Oncoepigenomics: Making histone lysine methylation count

Increasing studies show that methylation of histone lysine residues is implicated in the development and progression of varying disease states such as schizophrenia, diabetes, and multiple human cancers. Targeting the specific enzymes responsible for these processes has fueled global investigation into the understanding and correction of epigenetic pathology. This review aims to assemble a timely account of the current progress against chromatin-modifying histone lysine methyltransferases (KMTs) and demethylases (KDMs) to inform ongoing and future efforts into this promising field. In particular, we report on their role in tumor growth and progression and the development of small molecules that modulate these enzymes.

Graphical abstractThis review reports on the state of histone lysine methyltransferases and demethylases in tumor growth and the development of small molecules that modulate these enzymes.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Epigenetic enzymes are therapeutic targets for cancer drug development. ► Histone lysine methyltransferase and demethylase enzymes are implicated in multiple cancer types. ► Several classes of natural products and small molecules have been developed to target these enzymes.