摘要
ATP结合盒超家族(ABC)转运蛋白组成了由48成员组成的7个亚科(从ABCA到ABCG)。除了其重要的生理和药理功能,ABC转运蛋白在因通过促使抗癌药物的外排而产生的多药耐药性(MDR)中扮演着重要的角色,特别是ABCB1, ABCG2 和ABCC成员。ABCB1转运蛋白抑制剂已有的研究为寻找抑制ABCB1和其他MDR相关性 ABC转运蛋白的新化合物提供的见解和策略。本文对该领域的研究进行了概括总结,重点突出了正在进行临床前和临床试验研究的药物试剂,包括酪氨酸激酶抑制剂、天然产物、microRNA和新的化学实体,并讨论了新型针对抑制癌症干细胞ABC转运蛋白的方法和该领域未来的前景。
关键词: ABC转运蛋白抑制剂,癌症干细胞,化疗,microRNA,多药耐药,酪氨酸激酶抑制剂。
图形摘要
Current Drug Targets
Title:ABC Transporter Inhibitors in Reversing Multidrug Resistance to Chemotherapy
Volume: 16 Issue: 12
Author(s): Haigang Cui, Anna J. Zhang, Mingwei Chen and Johnson J. Liu
Affiliation:
关键词: ABC转运蛋白抑制剂,癌症干细胞,化疗,microRNA,多药耐药,酪氨酸激酶抑制剂。
摘要: The superfamily of human ATP-binding cassette (ABC) transporters comprises seven subfamilies (ABCA to G) with 48 members. In addition to their profound physiological and pharmacological functions, ABC transporters play important roles in instigating multidrug resistance (MDR) in cancer by mediating the efflux of many anticancer drugs, particularly, ABCB1, ABCG2 and ABCC subfamily members. Previous development of ABCB1 transporter inhibitors has provided insights into seeking novel strategies in developing new classes of compound that inhibit ABCB1 and other MDRrelated ABC transporters. We herein review and evaluate current evidence in this area, with an emphasis on experimental and investigational agents that are under preclinical and clinical tests, including tyrosine kinase inhibitors, natural products, microRNAs and novel chemical entities. New strategies targeting ABC transporters in cancer stem cells and future perspectives in this field are also discussed.
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Cite this article as:
Haigang Cui, Anna J. Zhang, Mingwei Chen and Johnson J. Liu , ABC Transporter Inhibitors in Reversing Multidrug Resistance to Chemotherapy, Current Drug Targets 2015; 16 (12) . https://dx.doi.org/10.2174/1389450116666150330113506
DOI https://dx.doi.org/10.2174/1389450116666150330113506 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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