HDAC6型
乙酰化
化学
组蛋白
计算生物学
基因亚型
HDAC10型
表观遗传学
组蛋白脱乙酰基酶
生物化学
药品
生物
药物开发
药理学
基因
作者
Xin-Hui Zhang,Qin-Ma,Hui-Pan Wu,Mussa Yussuf Khamis,Yihan Li,Liying Ma,Hong‐Min Liu
标识
DOI:10.1021/acs.jmedchem.0c01782
摘要
Histone deacetylases (HDACs) are essential for maintaining homeostasis by catalyzing histone deacetylation. Aberrant expression of HDACs is associated with various human diseases. Although HDAC inhibitors are used as effective chemotherapeutic agents in clinical practice, their applications remain limited due to associated side effects induced by weak isoform selectivity. HDAC6 displays unique structure and cellular localization as well as diverse substrates and exhibits a wider range of biological functions than other isoforms. HDAC6 inhibitors have been effectively used to treat cancers, neurodegenerative diseases, and autoimmune disorders without exerting significant toxic effects. Progress has been made in defining the crystal structures of HDAC6 catalytic domains which has influenced the structure-based drug design of HDAC6 inhibitors. This review summarizes recent literature on HDAC6 inhibitors with particular reference to structural specificity and functional diversity. It may provide up-to-date guidance for the development of HDAC6 inhibitors and perspectives for optimization of therapeutic applications.
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