Author/Authors :
Astrid Spannhoff، نويسنده , , Rospita Machmur، نويسنده , , Ralf Heinke، نويسنده , , Patrick Trojer، نويسنده , , Ingo Bauer، نويسنده , , Gerald Brosch، نويسنده , , Roland Schüle، نويسنده , , Wolfgang Hanefeld، نويسنده , , Wolfgang Sippl، نويسنده , , Manfred Jung، نويسنده ,
Abstract :
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 (IC50-PRMT1: 55.4 μM) 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 dependent cancers.
Keywords :
Arginine methyltransferase , PRMT , Virtual screening , Histone methyltransferase , Docking , chromatin
