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化学进展 2009, Vol. 21 Issue (05): 911-918 前一篇   后一篇

• 金属药物专辑 •

人肝细胞色素P450 2C金属酶与药物代谢*

蒋华麟; 谭相石**   

  1. （复旦大学化学系  生物医学研究院   上海 200433）
  • 收稿日期:2008-10-27 修回日期:2009-01-27 出版日期:2009-05-24 发布日期:2009-05-05
  • 通讯作者: 谭相石 E-mail:xstan@fudan.edu.cn
  • 基金资助:

    国家自然科学基金

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Human Hepatic Cytochrome P450 2C Metalloenzymes and Drug Metabolism

Jiang Hualin; Tan Xiangshi**   

  1. (Department of Chemistry, Institutes of Biomedical Sciences, Fudan University, Shanghai 200433, China)
  • Received:2008-10-27 Revised:2009-01-27 Online:2009-05-24 Published:2009-05-05
  • Contact: Tan Xiangshi E-mail:xstan@fudan.edu.cn

由于人肝细胞色素P450 2C亚家族与临床药物代谢的密切关系，其研究已引起人们的广泛关注。本文综述了四种人肝细胞色素P450 2C，着重综述了其中的三种：CYP2C9，CYP2C8，CYP2C19的研究进展。评述了CYP2C9，CYP2C8和CYP2C19的某些氨基酸残基在催化过程中的作用，这三种酶的基因多态在不同人种中的分布及药物代谢的差异，以及它们与用药的特异性及某些疾病的易感性的联系，介绍了目前提出的CYP2C8的底物药效团模型，最后总结了CYP2C9，CYP2C8，CYP2C19，CYP2C18的主要特性。

关键词： 细胞色素P450, 金属酶, 基因多态性, 用药特异性

Because of their close relationship to metabolism of clinically prescribed drugs, human hepatic cytochrome P450 2C subfamily have been paid wide attention. Research progress of four human hepatic cytochrome P450 2Cs are reviewed in this paper. Three of them, CYP2C9, CYP2C8, CYP2C19, are especially focused on. The function of some of their amino acid residues, distribution in various ethnic groups and difference in metabolizing drugs of their polymorphisms, and their relationship with drug specificity and some diseases susceptibility are reviewed. A pharmacophore model of CYP2C8 substrate is introduced, and main characteristics of CYP2C9, CYP2C8, CYP2C19, CYP2C18 are summarized.

Contents
1 Introduction
2 CYP2C9
3 CYP2C8
4 CYP2C19
5 Epilogue

Key words: cytochromes P450, metalloenzyme, gene polymorphisms, drug usage individuation

中图分类号: 

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