A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases.

ABSTRACT: Protein arginine methyltransferases (PRMTs) play a crucial role in a variety of biological processes. Overexpression of PRMTs has been implicated in various human diseases including cancer. Consequently, selective small-molecule inhibitors of PRMTs have been pursued by both academia and the pharmaceutical industry as chemical tools for testing biological and therapeutic hypotheses. PRMTs are divided into three categories: type I PRMTs which catalyze mono- and asymmetric dimethylation of arginine residues, type II PRMTs which catalyze mono- and symmetric dimethylation of arginine residues, and type III PRMT which catalyzes only monomethylation of arginine residues. Here, we report the discovery of a potent, selective, and cell-active inhibitor of human type I PRMTs, MS023, and characterizat

SUBMITTER: Eram MS 

PROVIDER: S-EPMC4798913 | biostudies-literature | 2016 Mar

REPOSITORIES: biostudies-literature