A novel arginine methyltransferase inhibitor with cellular activity.

  title={A novel arginine methyltransferase inhibitor with cellular activity.},
  author={Astrid Spannhoff and Rospita Machmur and Ralf Heinke and Patrick Trojer and Ingo Bauer and Gerald Brosch and Roland Sch{\"u}le and Wolfgang Hanefeld and Wolfgang Sippl and Manfred Jung},
  journal={Bioorganic & medicinal chemistry letters},
  volume={17 15},
Via virtual screening we identified a thioglycolic amide as an arginine methyltransferase (PRMT) inhibitor and tested it and related compounds against the fungal PRMT RmtA and human PRMT1. Compound RM65 was the most potent druglike inhibitor (IC(50)-PRMT1: 55.4 microM) and showed histone hypomethylation in HepG2 cells. Docking studies proposed binding at the substrate and SAM cofactor binding pocket. It may serve as a lead for further PRMT inhibitors useful for the treatment for hormone… CONTINUE READING