细胞色素酶CYP3A4基因多态性研究进展

Progress in research of cytochrome P450 3A4 gene polymorphism

背景药物代谢酶的基因多态性是导致药物在体内处置和反应存在明显个体差异的重要因素之一，而细胞色素酶P450家族的CYP3A4（cytochrome P450 3A4）酶是药物及外源性物质的主要代谢酶。CYP3A4基因多态性是导致这些药物代谢个体差异的主要原因。目的就CYP3A4基因多态性对药物代谢的影响作一综述。内容CYP3A4主要分布于肝脏和小肠内，其基因结构、酶活性的个体差异以及遗传多态性的种族差异，是导致药物作用和副作用个体差异的主要原因，甚至与许多疾病包括肿瘤等的发病有关。趋向对CYP3A4基因多态性的研究将有助于提高药物疗效，避免副作用发生，预防和治疗某些疾病尤其是肿瘤等疾病。

Background The polymorphism of drug metabolism enzyme is an important factor leading to the obvious therapy reaction to drugs. Cytochrome P450 3A4 （CYP3A4）, one of CYP 3A sub-family, is the main metabolism enzyme of many drugs. CYP3A4 gene polymorphism is the main reason that leads to interindividual differences of drugs metabolization. Objective This review was focused on the effects of CYP 3A4 gene polymorphism on drugs reaction in available literatures. Content CYP3A4 is the main microsomal cytochrome P450 enzyme which is mainly distributed in human liver and intestine. Its interindividual variations in gene structure, genetic polymorphism and enzyme activity may result in differences among races such as drug actions and adverse effects and even causes many diseases such as coronary heart disease and tumor. Trend The study of CYP3A4 gene polymorphism may help improve the actions and avoid adverse effects of drugs, as well prevent and treat some diseases especially tumor.