Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight

被引:546
作者
Ho, Terence C. S. [1 ]
Chan, Alex H. Y. [1 ]
Ganesan, A. [1 ]
机构
[1] Univ East Anglia, Sch Pharm, Norwich NR4 7TJ, Norfolk, England
关键词
D O I
10.1021/acs.jmedchem.0c00830
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
It is now 30 years since the first report of a potent zinc-dependent histone deacetylase (HDAC) inhibitor appeared. Since then, five HDAC inhibitors have received regulatory approval for cancer chemotherapy while many others are in clinical development for oncology as well as other therapeutic indications. This Perspective reviews the biological and medicinal chemistry advances over the past 3 decades with an emphasis on the design of selective inhibitors that discriminate between the 11 human HDAC isoforms.
引用
收藏
页码:12460 / 12484
页数:25
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