Biochimica et Biophysica Acta (BBA) - Gene Regulatory Mechanisms | VOL. 1865

Chemical biology and pharmacology of histone lysine methylation inhibitors

Publication Date Aug 1, 2022


Histone lysine methylation is a post-translational modification that plays a key role in the epigenetic regulation of a broad spectrum of biological processes. Moreover, the dysregulation of histone lysine methyltransferases (KMTs) has been implicated in the pathogenesis of several diseases particularly cancer. Due to their pathobiological importance, KMTs have garnered immense attention over the last decade as attractive therapeutic targets. These endeavors have culminated in tens of chemical probes that have been used to interrogate many aspects of histone lysine methylation. Besides, over a dozen inhibitors have been advanced to clinical trials, including the EZH2 inhibitor tazemetostat approved for the treatment of follicular lymphoma and advanced epithelioid sarcoma. In this Review, we highlight the chemical biology and pharmacology of KMT inhibitors and targeted protein degraders focusing on the clinical development of EZH1/2, DOT1L, Menin-MLL, and WDR5-MLL inhibitors. We also briefly discuss the pharmacologic targeting of other KMTs.


Advanced Epithelioid Sarcoma Histone Lysine Methylation Pathobiological Importance Histone Lysine Post-translational Modification Treatment Of Sarcoma Advanced Sarcoma Treatment Of Lymphoma Chemical Biology Pathogenesis Of Diseases

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