Discovery of a First-in-Class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor
Yudao Shen, Fengling Li, Magdalena M. Szewczyk, Levon Halabelian, Kwang‐Su Park, Irene Chau, Aiping Dong, Hong Zeng, He Chen, Fanye Meng, Dalia Baršytė-Lovejoy, C.H. Arrowsmith, Peter J. Brown, Jing Liu, Masoud Vedadi, Jian Jin
Abstract
(MS168). We provide these valuable chemical tools to the scientific community for further studying PRMT6 physiological and pathophysiological functions.
Topics & Concepts
ChemistryCocrystalCovalent bondEnzyme inhibitorArginineEnzymeMethyltransferaseStereochemistryBiochemistryStructure–activity relationshipActive siteCombinatorial chemistryAmino acidMoleculeIn vitroMethylationOrganic chemistryHydrogen bondGeneCancer-related gene regulation