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Human UDP-glucuronosyltransferases: metabolism, expression, and disease
1Department of Chemistry & Biochemistry, Cancer Center, University of California, San Diego, La Jolla 92093, USA. rtukey@ucsd.edu
Annual Review of Pharmacology and Toxicology
|June 3, 2000
Summary
UDP-glucuronosyltransferases (UGTs) are crucial for detoxifying lipophilic compounds in vertebrates. This review explores UGTs
Area of Science:
- Biochemistry
- Pharmacology
- Genetics
Background:
- UDP-glucuronosyltransferases (UGTs) catalyze the glucuronidation of lipophilic substances in vertebrates.
- This metabolic pathway generates water-soluble metabolites from endogenous and exogenous compounds.
- The UGT superfamily comprises 15 human enzymes involved in detoxification and first-pass metabolism.
Purpose of the Study:
- To review the role of UGTs in human metabolism and disease.
- To highlight the characterization of UGT gene products and their substrates.
- To discuss the contribution of glucuronidation to epithelial first-pass metabolism.
Main Methods:
- cDNA expression experiments to characterize individual UGT gene products.
- RNA detection techniques to study UGT gene expression patterns.
- Genetic studies focusing on the UGT1A locus and bilirubin glucuronidation.
Main Results:
- Over 350 compounds identified as UGT substrates.
- Understanding of UGTs' role in liver and gastrointestinal tract metabolism.
- Identification of genetic polymorphisms in UGTs linked to Crigler-Najjar's and Gilbert's syndromes.
Conclusions:
- UGTs play a significant role in metabolizing diverse compounds.
- UGT gene expression and polymorphisms are critical in human health and disease.
- Further research into UGTs can elucidate mechanisms of drug metabolism and genetic disorders.