Next-generation of selective histone deacetylase inhibitors

Feifei Yang; Na Zhao; Di Ge; Yihua Chen

doi:10.1039/c9ra02985k

Next-generation of selective histone deacetylase inhibitors

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

Authors

Feifei Yang^{1

2}, Na Zhao¹, Di Ge¹, Yihua Chen²

Affiliations

¹ School of Biological Science and Technology, University of Jinan Jinan Shandong Province 250022 China.
² Shanghai Key Laboratory of Regulatory Biology, The Institute of Biomedical Sciences and School of Life Sciences, East China Normal University Shanghai 200241 China yhchen@bio.ecnu.edu.cn.

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.

Publication types

Review