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Related Experiment Videos

UDP-glucuronosyltransferases.

C D King1, G R Rios, M D Green

  • 1Department of Drug Metabolism, Merck Research Laboratories, Rahway, New Jersey 07605, USA. christopher-king@merck.com

Current Drug Metabolism
|July 24, 2001
PubMed
Summary
This summary is machine-generated.

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UDP-glucuronosyltransferases (UGTs) are key enzymes for eliminating foreign and natural compounds. This review covers UGT families, their substrate specificities, and newly discovered roles in extrahepatic tissues.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Toxicology

Background:

  • Glucuronidation is a major metabolic pathway for eliminating lipophilic xenobiotics and endobiotics.
  • UDP-glucuronosyltransferases (UGTs) catalyze the transfer of a glucuronic acid moiety to various substrates.
  • Over 35 UGT gene products exist across species, divided into UGT1 and UGT2 subfamilies.

Purpose of the Study:

  • To review the two main UDP-glucuronosyltransferase (UGT) gene families.
  • To discuss the substrate specificities of different UGT isoforms.
  • To highlight recent discoveries of UGT expression in extrahepatic tissues.

Main Methods:

  • Review of existing literature on UGT gene families and functions.
  • Analysis of substrate specificities based on cultured cell experiments.

Related Experiment Videos

  • Examination of studies identifying UGT expression in extrahepatic tissues.

    • Main Results:

    • UGT1 and UGT2 subfamilies differ in gene structure and substrate specificities.
    • UGT1 isoforms metabolize substrates like bilirubin, amines, and phenols.
    • UGT2 enzymes are involved in glucuronidation of steroids, bile acids, and opioids.
    • UGT isoforms are expressed in extrahepatic tissues, including the kidney, gastrointestinal tract, and brain.

    Conclusions:

    • UGTs play a crucial role in the detoxification and elimination of a wide range of compounds.
    • Understanding UGT substrate specificities is vital for drug metabolism and toxicology.
    • The identification of UGTs in extrahepatic tissues expands our knowledge of their physiological and pathological roles.