ATP-binding cassette (ABC) transporters represent one of the largest and oldest families of membrane proteins in all extant phyla from prokaryotes to humans, which couple the energy derived from ATP hydrolysis essentially to translocate, among various substrates, toxic compounds across the membrane. The fundamental functions of these multiple transporter proteins include: (1) conserved mechanisms related to nutrition and pathogenesis in bacteria, (2) spore formation in fungi, and (3) signal transduction, protein secretion and antigen presentation in eukaryotes. Moreover, one of the major causes of multidrug resistance (MDR) and chemotherapeutic failure in cancer therapy is believed to be the ABC transporter-mediated active efflux of a multitude of structurally and mechanistically distinct cytotoxic compounds across membranes. It has been postulated that ABC transporter inhibitors known as chemosensitizers may be used in combination with standard chemotherapeutic agents to enhance their therapeutic efficacy. The current paper reviews the advance in the past decade in this important domain of cancer chemoresistance and summarizes the development of new compounds and the re-evaluation of compounds originally designed for other targets as transport inhibitors of ATP-dependent drug efflux pumps.

中文翻译：

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癌症中ABC转运蛋白介导的多药耐药性的调节：过去十年的回顾。

ATP结合盒（ABC）转运蛋白代表了从原核生物到人类的所有现存门中最大，最古老的膜蛋白家族之一，它结合了ATP水解产生的能量，从而在各种底物之间转移有毒化合物穿过膜。这些多种转运蛋白的基本功能包括：（1）与细菌营养和发病机理有关的保守机制，（2）真菌中孢子形成，以及（3）真核生物中的信号转导，蛋白分泌和抗原呈递。此外，据信癌症治疗中多药耐药性（MDR）和化学治疗失败的主要原因之一是ABC转运蛋白介导的多种结构上和机理上不同的细胞毒性化合物跨膜的主动外排。假定可以将称为化学增敏剂的ABC转运蛋白抑制剂与标准化学治疗剂联合使用，以增强其治疗功效。本篇论文回顾了过去十年间在这一重要的化学抗癌性领域取得的进展，并总结了新化合物的开发以及对最初设计用于其他靶点作为ATP依赖性药物外排泵转运抑制剂的化合物的重新评估。