title: The future therapeutic potential of histone demethylases: A critical analysis.
abstract: 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.
authors.affiliation: European Institue of Oncology, Department of Experimental Oncology, Milan, Italy. gioacchino.natoli@ifom-ieo-campus.it
authors.forename: Gioacchino
authors.initials: G
authors.lastname: Natoli
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Testa
authors.forename: Francesca
authors.initials: F
authors.lastname: De Santa
mesh_terms: D000818:Animals; D003640:Dealkylation; D015195:Drug Design; D055808:Drug Discovery; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D044127:Epigenesis, Genetic / Q000187:drug effects; D056466:Histone Demethylases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011495:Histone-Lysine N-Methyltransferase / Q000378:metabolism; D006657:Histones / Q000737:chemistry / Q000378:metabolism*; D006801:Humans; D056484:Jumonji Domain-Containing Histone Demethylases / Q000037:antagonists & inhibitors / Q000378:metabolism; D008239:Lysine; D008745:Methylation; D011499:Protein Processing, Post-Translational / Q000187:drug effects*; D055550:Protein Stability; D013379:Substrate Specificity; D014158:Transcription, Genetic / Q000187:drug effects
chemical_list: D004791:Enzyme Inhibitors; D006657:Histones; D056466:Histone Demethylases; D056484:Jumonji Domain-Containing Histone Demethylases; D011495:Histone-Lysine N-Methyltransferase; D008239:Lysine