ABCG2 is a half ATP-binding cassette (ABC) transporter that facilitates efflux of a wide variety of substrates ranging from natural products to synthetic anticancer drugs. Over-expression of ABCG2 has been shown to cause multidrug resistance in both laboratory model cell lines and in clinical settings. The polymorphism in ABCG2 has also been suggested to affect the function and clinical outcome in cancer patients. More recently, ABCG2 has been suggested to play a protective role for cancer and normal stem cells. Thus, ABCG2 is an ideal target for therapeutic development to chemosensitize drug resistant cancers. In this paper, the recent progress on understanding the structure, function, and pharmacology of ABCG2 and its role in drug resistance and cancer stem cells will be reviewed.%ABCG2是半ATP结合盒转运体.它可以转运内源性物质和人工合成的抗肿瘤药物等多种底物.细胞模型和临床研究证明ABCG2的过表达会引起多药耐药.同时,ABCG2的多态性可以影响其功能和肿瘤患者的临床疗效.新近的研究表明ABCG2对于干细胞和肿瘤干细胞有保护作用.因此,ABCG2成为提高化疗耐药肿瘤疗效的理想靶点.本文将综述ABCG2的结构、功能、药理学作用及其对多药耐药和肿瘤干细胞作用的最新进展.
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