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新一代选择性组蛋白去乙酰化酶抑制剂。

Next-generation of selective histone deacetylase inhibitors.

作者信息

Yang Feifei, Zhao Na, Ge Di, Chen Yihua

机构信息

School of Biological Science and Technology, University of Jinan Jinan Shandong Province 250022 China.

Shanghai Key Laboratory of Regulatory Biology, The Institute of Biomedical Sciences and School of Life Sciences, East China Normal University Shanghai 200241 China

出版信息

RSC Adv. 2019 Jun 24;9(34):19571-19583. doi: 10.1039/c9ra02985k. eCollection 2019 Jun 19.

Abstract

Histone deacetylases (HDACs) are clinically validated epigenetic drug targets for cancer treatment. HDACs inhibitors (HDACis) have been successfully applied against a series of cancers. First-generation inhibitors are mainly pan-HDACis that target multiple isoforms which might lead to serious side effects. At present, the next-generation HDACis are mainly focused on being class- or isoform-selective which can provide improved risk-benefit profiles compared to non-selective inhibitors. Because of the rapid development in next-generation HDACis, it is necessary to have an updated and state-of-the-art overview. Here, we summarize the strategies and achievements of the selective HDACis.

摘要

组蛋白去乙酰化酶(HDACs)是经临床验证的癌症治疗表观遗传药物靶点。HDACs抑制剂(HDACis)已成功应用于一系列癌症的治疗。第一代抑制剂主要是泛HDACis,可靶向多种亚型,这可能会导致严重的副作用。目前,新一代HDACis主要聚焦于具有类别或亚型选择性,与非选择性抑制剂相比,其风险效益比更佳。由于新一代HDACis的快速发展,有必要进行一次更新的、最前沿的综述。在此,我们总结了选择性HDACis的策略和成果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f464/9065321/10af47a58d0d/c9ra02985k-f1.jpg

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