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Reading Cancer: Chromatin Readers as Druggable Targets for Cancer Treatment.

ABSTRACT: 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.

SUBMITTER: Mio C

PROVIDER: S-EPMC6356452 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature

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Reading Cancer: Chromatin Readers as Druggable Targets for Cancer Treatment.

Mio Catia C Bulotta Stefania S Russo Diego D Damante Giuseppe G

Cancers 20190109 1

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 ...[more]

PMID: 30634442

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