CYP450氧化还原酶的药物基因组学研究进展

摘要/Abstract

摘要： 细胞色素P450氧化酶 (cytochrome P450 enzymes,CYP)的氧化还原反应是人体内重要的生理生化反应,参与许多内、外源化合物的代谢和激素类化合物的合成。CYP450氧化还原酶 (cytochrome P450 oxidoreductase, POR) 是所有肝微粒体内CYP酶的唯一电子供体。POR不仅可作为电子供体参与由CYP介导的药物代谢,而且可通过1-电子还原反应直接介导一些抗肿瘤前体药物的代谢和转化。可见,POR在药物代谢过程中发挥着极其重要的作用。众多研究证实,编码人POR的基因具有遗传多态性,对临床药物代谢乃至疗效有着显著影响,具有重要的临床意义。下面对近年来POR的药物基因组学最新研究进展作一综述。

关键词: CYP450氧化还原酶, 药物基因组学, 细胞色素P450氧化酶, 电子供体, 基因多态性, 药物代谢

Abstract: The redox reaction of the cytochrome P450 enzymes (CYP) are important physiological and biochemical reactions in the human body, involved in the metabolism of endogenous and exogenous compounds and steroids synthesis. POR (cytochrome P450 oxidoreductase) is the only electron donor for all the hepatic microsomal CYP enzymes. Not only acts as an electron donor involved in drug metabolism mediated by CYP enzymes, POR also directly induces the transformation and metabolism of some anti-tumor precursors. Therefore POR plays an important role in drug metabolism. The gene encoding human POR is highly polymorphic, which is of great clinical significance by having an significant effect on the metabolism and even curative effects of clinically used drugs. Studies on the pharmacogenomics of POR in recent years are summarized as follows.

Key words: Cytochrome P450 oxidoreductase, Pharmacogenomics, Cytochrome P450 enzymes, Electron donor, Genetic polymorphism, Drug metabolism

中图分类号:

R968

胡蕾, 高利臣, 卓伟, 周宏灏, 范岚. CYP450氧化还原酶的药物基因组学研究进展[J]. 中国临床药理学与治疗学, 2012, 17(7): 821-827.

HU Lei, GAO Li-chen, ZHUO Wei, ZHOU Hong-hao, FAN Lan. Advances in pharmacogenomics of cytochrome P450 oxidoreductase[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2012, 17(7): 821-827.

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