[關(guān)鍵詞]
[摘要]
多藥耐藥(MDR)是阻礙腫瘤化療成功的一大障礙,其機(jī)制之一就是耐藥的腫瘤細(xì)胞高表達(dá)三磷酸腺苷(ATP)結(jié)合盒(ABC)轉(zhuǎn)運(yùn)體。依據(jù)此機(jī)制提出克服腫瘤細(xì)胞耐藥的策略即開(kāi)發(fā)外排轉(zhuǎn)運(yùn)體抑制劑,以期逆轉(zhuǎn)MDR。最近的研究發(fā)現(xiàn)腫瘤干細(xì)胞也可能是通過(guò)表達(dá)外排轉(zhuǎn)運(yùn)體天然耐藥,這就提供了一個(gè)新的抗癌藥物作用靶點(diǎn)。對(duì)介導(dǎo)腫瘤細(xì)胞多藥耐藥的ABC轉(zhuǎn)運(yùn)體及其抑制劑的開(kāi)發(fā)作一綜述。
[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.
[中圖分類號(hào)]
[基金項(xiàng)目]
國(guó)家自然科學(xué)基金資助項(xiàng)目(81273580, 81072694)