P‐glycoprotein (P‐gp) has been considered an important molecular target in the reversal of multidrug resistance (MDR). As such, the development of P‐gp modulators able to restore drug sensitivity in resistant cells is still considered one of the most promising strategies for overcoming MDR. Since the identification of the P‐gp's role in MDR, several studies have been performed in order to develop effective P‐gp modulators and understand the efflux mechanism. However, no efflux modulator is still clinically available for treating multidrug‐resistant cancers. Nevertheless, recent experimental studies suggest that MDR can be surpassed by targeting a specific region within the ABC transporter structure rather than the polyspecific drug‐binding pocket. This article will focus on the information available about this new target region and on a brief overview of which scaffolds would be suitable for modulating P‐gp at this new location. WIREs Comput Mol Sci 2017, 7:e1316. doi: 10.1002/wcms.1316

中文翻译：

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关于P糖蛋白：结构数据正在形成一个新的可药物治疗领域

P-糖蛋白（P-gp）被认为是逆转多药耐药性（MDR）的重要分子靶标。因此，开发能够在耐药细胞中恢复药物敏感性的P-gp调节剂仍被认为是克服MDR的最有希望的策略之一。自从确定P‐gp在MDR中的作用以来，已经进行了数项研究，以开发有效的P‐gp调节剂并了解外排机制。但是，临床上尚无外排调节剂可用于治疗多药耐药性癌症。尽管如此，最近的实验研究表明，通过靶向ABC转运蛋白结构内的特定区域而不是多特异性药物结合口袋，可以超越MDR。电线Comput Mol Sci 2017，7：e1316。doi：10.1002 / wcms.1316