基于HDAC的双靶点抗肿瘤药物研究进展

The recent progress of dual inhibitors of HDAC

多靶点作用的抗肿瘤药物比目前单靶点药物具有更好的药效,且能够降低耐药性和毒副作用。为了探索多靶点药物在肿瘤化疗中的应用前景,以组蛋白去乙酰化酶(HDAC)抑制剂为基础设计多种作用的双靶点抑制剂已经成为了研究热点,其中部分化合物抑制肿瘤细胞增殖活性比现有的上市药物更好。本文综述了基于HDAC的双靶点抑制剂的研究进展,重点介绍了作用机制、设计策略和生物活性。

The multiple targets antitumor drugs have better efficacy than the single target drugs,and can reduce drug resistance and side effects. In order to explore the application prospect of multiple targets antitumor drugs in tumor chemotherapy,a variety of research on the basis of the HDAC inhibitor to design dual targets inhibitor has become a research hotspot,some compounds that inhibit tumor cell proliferation are better than existing listed drugs. This review mainly introduces the mechanism,design strategy,and biological activity.