Drug discovery of histone lysine demethylases (KDMs) inhibitors (progress from 2018 to present).

Xingrui He, Hang Zhang, Yingqian Zhang, Yang Ye, Shuo Wang, Renren Bai, Tian Xie, Xiang-Yang Ye

European journal of medicinal chemistry 2022 Mar 05

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Post-translational modifications (PTMs) of histone by histone demethylases (KDMs) play an important role in the regulation of gene expression, which implicates the development of various human cancers and other diseases. Discovering and developing inhibitors targeting KDMs have become an active and fast-growing research area over the past decades. In this review, the latest emerging small-molecule inhibitors of KDMs were surveyed with the emphasis on the literature since 2018, including lysine specific demethylases (LSD or KDM1) inhibitors and JmjC family N-methyl lysine demethylases (JmjC KDMs, i.e. KDM2-7) inhibitors. The drug design strategy, the structure-activity relationships (SARs), the analysis and insight of co-crystal structures, and the mechanisms of action (MOA) were also discussed. Copyright © 2022 Elsevier Masson SAS. All rights reserved.

Citation

Xingrui He, Hang Zhang, Yingqian Zhang, Yang Ye, Shuo Wang, Renren Bai, Tian Xie, Xiang-Yang Ye. Drug discovery of histone lysine demethylases (KDMs) inhibitors (progress from 2018 to present). European journal of medicinal chemistry. 2022 Mar 05;231:114143