人CYP的异源表达及其在新药研发早期的作用  

Heterogeneous expression of human CYP and its application in early stage of new drug research and development

作　　者：谢章明[1] 陈枢青[1] 

机构地区：[1]浙江大学药学院药理毒理与生化药学研究所,浙江杭州310058

出　　处：《浙江大学学报（医学版）》2013年第1期109-113,共5页Journal of Zhejiang University(Medical Sciences)

基　　金：国家科技重大专项基金(重大新药专项)(2012ZX09506001-004)

摘　　要：人细胞色素P450(cytochrome P450,CYP)在临床上对外源及内源性的物质代谢起着至关重要的作用。由于从人组织中获取的CYP成分较为复杂,且人组织本身不易获得,人们开始用各种表达系统来进行CYP的异源表达,并将表达得到的单一CYP用于药物代谢及药物-药物相互作用的研究,从而大大提高了药物高通量筛选的效率。另外,由于药物代谢酶的多态性使不同人群表现出对某种药物药效的差异,因此对某种CYP突变体的异源表达和药物代谢研究,将有助于指导治疗方案的优化,实施个体化药物治疗。Human cytochrome P450 （CYP） has a pivotal role on metabolism of xenobiotics and endogenous substances in clinical practice. Since the CYP from human tissue is very complex, and the human tissue itself is not easy to obtain, investigators begin to use all kinds of expression system to heterogeneously express the CYP. The single CYP expressed was then used for drug metabolism and drug-drug interaction research, to improve the efficiency of high-throughput drug screening greatly. Besides, since the polymorphism of drug-metabolizing enzymes makes efficacy variance for some drugs in different population, the heterougeneous expression and drug metabolizing research of certain CYP mutants will be helpful to guide the optimization of therapeutic regimen and conduct the personalized medication.

关 键 词：细胞色素P450酶系统 异源表达 药物利用 药物设计 

分 类 号：R91[医药卫生—药学]