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Target intelligence / Profile preview
UDP-glucuronosyltransferase 1A1 (UGT1A1)
- Target
- UGT1A1
- Molecular classification
- Enzyme, Transferase
01
Overview
UDP-glucuronosyltransferase 1A1 (UGT1A1) is a key enzyme in the glucuronidation pathway, responsible for conjugating glucuronic acid to various lipophilic compounds, including bilirubin, drugs, hormones, and xenobiotics, to facilitate their elimination from the body. Genetic variations in UGT1A1 can lead to reduced enzyme activity and conditions like Gilbert syndrome and Crigler-Najjar syndrome. UGT1A1 activity also affects drug metabolism, influencing drug efficacy and toxicity.
- Other names
- UDP glucuronosyltransferase 1 family, polypeptide A1UDP-glucuronosyltransferase 1 family polypeptide A member 1UGT-1A1
02
Mechanism of action
Catalyzes the conjugation of glucuronic acid to lipophilic substrates, increasing their water solubility and facilitating their excretion.
03
Biological functions
GlucuronidationDetoxificationBilirubin metabolismDrug metabolismXenobiotic metabolism
04
Disease associations
Gilbert syndromeCrigler-Najjar syndromeHyperbilirubinemiaDrug toxicity
05
Safety considerations
Increased risk of irinotecan toxicity in patients with reduced UGT1A1 activityDrug-drug interactions due to altered metabolismNeonatal jaundice in individuals with UGT1A1 deficiency
06
Interacting drugs
Irinotecan
3 more in the full profile.
07
Biomarkers
UGT1A1 polymorphisms (e.g., TA repeats)Bilirubin levels
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