Xiao Huan, Zheng Yongcheng, Ma Lingling, Tian Lili, Sun Qiu
State Key Laboratory of Biotherapy, Cancer Center, West China Hospital, Sichuan University and Collaborative Innovation Center for Biotherapy, Chengdu, China.
Department of Anesthesiology, Sichuan Provincial People's Hospital, University of Electronic Science and Technology of China, Chengdu, China.
Front Pharmacol. 2021 Apr 19;12:648407. doi: 10.3389/fphar.2021.648407. eCollection 2021.
Multiple drug resistance (MDR), referring to the resistance of cancer cells to a broad spectrum of structurally and mechanistically unrelated drugs across membranes, severely impairs the response to chemotherapy and leads to chemotherapy failure. Overexpression of ATP binding cassette (ABC) transporters is a major contributing factor resulting in MDR, which can recognize and mediate the efflux of diverse drugs from cancer cells, thereby decreasing intracellular drug concentration. Therefore, modulators of ABC transporter could be used in combination with standard chemotherapeutic anticancer drugs to augment the therapeutic efficacy. This review summarizes the recent advances of important cancer-related ABC transporters, focusing on their physiological functions, structures, and the development of new compounds as ABC transporter inhibitors.
多药耐药性（MDR）是指癌细胞对多种结构和作用机制不同的跨膜药物产生耐药性，这严重削弱了化疗反应并导致化疗失败。ATP结合盒（ABC）转运蛋白的过表达是导致MDR的一个主要因素，它能够识别并介导多种药物从癌细胞中流出，从而降低细胞内药物浓度。因此，ABC转运蛋白调节剂可与标准化疗抗癌药物联合使用，以提高治疗效果。本综述总结了重要的癌症相关ABC转运蛋白的最新进展，重点关注它们的生理功能、结构以及作为ABC转运蛋白抑制剂的新化合物的开发。
