多藥耐藥（MDR）是指腫瘤細胞接觸一種抗腫瘤藥物后，也對其他多種結構不同、功能不同的抗腫瘤藥物產生耐藥性，其中外排型轉運體所介導的MDR是其中至關重要的一部分。外排型轉運體是指位于腫瘤細胞生物膜上的具有將抗腫瘤藥物從細胞內外排到細胞外的轉運體。已知的具有外排作用的轉運體有P糖蛋白（P-gp）、多藥耐藥相關蛋白（MRP）、乳腺癌耐藥蛋白（BCRP）和肺耐藥蛋白（LRP）。綜述這幾種外排型轉運體的一般性質并著重于闡述逆轉這些轉運體介導的多藥耐藥的藥物及方法。

Multidrug resistance (MDR) refers to the resistance that the cancer cells will display to multiple structurally dissimilar and functionally diverse drugs after exposing to an anticancer drug and MDR mediated by efflux transporters is one crucial part of MDR. Multidrug resistance (MDR) is defined as the resistance to Efflux transporters, located in the biological membranes, can extrudea variety of structurally diverse drugs from the cell. There are several sorts of known efflux transporters:P-glycoprotein (P-gp), the multidrug resistance proteins (MRPs) 1-5, the breast cancer resistance protein (BCRP) and lung resistant protein. This review concentrates the general propertieson those efflux transporters and the revier will be more focus on the drugs and methods to reversing MDR.

國家自然科學基金項目（81473280）