Department of Pharmacy, Anhui Provincial Hospital, 17 Lujiang Road, Hefei, Anhui 230001, China; Institute for Liver Diseases of Anhui Medical University (AMU), Anhui Institute of Innovative Drugs, Anhui Key Laboratory of Bioactivity of Natural Products, School of Pharmacy, Anhui Medical University, Hefei, Anhui 230032, China.
Department of Pharmacy, Anhui Provincial Hospital, 17 Lujiang Road, Hefei, Anhui 230001, China.
Cancer Lett. 2016 Jan 1;370(1):153-64. doi: 10.1016/j.canlet.2015.10.010. Epub 2015 Oct 20.
Multidrug resistance (MDR) is a serious phenomenon employed by cancer cells which hampers the success of cancer pharmacotherapy. One of the common mechanisms of MDR is the overexpression of ATP-binding cassette (ABC) efflux transporters in cancer cells such as P-glycoprotein (P-gp/ABCB1), multidrug resistance-associated protein 2 (MRP2/ABCC2), and breast cancer resistance protein (BCRP/ABCG2) that limits the prolonged and effective use of chemotherapeutic drugs. Researchers have found that developing inhibitors of ABC efflux transporters as chemosensitizers could overcome MDR. But the clinical trials have shown that most of these chemosensitizers are merely toxic and only show limited or no benefits to cancer patients, thus new inhibitors are being explored. Recent findings also suggest that efflux pumps of the ABC transporter family are subject to epigenetic gene regulation. In this review, we summarize recent findings of the role of ABC efflux transporters in MDR.
多药耐药（MDR）是癌细胞采用的一种严重现象，它阻碍了癌症化疗的成功。MDR 的常见机制之一是 ABC 转运蛋白（ABC）外排转运体在癌细胞中的过度表达，如 P-糖蛋白（P-gp/ABCB1）、多药耐药相关蛋白 2（MRP2/ABCC2）和乳腺癌耐药蛋白（BCRP/ABCG2），这限制了化疗药物的长期和有效使用。研究人员发现，开发 ABC 外排转运体抑制剂作为化疗增敏剂可以克服 MDR。但临床试验表明，这些化疗增敏剂大多数仅具有毒性，对癌症患者仅显示有限或没有益处，因此正在探索新的抑制剂。最近的研究结果还表明，ABC 转运蛋白家族的外排泵受到表观遗传基因调控。在这篇综述中，我们总结了 ABC 外排转运体在 MDR 中的作用的最新发现。
