Advances in histone deacetylase 8 selective inhibitors
10.11665/j.issn.1000-5048.20160301
- VernacularTitle:组蛋白去乙酰化酶8选择性抑制剂的研究进展
- Author:
Jiaqi NIU
1
;
Yong ZHU
;
Shuang ZHAO
;
Xiaotian TANG
;
Zhimin ZHANG
;
Tao LU
Author Information
1. 中国药科大学理学院
- Publication Type:Journal Article
- Keywords:
histone deacetylase 8;
structure;
function;
selective inhibitor;
target;
antitumor activity;
advance
- From:
Journal of China Pharmaceutical University
2016;47(3):251-258
- CountryChina
- Language:Chinese
-
Abstract:
Histone deacetylase 8(HDAC8)is a zinc-dependent class I histone deacetylase, closely related to human pathophysiology. HDAC8 involves in various critical signaling networks and is implicated as a therapeutic target in various diseases, including cancer, X-linked intellectual disability and parasitic infections. More and more selective HDAC8 inhibitors have been developed based on deepening study of its well-characterized crystal structure. They are mainly divided into several categories such as phenyl hydroxamic acids, indoles, ortho-aryl-N-hydroxycinnamides, azetidinones etc. . Current challenges remain in the development of potent selective inhibitors that would specifically target HDAC8 with fewer adverse effects compared with pan-HDAC inhibitors. Herein, we reviewed the progress in the study of structure and functions of HDAC8 as well as the development of selective HDAC8 inhibitors.
