Chemical Inhibitors Targeting the Histone Lysine Demethylase Families with Potential for Drug Discovery

Epigenomes

article

Nando Dulal Das¹  Hideaki Niwa¹  Takashi Umehara¹ 

[1] Laboratory for Epigenetics Drug Discovery, RIKEN Center for Biosystems Dynamics Research

关键词: chromatin;    epigenetics;    gene expression;    post-translational modification;    histone demethylation;   

DOI  :  10.3390/epigenomes7010007

学科分类：分子生物学，细胞生物学和基因

来源: mdpi

【 摘 要 】

The dynamic regulation of histone methylation and demethylation plays an important role in the regulation of gene expression. Aberrant expression of histone lysine demethylases has been implicated in various diseases including intractable cancers, and thus lysine demethylases serve as promising therapeutic targets. Recent studies in epigenomics and chemical biology have led to the development of a series of small-molecule demethylase inhibitors that are potent, specific, and have in vivo efficacy. In this review, we highlight emerging small-molecule inhibitors targeting the histone lysine demethylases and their progress toward drug discovery.

【 授权许可】

CC BY