Epigenetics and Novel Therapeutic Approaches

Abstract

Epigenetic changes are targeted to the DNA, as well as chromatin core histones and unlike genetic mutations these changes are reversible, making them attractive targets for therapeutic purposes [1]. Multiple levels of epigenetic regulatory mechanisms provide orchestration of chromatin structure for gene expression in healthy cells; however, result inappropriate silencing or activation of gene expressions, finally leading to various disease states such as cancer [2]. Epigenetic modifications can be a determinant factor to characterize the disease states, and detailed profiling of these modifications may allow predictions of disease outcome or therapeutic strategies. Epigenetic therapy can offer promising tools to restore/reverse changes. Interestingly, several epigenetic inhibitors such as DNA methyltransferase inhibitors (DNMTis), and histone deacetylase inhibitors (HDACis) approved by the US Food and Drug Administration (FDA) are in clinics for the treatment of various hematological malignancies. Potential epigenetic modifications, such as DNA methylation, covalent histone modifications, such as histone acetylation/deacetylation, histone methylation/demethylation, histone phosphorylation, non-covalent mechanisms, such as incorporation of histone variants, nucleosome remodeling and positioning, microRNAs (miRNAs) expression are important targets for therapeutic purposes [2,3]. How these effectors interact to each other to affect gene expression and cause disease is the active field of study in epigenetics.