Next-generation of selective histone deacetylase inhibitors

被引：104

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

页码：19571 / 19583

页数：13

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