Next-generation of selective histone deacetylase inhibitors

被引:94
|
作者
Yang, Feifei [1 ,2 ,3 ]
Zhao, Na [1 ]
Ge, Di [1 ]
Chen, Yihua [2 ,3 ]
机构
[1] Univ Jinan, Sch Biol Sci & Technol, Jinan 250022, Shandong, Peoples R China
[2] East China Normal Univ, Shanghai Key Lab Regulatory Biol, Inst Biomed Sci, Shanghai 200241, Peoples R China
[3] East China Normal Univ, Sch Life Sci, Shanghai 200241, Peoples R China
来源
RSC ADVANCES | 2019年 / 9卷 / 34期
基金
中国国家自然科学基金;
关键词
DIVERSITY-ORIENTED SYNTHESIS; BIOLOGICAL EVALUATION; HDAC INHIBITORS; CANCER-THERAPY; MOLECULAR-MECHANISMS; ISOFORM SELECTIVITY; EPIGENETIC THERAPY; ACID-DERIVATIVES; RATIONAL DESIGN; ACTIVITY ASSAY;
D O I
10.1039/c9ra02985k
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
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.
引用
收藏
页码:19571 / 19583
页数:13
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