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Target intelligence / Profile preview
UDP-glucuronosyltransferase (UGT)
- Target
- UGT
- Molecular classification
- Enzyme, Glycosyltransferase
01
Overview
UDP-glucuronosyltransferases (UGTs) are a superfamily of membrane-bound enzymes that play a central role in phase II metabolism by catalyzing the glucuronidation reaction. This process involves transferring glucuronic acid from uridine 5'-diphospho-glucuronic acid (UDPGA) to various endogenous and exogenous substrates, including drugs, toxins, hormones, and metabolic byproducts. The resulting glucuronides are more polar and hydrophilic than their parent compounds, facilitating their elimination via urine or bile. UGTs detoxify lipophilic substances by making them water-soluble for excretion. Genetic polymorphisms in *UGT* genes can significantly affect drug pharmacokinetics and responses among individuals.
- Other names
- UDP glucuronosyltransferaseUDP-glucuronyltransferaseGlucuronosyltransferase
02
Mechanism of action
Catalyzes the transfer of glucuronic acid from UDPGA to a substrate, increasing its water solubility for excretion.
03
Biological functions
DetoxificationDrug metabolismHormone metabolismBilirubin metabolismPhase II metabolismGlucuronidation
04
Disease associations
HyperbilirubinemiaGilbert's syndromeDrug toxicityNeurotoxicity
05
Safety considerations
Genetic polymorphisms leading to altered drug metabolismDrug-drug interactions due to competition for UGT enzymesHyperbilirubinemia due to UGT deficienciesInterindividual variability in drug response
06
Interacting drugs
Opioids
3 more in the full profile.
07
Biomarkers
UGT1A1 variants (e.g., for irinotecan toxicity)UGT2B7 variants (e.g., for morphine metabolism)
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