基于ATP结合盒转运蛋白逆转肿瘤多药耐药的研究进展药学学报.PDFVIP

药学学报 Acta Pharmaceutica Sinica 2010, 45 ( 10) : 1205 1211 ·1205 · 基于ATP-结合盒转运蛋白逆转肿瘤多药耐药的研究进展 * 宁, 孙 华, 刘耕陶 ( 中国医学科学院、北京协和医学院 物研究所, 北京 100050) 摘要: ATP-结合盒 (ATP-binding cassette , ABC) 转运蛋白是ATP 依赖性药物外排泵, 其表达或功能异常是 肿瘤细胞产生多药耐 (multi-drug resistance, MDR) 的重要机制之一。目前, 以ABC 转运蛋白为靶点的逆转肿 瘤MDR 的研究最为广泛与深入。本文总结了ABC 转运蛋白的结构与功能、ABC 转运蛋白与肿瘤MDR 的关系 及以其为靶点的MDR 逆转剂与逆转策略的研究进展。 关键词: 多 耐 ; ABC 转运蛋白; P-糖蛋白; 多 耐 相关蛋白; 乳腺癌耐药蛋白 中图分类号: R963 文献标识码:A 文章编号: 05 13-4870 (2010) 10-1205-07 Advances in the targeting ATP-binding cassette transporters to overcome tumor multi-drug resistance * WEI Ning , SUN Hua, LIU Geng-tao (Institute of Materia Medica, Chinese Academy of M edical Sciences and Peking Union M edical College, Beij ing 100050, China) Abstract: ATP-binding cassette (ABC) transporters are a family of proteins that mediate multi-drug resistance (MDR) via ATP-dependent drug efflux pumps. Abnormally expression and function would result in tumor MDR. That is the most important mechanism of MDR. The inhibition of ABC transporters as a strategy to reverse MDR in cancer has been studied extensively. In this review, we reviewed the structure and function of ABC transporters, and focused on the research advances in the mechanism of tumors MDR mediated by ABC transporters and the development of their modulators and reversal strategies. Key words: multi-drug resistance; ABC transporter; P-glycoprotein ; multi-drug resistance associated protein ; breast cancer resistance protein 当前肿瘤化学治疗最大障碍之一就是肿瘤细胞