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Mol Oncol. 2012 Dec;6(6):657-82. doi: 10.1016/j.molonc.2012.09.004. Epub 2012 Oct 6.

Trials with 'epigenetic' drugs: an update.

Author information

1
Dipartimento di Patologia Generale, Seconda Università degli Studi di Napoli, Vico L. de Crecchio 7, Napoli 80138, Italy.

Abstract

Epigenetic inactivation of pivotal genes involved in correct cell growth is a hallmark of human pathologies, in particular cancer. These epigenetic mechanisms, including crosstalk between DNA methylation, histone modifications and non-coding RNAs, affect gene expression and are associated with disease progression. In contrast to genetic mutations, epigenetic changes are potentially reversible. Re-expression of genes epigenetically inactivated can result in the suppression of disease state or sensitization to specific therapies. Small molecules that reverse epigenetic inactivation, so-called epi-drugs, are now undergoing clinical trials. Accordingly, the Food and Drug Administration (FDA) and the European Medicines Agency (EMA) for cancer treatment have approved some of these drugs. Here, we focus on the biological features of epigenetic molecules, analyzing the mechanism(s) of action and their current use in clinical practice.

PMID:
23103179
PMCID:
PMC5528349
DOI:
10.1016/j.molonc.2012.09.004
[Indexed for MEDLINE]
Free PMC Article

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