Substrate specificity of human hepatic Udp-glucuronosyltransferases

被引：26
作者：
Burchell, B [1 ]
Lockley, DJ
Staines, A
Uesawa, Y
Coughtrie, MWH
机构：
[1] Univ Dundee, Ninewells Hosp & Med Sch, Dept Mol & Cellular Pathol, Dundee DD1 9SY, Scotland
[2] Univ Dundee, Ninewells Hosp & Med Sch, Div Pathol & Neurosci, Dundee DD1 9SY, Scotland
来源：
PHASE II CONJUGATION ENZYMES AND TRANSPORT SYSTEMS | 2005年 / 400卷
基金：
英国惠康基金;
关键词：
D O I：
10.1016/S0076-6879(05)00003-0
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
Five human hepatic UDP-glucuronosyltransferases (UGTs) catalyze the facilitated excretion of more than 90% of drugs eliminated by glucuronidation. The substrate specificity of these UGTs has been examined using cloned expressed enzymes and liquid chromatography-mass spectrometry assays to determine the intrinsic clearance of drug glucuronidation in vitro. Specific substrates for the five individual UGTs have been identified. These five probe substrates could be used to predict the drug clearance catalyzed by individual UGTs in vivo.
引用
收藏
页码：46 / +
页数：13
相关论文
共 36 条
  • [1] THE GENETIC-BASIS OF THE REDUCED EXPRESSION OF BILIRUBIN UDP-GLUCURONOSYLTRANSFERASE-1 IN GILBERTS-SYNDROME
    BOSMA, PJ
    CHOWDHURY, JR
    BAKKER, C
    GANTLA, S
    DEBOER, A
    OOSTRA, BA
    LINDHOUT, D
    TYTGAT, GNJ
    JANSEN, PLM
    ELFERINK, RPJO
    CHOWDHURY, NR
    [J]. NEW ENGLAND JOURNAL OF MEDICINE, 1995, 333 (18) : 1171 - 1175
  • [2] Drug-mediated toxicity caused by genetic deficiency of UDP-glucuronosyltransferases
    Burchell, B
    Soars, M
    Monaghan, G
    Cassidy, A
    Smith, D
    Ethell, B
    [J]. TOXICOLOGY LETTERS, 2000, 112 : 333 - 340
  • [3] STUDIES ON PURIFICATION OF RAT-LIVER URIDINE-DIPHOSPHATE GLUCURONYLTRANSFERASE
    BURCHELL, B
    [J]. BIOCHEMICAL JOURNAL, 1977, 161 (03) : 543 - +
  • [4] BURCHELL B, 1997, COMPREHENSIVE TOXICO
  • [5] Burchell Brian, 2003, Am J Pharmacogenomics, V3, P37, DOI 10.2165/00129785-200303010-00006
  • [6] COUGHTRIE MWH, 1991, CLIN CHEM, V37, P739
  • [7] PURIFICATION AND PROPERTIES OF RAT-KIDNEY UDPGLUCURONOSYLTRANSFERASE
    COUGHTRIE, MWH
    BURCHELL, B
    BEND, JR
    [J]. BIOCHEMICAL PHARMACOLOGY, 1987, 36 (02) : 245 - 251
  • [8] COURT MH, 2005, METHODS ENZYMOL, V400
  • [9] A Gilbert's syndrome UGT1A1 variant confers susceptibility to tranilast-induced hyperbilirubinemia
    Danoff, TM
    Campbell, DA
    McCarthy, LC
    Lewis, KF
    Repasch, MH
    Saunders, AM
    Spurr, NK
    Purvis, IJ
    Roses, AD
    Xu, CF
    [J]. PHARMACOGENOMICS JOURNAL, 2004, 4 (01) : 49 - 53
  • [10] DUTON GJ, 1980, GLUCURONIDATION DRUG
1234