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

ABSTRACT: 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.

SUBMITTER: Das ND

PROVIDER: S-EPMC10048553 | biostudies-literature | 2023 Mar

REPOSITORIES: biostudies-literature

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

Das Nando Dulal ND Niwa Hideaki H Umehara Takashi T

Epigenomes 20230311 1

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 efficac ...[more]

PMID: 36975603

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