肿瘤细胞中药物代谢酶表达和活性的研究与进展  

A review of the expression and activity of drug metabolism enzymes in tumorous cells

作　　者：肖文璟[1] 王广基[1] 阿基业[1] 

机构地区：[1]中国药科大学药物代谢动力学重点实验室,江苏南京210009

出　　处：《药学学报》2014年第10期1377-1386,共10页Acta Pharmaceutica Sinica

基　　金：江苏省自然科学基金资助项目(BK2012762)

摘　　要：肿瘤细胞具有十分独特的生存与代谢模式,研究肿瘤细胞的药物代谢特征对于了解药物在肿瘤细胞中的代谢和消除快慢进而评估并预测药效、基于代谢特征优化抗肿瘤药物/前体药物设计具有重要意义。本文综述了肝、肠、乳腺和肺等常见癌组织的主要药物代谢相关酶的表达/活性及其与正常组织的差异,阐述了部分典型抗肿瘤药物在肿瘤组织中的代谢特征,结合对应的常用体外培养肿瘤细胞株中药物代谢酶的表达/活性特征,探讨实体肿瘤组织(体内)和肿瘤细胞株(体外)中酶表达与功能的异同性及差异的产生原因。Tumorous cells are characterized by distinctive metabolic reprogramming and living conditions. Understanding drug metabolizing features in tumor cells will not only favor the estimation of metabolic rate, elimination half life and the assessment of potency, but also facilitate the optimal design of anti-tumor drugs/prodrugs. This article reviewed the expression and activity features of major drug metabolizing enzymes （DMEs） in solid tumorous tissues, such as liver, intestine, breast and lung, and the difference from the correspondingly normal tissues, exemplified by the metabolic properties of some classic antitumor-agents in tumorous tissues. In combination with the data retrieved in vitro tumor cell lines, we discussed the similarities and differences of DMEs expression and function between tumor tissues （in vivo） and tumor cells （in vitro）, and proposed the possible factors that cause the differences.

关 键 词：肿瘤组织/细胞 体外培养细胞株 药物代谢酶 药物设计 

分 类 号：R963[医药卫生—微生物与生化药学]