Development of Macrocyclic PRMT5–Adaptor Protein Interaction Inhibitors
Adrian Krzyzanowski, Lea Marie Esser, Anthony Willaume, Renaud Prudent, Christoph Peter, Peter ‘t Hart, Herbert Waldmann
Abstract
= 654 nM) but not with the alternative adaptor protein MEP50. The inhibitor is a promising tool for further biological investigation of this intriguing protein interface.
Topics & Concepts
ChemistryProtein arginine methyltransferase 5Signal transducing adaptor proteinPeptideBiochemistryProtein–protein interactionAmino acidPeptide libraryCombinatorial chemistryPeptide sequenceSignal transductionMethyltransferaseGeneMethylationCancer-related gene regulationChemical Synthesis and Analysis