在众多已知的多重耐药机制中，ATP结合盒（ABC）转运蛋白将药物分子从细胞中排出是限制现代抗癌药物疗效的主要因素。在本综述中，我们突出了有关主要MDR相关ABC转运蛋白（例如P糖蛋白（P-gp），多药抗性蛋白1（MRP1）和乳腺癌耐药蛋白（BCRP））的结构、功能和调节机制的更新信息，以及调节剂对其功能的影响。我们还提供了有关可用于对抗癌症治疗中出现的MDR危机的不同ABC转运蛋白调节剂的重点信息。最后，我们还讨论了将ABC转运蛋白作为治疗靶点的重要性，以及将ABC转运蛋白抑制剂转化为临床实践的未来战略规划。版权所有© 2023 Elsevier Ltd.。保留所有权利。

Of the many known multidrug resistance (MDR) mechanisms, ATP-binding cassette (ABC) transporters expelling drug molecules out of cells is a major factor limiting the efficacy of present-day anticancer drugs. In this review, we highlights updated information on the structure, function, and regulatory mechanisms of major MDR-related ABC transporters, such as P-glycoprotein (P-gp), multidrug resistance protein 1 (MRP1), and breast cancer resistance protein (BCRP), and the effect of modulators on their functions. We also provide focused information on different modulators of ABC transporters that could be utilized against the emerging MDR crisis in cancer treatment. Finally, we discuss the importance of ABC transporters as therapeutic targets in light of future strategic planning for translating ABC transporter inhibitors into clinical practice.Copyright © 2023 Elsevier Ltd. All rights reserved.