The future therapeutic potential of histone demethylases: A critical analysis

Gioacchino Natoli, Giuseppe Testa, Francesca De Santa

Research output: Contribution to journalArticlepeer-review


Once regarded as an irreversible modification, the methylation of histone protein tails has recently been highlighted following the identification of enzymes capable of histone demethylation in response to developmental or environmental cues. An awareness of the dynamic nature of histone modification has stimulated interest in the concept that drugs targeting histone methylation/demethylation might provide treatments for cancer, inflammation and metabolic disorders. However, epigenetic therapies that target histone demethylation are at the concept stage. Histone demethylases and their potential as therapeutic targets are discussed in this review.

Original languageEnglish
Pages (from-to)607-615
Number of pages9
JournalCurrent Opinion in Drug Discovery and Development
Issue number5
Publication statusPublished - Sep 2009


  • Histone demethylation
  • Histone methylation
  • Hydroxylation
  • JmjC domain
  • Substrate specificity
  • Transcription

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology

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