逆转肿瘤耐药性的策略及相关小分子药物的研究进展

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。

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

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.