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Genet Epigenet. 2014 May 27;6:9-19. doi: 10.4137/GEG.S12270. eCollection 2014.

Use of epigenetic drugs in disease: an overview.

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Cancer Center, Department of Medicine, Boston University School of Medicine, Boston, MA, USA.


Epigenetic changes such as DNA methylation and histone methylation and acetylation alter gene expression at the level of transcription by upregulating, downregulating, or silencing genes completely. Dysregulation of epigenetic events can be pathological, leading to cardiovascular disease, neurological disorders, metabolic disorders, and cancer development. Therefore, identifying drugs that inhibit these epigenetic changes are of great clinical interest. In this review, we summarize the epigenetic events associated with different disorders and diseases including cardiovascular, neurological, and metabolic disorders, and cancer. Knowledge of the specific epigenetic changes associated with these types of diseases facilitates the development of specific inhibitors, which can be used as epigenetic drugs. In this review, we discuss the major classes of epigenetic drugs currently in use, such as DNA methylation inhibiting drugs, bromodomain inhibitors, histone acetyl transferase inhibitors, histone deacetylase inhibitors, protein methyltransferase inhibitors, and histone methylation inhibitors and their role in reversing epigenetic changes and treating disease.


DNA methylation; cancer; cardiovascular; drugs; epigenetics; gene expression; gene silencing; histone acetylation; histone methylation; metabolic; neurological; tumor suppressor genes

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