The regulation, functions and clinical relevance of arginine methylation

Methylation of arginine residues by protein arginine methyltransferases (PRMTs) is involved in the regulation of fundamental cellular processes, including transcription, RNA processing, signal transduction cascades, the DNA damage response and liquid–liquid phase separation. Recent studies have provided considerable advances in the development of experimental tools and the identification of clinically relevant PRMT inhibitors. In this review, we discuss the regulation of PRMTs, their various cellular roles and the clinical relevance of PRMT inhibitors for the therapy of neurodegenerative diseases and cancer. The methylation of arginine residues regulates gene expression, DNA repair, growth factor signalling and liquid–liquid phase separation. Targeting this modification can thus be therapeutically relevant and inhibitors of arginine methylation are being tested in clinical trials, especially for neurodegenerative diseases and cancer.