New paper in the Journal of Medicinal Chemistry


Our paper ‘Diamidine Compounds for Selective Inhibition of Protein Arginine Methyltransferase 1’ has just been accepted by the Journal of Medicinal Chemistry. Misregulation of protein arginine methyltransferase enzymes (PRMTs) have been linked to many pathological conditions. In collaboration with Dr. Zheng’s group at UGA we report diamidine compounds as specific inhibitors of PRMT1, the primary type-I PRMT. Docking, molecular dynamics and MM/PBSA analysis together with biochemical assays were conducted to understand the binding modes of these inhibitors and the molecular basis of selective inhibition for PRMT1.