Small Molecule Inhibitors of Protein Arginine Methyltransferases.
Athens, United States. In Expert Opin Investig Drugs, Feb 2016
Great efforts are seen in screening and designing potent and selective PRMT inhibitors, and a number of micromolar and submicromolar inhibitors have been obtained for key PRMT enzymes such as PRMT1, CARM1, and PRMT5.
HiJAKing the methylosome in myeloproliferative disorders.
Basel, Switzerland. In Cancer Cell, 2011
(2011) demonstrate that these JAK2 mutants, but not wild-type JAK2, directly phosphorylate PRMT5 and inhibit its arginine methyltransferase activity, establishing a link between mutant JAK2 and histone arginine methylation.