Chapter 11: Inhibiting Arginine Methylation
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Published:30 Sep 2024
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Special Collection: 2024 eBook CollectionSeries: Drug Discovery
G. Sbardella and M. T. Bedford, in Epigenetic Drug Discovery, ed. H. M. Chan and C. Arrowsmith, Royal Society of Chemistry, 2024, vol. 83, ch. 11, pp. 343-382.
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The misregulation of protein arginine methyltransferases (PRMTs) has been implicated in cancer and other diseases. There are nine PRMTs and small molecule inhibitors have been developed that selectively target most of the family members. These inhibitors have progressed from the chemical probe stage, where they have played a role in dissecting out PRMT-related mechanistic pathways and have been used in pre-clinical in vivo settings, to the development of drugs that are currently being leveraged in clinical trials. Here we will discuss the evolution of this field.