Targeting PRMT3 for therapeutic intervention: underlying mechanisms and translational perspectives

PRMT3, a member of type I protein arginine methyltransferases (PRMTs), can catalyze the formation of asymmetric dimethylarginine (ADMA) and thereby modulates gene expression, cell differentiation, and disease progression. This review covers the PRMT3 structure, biological functions, and its contributions to cancer and other pathologies. We surveyed the emerging landscape of PRMT3 regulation, encompassing pan-inhibitors, selective inhibitors, and degraders, and addressed the hurdles that still impede their clinical translation. Collectively, PRMT3 constitutes a viable epigenetic target, and expanding its pharmacological modality repertoire warrants continued investigation.