Targeting components of epigenome by small molecules

The diverse epigenetic modifications regulate the gene expression and determine the cellular identity. Pioneering work over the past decades has highlighted that these epigenetic regulations establish normal development but also contribute various diseases. Furthermore, the epigenetic priming events are considered as a key factor for efficient master transcription factor(s) mediated reprogramming process. With the advent of numerous small molecules that target specific enzymes or proteins involved in the epigenetic regulation of gene expression, the utilization of epigenetic targets is emerging as a valuable approach to cancer therapy and cellular reprogramming. Here, we briefly present the basic principles of epigenetic regulations and review the recent application of epigenetic targeting small molecules.