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.

The future therapeutic potential of histone demethylases : a critical analysis / G. Natoli, G. Testa, F. De Santa. - In: CURRENT OPINION IN DRUG DISCOVERY & DEVELOPMENT. - ISSN 1367-6733. - 12:5(2009 Sep), pp. 607-615.

The future therapeutic potential of histone demethylases : a critical analysis

G. Testa
Secondo
;
2009

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.
Animals; Dealkylation; Drug Design; Enzyme Inhibitors; Epigenesis, Genetic; Histone Demethylases; Histone-Lysine N-Methyltransferase; Histones; Humans; Jumonji Domain-Containing Histone Demethylases; Lysine; Methylation; Protein Processing, Post-Translational; Protein Stability; Substrate Specificity; Transcription, Genetic; Drug Discovery
Settore BIO/11 - Biologia Molecolare
Settore BIO/13 - Biologia Applicata
Settore BIO/10 - Biochimica
Settore BIO/14 - Farmacologia
Settore BIO/15 - Biologia Farmaceutica
Settore BIO/18 - Genetica
Settore MED/04 - Patologia Generale
set-2009
Article (author)
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/450831
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