Bioactive Small Molecules for Epigenetic Research

Epigenetic modification of chromatin includes methylation of genomic DNA as well as post-translational modification of chromatin-associated proteins, mainly histones. Cell-permeable small-molecule modulators have become a valuable tool in the investigation of gene and protein functions. The use of small molecules to modulate cellular and in vivo systems is receiving strong interest among researchers in academia as well as pharma. The discovery of small molecule regulators (activators or inhibitors) of epigenetic modification enzymes provides researchers with pharmacological tools with which to investigate the biological consequences of chromatin modifications. The major classes of inhibitors/modulators are classified based on their activity and use.