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用于克服癌症多药耐药性的天然产物调节剂。

Natural product modulators to overcome multidrug resistance in cancer.

作者信息

Cort Aysegul, Ozben Tomris

机构信息

a Department of Biochemistry, Faculty of Medicine , Akdeniz University , Antalya , Turkey.

出版信息

Nutr Cancer. 2015;67(3):411-23. doi: 10.1080/01635581.2015.1002624. Epub 2015 Feb 3.

Abstract

Multidrug resistance (MDR) is a condition that makes cells simultaneously unresponsive to different drugs, unrelated to their chemical structure and mechanism of action. MDR caused by the presence and overexpression of ABC transporters makes obstacles in cancer treatment and lower the effectiveness of chemotherapy. Natural products are investigated by many researchers as MDR modulators for their low toxicity and potent, selective behavior. When coadministered, MDR modulators compete with cytotoxic agents for binding to the active site of the membrane transporters and reduce drug efflux. Natural product-based drugs are important in struggling against drug resistance during cancer therapy. This review is focused on the potential mechanisms against drug resistance, the development of inhibitors for ABC drug transporters, natural product modulators, and nanoparticle drug delivery.

摘要

多药耐药性(MDR)是一种使细胞同时对不同药物无反应的状态,这些药物与其化学结构和作用机制无关。由ABC转运蛋白的存在和过表达引起的MDR给癌症治疗带来了障碍,并降低了化疗的效果。许多研究人员对天然产物作为MDR调节剂进行了研究,因为它们具有低毒性以及强效、选择性的特性。当联合使用时,MDR调节剂与细胞毒性药物竞争结合膜转运蛋白的活性位点,减少药物外排。基于天然产物的药物在癌症治疗中对抗耐药性方面具有重要意义。本综述聚焦于抗耐药性的潜在机制、ABC药物转运蛋白抑制剂的开发、天然产物调节剂以及纳米颗粒药物递送。

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