CYP2D6基因多态性及对药物代谢的影响  

Polymorphism of CYP2D6 and the influence to the drug metabolism

作　　者：韩璐[1] 刘洁 

机构地区：[1]中南大学临床药理研究所

出　　处：《中国临床药理学与治疗学》2011年第1期105-110,共6页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：国家自然科学基金项目(30600774及81070902);教育部"新世纪优秀人才支持计划"(NCET-08-0567);2010年中南大学硕士生学位论文创新资助项目资助

摘　　要：CYP2D6代谢酶是细胞色素P450家族中的成员之一,是参与Ⅰ相代谢和众多内源性物质和不同药物消除的酶。虽然它在肝脏中的含量大约只占肝脏总量的2%,但在临床上却参与了25%以上的常用药物的代谢活动。在所有参与药物代谢的细胞色素P450基因家族中,CYP2D6是唯一不能被诱导的酶,这种酶具有广泛的多态性,这种多态性对酶的药物代谢功能具有重要影响,CYP2D6的这种多态性和药物代谢功能所表现的对个体活性的差异,在遗传药理学上具有重要意义。本文从CYP2D6基因多态性和它对药物代谢的影响这两方面进行了阐述。CYP2D6 is a member of cytochrome P450 gene family-a group of enzymes that is responsible for phase I metabolism and elimination of numerous endogenous substrates and a diverse array of drugs.It is now thought to be involved in the metabolism of up to 25% of the drugs that are in common use in the clinic,despite its low hepatic content（about 2 %）.Among the drug-metabolizing cytochrome P450s,CYP2D6 is the only non-inducible enzyme and is highly polymorphic,which results in a large contribution of genetic variation to its inter-individual variation in enzyme activity and is an enzyme of great historical importance for pharmacogenetics.Here we summarize the polymorphism of CYP2D6 gene and their influence to drug metabolism.

关 键 词：CYP2D6 基因多态性 药物代谢 

分 类 号：R969[医药卫生—药理学]