[关键词]
[摘要]
多药耐药(MDR)是阻碍肿瘤化疗成功的一大障碍,其机制之一就是耐药的肿瘤细胞高表达三磷酸腺苷(ATP)结合盒(ABC)转运体。依据此机制提出克服肿瘤细胞耐药的策略即开发外排转运体抑制剂,以期逆转MDR。最近的研究发现肿瘤干细胞也可能是通过表达外排转运体天然耐药,这就提供了一个新的抗癌药物作用靶点。对介导肿瘤细胞多药耐药的ABC转运体及其抑制剂的开发作一综述。
[Key word]
[Abstract]
Multidrug resistance (MDR) is a formidable obstacle in cancer pharmacotherapy. One of the mechanism is ATP-binding cassette (ABC) transporters overexpression in multidrug resistant tumor cells. The strategy to overcome MDR in cells expressing ABC efflux transporters is to develop the inhibitors of efflux transporters, likely reversing MDR. Furthermore, the recent studies demonstrated that the tumor stem cells may be innately resisted through the expressing efflux transporters. This provides one new therapeutic target for anti-cancer. In this review, we provide the overviews of ABC transporters in multidrug resistant tumor cells and the development of ABC transporter inhibitors.
[中图分类号]
[基金项目]
国家自然科学基金资助项目(81273580, 81072694)