Peptidic Partial Bisubstrates as Inhibitors of the Protein Arginine <i>N</i>‐Methyltransferases

Abstract

Double player: Protein arginine N-methyltransferases (PRMTs) employ a general SN2-like bisubstrate reaction mechanism with the cofactor S-adenosyl-L-methionine (AdoMet) to methylate L-arginine residues in target proteins. In this study, new peptidic partial bisubstrate analogues, bearing a minimal AdoMet fragment (highlighted in yellow) were prepared and evaluated as PRMT inhibitors. Detailed facts of importance to specialist readers are published as ”Supporting Information”. Such documents are peer-reviewed, but not copy-edited or typeset. They are made available as submitted by the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.