中文摘要：

肿瘤多药耐药（MDR）是导致肿瘤化疗失败的主要原因之一，是多种复杂机制：共同作用的结果。其中，肿瘤细胞膜上ATP结合盒（ABC）转运蛋白的表达或功能异常是肿瘤细胞产生MDR的重要机制之一。现以P-糖蛋白、多药耐药相关蛋白、乳腺癌耐药蛋白等为例，综述ABC转运蛋白的结构功能、与肿瘤的关系以及MDR逆转剂的研发进展。

英文摘要：

A significant impediment to the success of cancer chemotherapy is muhidrug resistance （MDR） and this could be attributable to concomitance of multiple intricate mechanisms. Overexpression or functional abnormality of membrane drug transport proteins of ATP-binding cassette （ABC） family which results in an increased drug efflux, could be one of the main mechanisms. Accumulative evidence shows that P- glycoprotein （ P- gp）, Muhidrug resistance- associated proteins （MRPs） and breast cancer resistance protein （BCRP）, identified in last three decades, confer resistance to multiple chemotherapeutic agents when overexpressed in human tumors. This review will address the structure and function of drug transporters in ABC family and focus on the research advancement on the mechanism of tumors muhidrug resistance mediated by ABC transporters family and the development of their inhibitors.