SPECIFICITY OF HUMAN UDP-GLUCURONOSYLTRANSFERASES AND XENOBIOTIC GLUCURONIDATION

被引：181

作者：

BURCHELL, B ^{[1
]}

BRIERLEY, CH ^{[1
]}

RANCE, D ^{[1
]}

机构：

[1] PFIZER LTD,CENT RES,DEPT DRUG METAB,SANDWICH CT13 9NJ,KENT,ENGLAND

来源：

LIFE SCIENCES | 1995年 / 57卷 / 20期

基金：

英国惠康基金;

关键词：

CDNA EXPRESSION; LATENCY; MICROSOMAL PREPARATION; ASSAY; KINETIC ANALYSIS; VALIDATION;

D O I：

10.1016/0024-3205(95)02073-R

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

Several human liver UDP-Glucuronosyltransferases (UGTs) have been cloned and the cDNAs expressed in heterologous cell lines. This technological advance has allowed the assessment of the functional substrate specificity of these UGTs. The problems which may be encountered with the latency and assay of UGTs are briefly described. The data accumulated to date indicate that the Km, and possibly the Vmax/Km, for individual substrates are the best parameters to assess the specificity of the enzymes towards xenobiotic molecules. The substrate specificity of seven UGTs has been summarised from the currently available information. Of these, UGT1*02 and UGT2B8 appear to be key isoforms in the glucuronidation of a wide range of xenobiotic substrates. Additional UGTs have yet to be identified and characterised and their future inclusion may provide further insights. Finally, the functional role of each UGT in vivo has to be determined.

引用

页码：1819 / 1831

页数：13

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