逆转肿瘤耐药性的策略及相关小分子药物的研究进展  

Strategies for reversing multidrug resistance and advances in related small molecular anticancer drugs

作　　者：姚广丰[1] 刘丹[1] 陈曦[1] 程杰[1] 赵临襄[1] 

机构地区：[1]教育部基于靶点的药物设计与评价重点实验室,沈阳药科大学,辽宁沈阳110016

出　　处：《中国药物化学杂志》2010年第5期450-459,共10页Chinese Journal of Medicinal Chemistry

基　　金：辽宁省教育厅项目(LS2010159)

摘　　要：多药耐药(multidrug resistance,MDR)是肿瘤化疗失败最常见而又最难解决的问题。研究MDR机制,开发具有克服MDR作用的新型化疗药物是抗肿瘤药物研究的一个热点领域。肿瘤细胞耐药是一个复杂的、动态的体系,可以发生在细胞膜或细胞质水平,也可发生在细胞解毒系统、DNA修复系统以及药物作用靶点的改变上。该文在总结逆转肿瘤耐药性策略的基础上,对MDR逆转剂、作用于细胞解毒系统以及作用于Bcl-2家族、DNMT和p53等新靶点的小分子药物的研究进展进行综述。Cancer multidrug resistance（MDR） is one of the major causes of chemotherapy failure.Investigating the mechanisms of MDR and developing new anticancer drugs which can overcome MDR are hot research fields in anticancer drugs developing.Cancer drug resistance which is a complex and dynamic system can occur not only in cellular membrane or cytoplasm level,but also in cellular detoxification system,DNA repair system and the change of drug targets.On the basis of the strategies for reversing MDR,this article describes the advances in the research of MDR reversal agents and related small molecule anticancer drugs which act on the cellular detoxification system or drug targets such as Bcl-2,DNMT and p53.

关 键 词：多药耐药 ABC转运蛋白 谷胱甘肽 硫氧还蛋白 Bcl-2 DNA甲基化 p53 坏死状凋亡 

分 类 号：R979.1[医药卫生—药品]