UGT酶的遗传药理学研究进展  

Progress in the pharmacogenomics of UDP-glucuronosyltransferase

作　　者：郭栋[1] 庞良芳[1] 周宏灏[1] 

机构地区：[1]中南大学临床药理研究所,长沙410078

出　　处：《中国新药杂志》2011年第13期1188-1193,共6页Chinese Journal of New Drugs

基　　金：国家高技术研究发展计划(863计划)(2009AA022710);国家"重大新药创制"科技重大专项(2009ZX09501-032)

摘　　要：尿苷二磷酸葡萄糖醛酸基转移酶(UDP-glucuronosyltransferase,UGT),是人体内重要的催化II相结合反应的酶。UGT广泛分布于人体的肝、肾、胃肠道以及各种腺体组织,因其结构和细胞内分布的特殊性,对其研究落后于CYP450酶。近20年来随着实验技术的发展,越来越多的研究开始关注UGT。随着研究进展,UGT的底物在不断地扩展,包括有内源性激素、药物以及毒物。个体间、种族间葡萄糖醛酸化活性存在明显差异,UGT基因多态性是此现象的重要原因之一。对UGT基因多态性的研究日益增多,已经成立命名委员会。UGT按照序列相似性分两个大的亚家族,本文分别对其中主要参与药物代谢的UGT1A和UGT2家族的某些成员的遗传药理学研究进展进行综述。UDP-glucuronosyltransferase is an important enzyme involved in the phase II conjugation reaction.UGT is wildly expressed in human liver,kidney,stomach intestine tract and glandular organs.Because of the specificity of its structure and intra-cellular distribution,the study in UGT is lagged behind of the CYP450.Recent two decades,following the progress of the experiment technology,more and more research were focused on the UGT.Following these,the probe drug of UGT are enlarging,it involved in the metabolism of endogenous hormone,drugs and some kinds of toxicity.The polymorphisms of UGT gene were one of the most important reasons lead to the large inter-individual and inter-racial variability of the glucuronodiation activity.There are two subgroups,UGT1A and UGT2,depending on the similarity of the amino acid sequence.This paper reviews the current concept and new advances in the pharmacogenomics of UGT genes which have played an important role in drug metabolism.

关 键 词：尿苷二磷酸葡萄糖醛酸基转移酶 基因多态性 遗传药理学 

分 类 号：R96[医药卫生—药理学]