety considerations

Genetic variability could affect drug clearance, leading to altered efficacy or toxicityPotential risk for adverse drug reactions if function impaired[1][7]
06

Interacting drugs

Zolarsatan (angiotensin receptor antagonist)[1][7]

1 more in the full profile.

07

Biomarkers

Variants in UGT1A5 may inform on metabolism rate of certain drugs or risk for bilirubin-related disorders, but it is not a common clinical biomarker[1][6]

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