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

Nando Dulal DasHideaki NiwaTakashi Umehara
Published in: Epigenomes (2023)
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.
Keyphrases
  • drug discovery
  • small molecule
  • dna methylation
  • gene expression
  • genome wide
  • protein protein
  • poor prognosis
  • amino acid
  • cancer therapy
  • young adults
  • binding protein