多藥耐藥（MDR）是阻礙腫瘤化療成功的一大障礙，其機制之一就是耐藥的腫瘤細胞高表達三磷酸腺苷（ATP）結(jié)合盒（ABC）轉(zhuǎn)運體。依據(jù)此機制提出克服腫瘤細胞耐藥的策略即開發(fā)外排轉(zhuǎn)運體抑制劑，以期逆轉(zhuǎn)MDR。最近的研究發(fā)現(xiàn)腫瘤干細胞也可能是通過表達外排轉(zhuǎn)運體天然耐藥，這就提供了一個新的抗癌藥物作用靶點。對介導(dǎo)腫瘤細胞多藥耐藥的ABC轉(zhuǎn)運體及其抑制劑的開發(fā)作一綜述。

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.

國家自然科學(xué)基金資助項目（81273580, 81072694）