Chemical Control System of Epigenetics.

Epigenetics represents the inheritable changes to the chemical control system governing the gene expression with no ensuing changes to the underlying DNA sequence. Environment-mediated modification of the natural epigenetic interactions can perturb the cellular homeostasis and drive cells to a diseased state by switching therapeutically essential genes ON and OFF. Contemporary bioinformatics tools have revealed the structural chemical modifications of the epigenetic enzymes associated with several complex diseases, including cancers, immune disorders, and neurodegenerative disorders at the fundamental level. The amenable nature of the epigenetic enzymes to chemical modifications aided the screening and identification of synthetic small-molecule inhibitors. Continuing the current steady progress in the development of these small-molecule inhibitors as 'epi-drugs' in preclinical studies requires further advances to enable existing clinical barriers to be overcome. Recently, an epigenetic modifier complemented with selective DNA-binding small molecules was shown to function as an artificial biomimetic epigenetic code. Herein, we summarize the chemical aspects of the natural epigenetic control system and detail the recent advances in the synthetic strategies to mimic the genetic and epigenetic control system.