Inhibitors of Protein Methyltransferases and Demethylases.
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 potential 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.
Departments of Pharmacological Sciences and Oncological Sciences, Icahn School of Medicine at Mount Sinai , New York, New York 10029, United States.
H Ümit
HÜ
Kaniskan
Departments of Pharmacological Sciences and Oncological Sciences, Icahn School of Medicine at Mount Sinai , New York, New York 10029, United States.
Michael L
ML
Martini
Departments of Pharmacological Sciences and Oncological Sciences, Icahn School of Medicine at Mount Sinai , New York, New York 10029, United States.
Jian
0000-0002-2387-3862
J
Jin
D004791:Enzyme Inhibitors / Q000737:chemistry / Q000378:metabolism*; D056466:Histone Demethylases / Q000037:antagonists & inhibitors / Q000145:classification / Q000378:metabolism*; D006801:Humans; D007700:Kinetics; D008239:Lysine / Q000378:metabolism; D011496:Protein Methyltransferases / Q000037:antagonists & inhibitors / Q000145:classification / Q000378:metabolism*; D011499:Protein Processing, Post-Translational; D054852:Small Molecule Libraries / Q000737:chemistry / Q000378:metabolism
D004791:Enzyme Inhibitors; D054852:Small Molecule Libraries; D056466:Histone Demethylases; D011496:Protein Methyltransferases; D008239:Lysine