Leading approaches in synthetic epigenetics for novel therapeutic strategies

• Published in: Current opinion in chemical biology Vol. 46; pp. 10 - 17
• Main Authors: Yamatsugu, Kenzo, Kawashima, Shigehiro A, Kanai, Motomu
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01-10-2018
• ISSN: 1367-5931; 1879-0402
• DOI: 10.1016/j.cbpa.2018.03.011

In recent years, our knowledge of the epigenetic functions regulated by post-translational modifications (PTMs) of histones, and their role in various diseases, has expanded rapidly, opening the way to novel therapeutic strategies that treat epigenetic abnormalities. Many of the current approaches have been focusing on the chemical inhibition of histone-modifying enzymes to modulate histone PTM states for attaining therapeutic effects. However, recent developments in chemistry and molecular biology have contributed to the emergence of new methods that introduce histone PTMs entirely through artificial means, without reliance on endogenous enzymes. In this review article, we summarize several state-of-the-art approaches for the introduction of synthetic epigenetic modifications in cells, and discuss both their therapeutic potential and the possible challenges in developing novel therapeutic strategies utilizing them.