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Reading Cancer: Chromatin Readers as Druggable Targets for Cancer Treatment

Department of Medical Area, University of Udine, 33100 Udine, Italy
Department of Health Sciences, “Magna Graecia” University of Catanzaro, 88100 Catanzaro, Italy
Medical Genetics Institute, University Hospital of Udine, 33100 Udine, Italy
Authors to whom correspondence should be addressed.
Cancers 2019, 11(1), 61;
Received: 13 December 2018 / Revised: 30 December 2018 / Accepted: 3 January 2019 / Published: 9 January 2019
(This article belongs to the Collection Histone Modification in Cancer)
PDF [1196 KB, uploaded 9 January 2019]


The epigenetic machinery deputed to control histone post-translational modifications is frequently dysregulated in cancer cells. With epigenetics being naturally reversible, it represents a good target for therapies directed to restore normal gene expression. Since the discovery of Bromodomain and Extra Terminal (BET) inhibitors, a great effort has been spent investigating the effects of chromatin readers’ inhibition, specifically the class of proteins assigned to bind acetylated and methylated residues. So far, focused studies have been produced on epigenetic regulation, dissecting a specific class of epigenetic-related proteins or investigating epigenetic therapy in a specific tumor type. In this review, recent steps toward drug discovery on the different classes of chromatin readers have been outlined, highlighting the pros and cons of current therapeutic approaches. View Full-Text
Keywords: chromatin readers; druggable epigenome; small molecule inhibitors chromatin readers; druggable epigenome; small molecule inhibitors

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Mio, C.; Bulotta, S.; Russo, D.; Damante, G. Reading Cancer: Chromatin Readers as Druggable Targets for Cancer Treatment. Cancers 2019, 11, 61.

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