Human UDP-Glucuronosyltransferase 2B7

Authors: Radominska-Pandya A.; Little J.M.; Czernik P.J.

Source: Current Drug Metabolism, Volume 2, Number 3, September 2001 , pp. 283-298(16)

Publisher: Bentham Science Publishers

Abstract:

UDP-Glucuronosyltransferases (UGTs) are glycoproteins, localized in endoplasmic reticulum (ER) and nuclear membranes, which catalyze the conjugation of a broad variety of lipophilic aglycon substrates with glucuronic acid using UDP-glucuronic acid (UDP-GlcUA) as the sugar donor. The major function of glucuronidation is to change hydrophobic compounds into hydrophilic derivatives, a process which facilitates their detoxification and excretion. However, it is also widely recognized that glucuronidation can result in compounds which are biologically active or demonstrate increased toxicity. UGTs, like other drug-metabolizing enzymes, have been postulated to be involved in controlling the steady state concentrations of nuclear receptor ligands for interactions with nuclear receptors (1,2). One of the isoforms from the UGT2B subfamily, UGT2B7, has been found to be a major human UGT2B isoform, involved in the glucuronidation of a variety of endogenous compounds and xenobiotics.

In this review, we included all available information from our studies and those of other investigators on a) the history of the identification and expression of UGT2B7 in human tissues, b) the substrate specificity of UGT2B7, c) the extrahepatic localization of UGT2B7 d) the nuclear localization of UGT2B7 and e) characterization of the UGT2B7 gene and promoter.

Keywords: Human UDP-Glucuronosyltransferase 2B7; UDP-Glucuronosyltransferases (UGTs); UGT2B isoform; UGT2B7; Polycyclic; Aromatic hydrocarbons (PAH); UGT2B7(H); UGT2B7(Y); Glu curon idation; Glucuronidation

Language: English

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1389200013338379

Publication date: 2001-09-01

• Current Drug Metabolism aims to cover all the latest and outstanding developments in drug metabolism and disposition. The journal serves as an international forum for the publication of timely reviews in drug metabolism. Current Drug Metabolism is an essential journal for academic, clinical, government and pharmaceutical scientists who wish to be kept informed and up-to-date with the latest and most important developments. The journal covers the following areas:
  
  In vitro systems including CYP-450; enzyme induction and inhibition; drug-drug interactions and enzyme kinetics; pharmacokinetics, toxicokinetics, species scaling and extrapolations; P-glycoprotein and transport carriers; target organ toxicity and interindividual variability; drug metabolism and disposition studies; extrahepatic metabolism; phase I and phase II metabolism; recent developments for the identification of drug metabolites and adducts.

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• By this author: Radominska-Pandya A. ;  Little J.M. ;  Czernik P.J.

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