Inhibitors of Protein Methyltransferases and Demethylases

H. Ümit Kaniskan, Michael L. Martini, Jian Jin
2017 Chemical Reviews  
Post-translational modifications of histones by protein methyltransferases (PMTs) and histone demethylases (KDMs) play an important role in the regulation of gene expression and transcription and are implicated in cancer and many other diseases. Many of these enzymes also target various nonhistone proteins impacting numerous crucial biological pathways. Given their key biological functions and implications in human diseases, there has been a growing interest in assessing these enzymes as
more » ... al therapeutic targets. Consequently, discovering and developing inhibitors of these enzymes has become a very active and fast-growing research area over the past decade. In this review, we cover the discovery, characterization, and biological application of inhibitors of PMTs and KDMs with emphasis on key advancements in the field. We also discuss challenges, opportunities, and future directions in this emerging, exciting research field. CONTENTS 1044 4. Concluding Remarks and Future Directions
doi:10.1021/acs.chemrev.6b00801 pmid:28338320 pmcid:PMC5610952 fatcat:ifwczoutfndpljmpeqkyw2tsxm