多藥耐藥（MDR）是指腫瘤細(xì)胞接觸一種抗腫瘤藥物后，也對(duì)其他多種結(jié)構(gòu)不同、功能不同的抗腫瘤藥物產(chǎn)生耐藥性，其中外排型轉(zhuǎn)運(yùn)體所介導(dǎo)的MDR是其中至關(guān)重要的一部分。外排型轉(zhuǎn)運(yùn)體是指位于腫瘤細(xì)胞生物膜上的具有將抗腫瘤藥物從細(xì)胞內(nèi)外排到細(xì)胞外的轉(zhuǎn)運(yùn)體。已知的具有外排作用的轉(zhuǎn)運(yùn)體有P糖蛋白（P-gp）、多藥耐藥相關(guān)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(zhuǎn)運(yùn)體的一般性質(zhì)并著重于闡述逆轉(zhuǎn)這些轉(zhuǎn)運(yùn)體介導(dǎo)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(guó)家自然科學(xué)基金項(xiàng)目（81473280）