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Targeting the histone orthography of cancer: drugs for writers, erasers and readers.

ABSTRACT: Gene expression is dynamically controlled by epigenetics through post-translational modifications of histones, chromatin-associated proteins and DNA itself. All these elements are required for the maintenance of chromatin structure and cell identity in the context of a normal cellular phenotype. Disruption of epigenetic regulation is a common event in human cancer. Here, we review the key protein families that control epigenetic signalling through writing, erasing or reading specific post-translational modifications. By exploiting the leading role of epigenetics in tumour development and the reversibility of epigenetic modifications, promising novel epigenetic-based therapies are being developed. In this article, we highlight the emerging low MW inhibitors targeting each class of chromatin-associated protein, their current use in preclinical and clinical trials and the likelihood of their being approved in the near future.

SUBMITTER: Simo-Riudalbas L

PROVIDER: S-EPMC4439870 | biostudies-literature | 2015 Jun

REPOSITORIES: biostudies-literature

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Targeting the histone orthography of cancer: drugs for writers, erasers and readers.

Simó-Riudalbas Laia L Esteller Manel M

British journal of pharmacology 20140905 11

Gene expression is dynamically controlled by epigenetics through post-translational modifications of histones, chromatin-associated proteins and DNA itself. All these elements are required for the maintenance of chromatin structure and cell identity in the context of a normal cellular phenotype. Disruption of epigenetic regulation is a common event in human cancer. Here, we review the key protein families that control epigenetic signalling through writing, erasing or reading specific post-transl ...[more]

PMID: 25039449

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