Recent advances in targeting protein arginine methyltransferase enzymes in cancer therapy

Expert Opinion on Therapeutic Targets
Emily SmithRobert A Baiocchi

Abstract

Exploration in the field of epigenetics has revealed the diverse roles of the protein arginine methyltransferase (PRMT) family of proteins in multiple disease states. These findings have led to the development of specific inhibitors and discovery of several new classes of drugs with potential to treat both benign and malignant conditions. Areas covered: We provide an overview on the role of PRMT enzymes in healthy and malignant cells, highlighting the role of arginine methylation in specific pathways relevant to cancer pathogenesis. Additionally, we describe structure and catalytic activity of PRMT and discuss the mechanisms of action of novel small molecule inhibitors of specific members of the arginine methyltransferase family. Expert opinion: As the field of PRMT biology advances, it's becoming clear that this class of enzymes is highly relevant to maintaining normal physiologic processes as well and disease pathogenesis. We discuss the potential impact of PRMT inhibitors as a broad class of drugs, including the pleiotropic effects, off target effects the need for more detailed PRMT-centric interactomes, and finally, the potential for targeting this class of enzymes in clinical development of experimental therapeutics for ca...Continue Reading

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Citations

Oct 1, 2020·Critical Reviews in Food Science and Nutrition·Davi Vieira Teixeira da SilvaVania Margaret Flosi Paschoalin
Nov 5, 2019·Frontiers in Genetics·Marcelo L RibeiroGaël Roué
Jan 9, 2019·Frontiers in Oncology·Eva De SmedtElke De Bruyne
Jan 15, 2021·Cells·Jean-Paul BryantYeshavanth Kumar Banasavadi-Siddegowda
Feb 19, 2021·Journal of Medicinal Chemistry·Yi ZhangYuanxiang Wang
May 20, 2021·Experimental & Molecular Medicine·Jee Won HwangYong Kee Kim

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