Inhibit or Evade Multidrug Resistance P-Glycoprotein in Cancer Treatment,Journal of Medicinal Chemistry

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Inhibit or Evade Multidrug Resistance P-Glycoprotein in Cancer Treatment
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2017-12-18 00:00:00 , DOI: 10.1021/acs.jmedchem.7b01457
Deepali Waghray ₁ , Qinghai Zhang ₁

Affiliation

Multidrug resistance (MDR) is a major cause of failure in cancer chemotherapy. P-glycoprotein (P-gp), a promiscuous drug efflux pump, has been extensively studied for its association with MDR due to overexpression in cancer cells. Several P-gp inhibitors or modulators have been investigated in clinical trials in hope of circumventing MDR, with only limited success. Alternative strategies are actively pursued, such as the modification of existing drugs, development of new drugs, or combination of novel drug delivery agents to evade P-gp-dependent efflux. Despite the importance and numerous studies, these efforts have mostly been undertaken without a priori knowledge of how drugs interact with P-gp at the molecular level. This review highlights and discusses progress toward and challenges impeding drug development for inhibiting or evading P-gp in the context of our improved understanding of the structural basis and mechanism of P-gp-mediated MDR.

中文翻译：

抑制或避免多药耐药性P-糖蛋白在癌症治疗中的作用

多药耐药性（MDR）是癌症化疗失败的主要原因。P-糖蛋白（P-gp）是一种混杂的药物外排泵，由于其在癌细胞中的过表达而与MDR相关联，因此已被广泛研究。在临床试验中已经研究了几种P-gp抑制剂或调节剂，希望绕开MDR，但仅获得有限的成功。积极地寻求替代策略，例如修改现有药物，开发新药物或组合新型药物输送剂，以逃避P-gp依赖性外排。尽管很重要，并且进行了许多研究，但是这些努力大多是在没有先验知识的情况下进行的，这些研究涉及药物如何在分子水平上与P-gp相互作用。

更新日期：2017-12-18

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