Open AccessTrials with ‘epigenetic’ drugs: An update
Author(s) -
Nebbioso Angela,
Carafa Vincenzo,
Benedetti Rosaria,
Altucci Lucia
Publication year - 2012
Publication title -
molecular oncology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.332
H-Index - 88
eISSN - 1878-0261
pISSN - 1574-7891
DOI - 10.1016/j.molonc.2012.09.004
Subject(s) - epigenetics , histone , biology , dna methylation , cancer epigenetics , gene , computational biology , disease , genetics , bioinformatics , regulation of gene expression , gene expression , medicine , histone methyltransferase , pathology
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.