Ontology highlight
ABSTRACT:
SUBMITTER: Shen Y
PROVIDER: S-EPMC5063716 | biostudies-literature | 2016 Oct
REPOSITORIES: biostudies-literature
Shen Yudao Y Szewczyk Magdalena M MM Eram Mohammad S MS Smil David D Kaniskan H Ümit HÜ de Freitas Renato Ferreira RF Senisterra Guillermo G Li Fengling F Schapira Matthieu M Brown Peter J PJ Arrowsmith Cheryl H CH Barsyte-Lovejoy Dalia D Liu Jing J Vedadi Masoud M Jin Jian J
Journal of medicinal chemistry 20160915 19
Well-characterized selective inhibitors of protein arginine methyltransferases (PRMTs) are invaluable chemical tools for testing biological and therapeutic hypotheses. Based on 4, a fragment-like inhibitor of type I PRMTs, we conducted structure-activity relationship (SAR) studies and explored three regions of this scaffold. The studies led to the discovery of a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6, 17 (MS049). As compared to 4, 17 displayed much improved potency ...[more]