1226853-40-2Relevant academic research and scientific papers
Preparation of novel alkylated arginine derivatives suitable for click-cycloaddition chemistry and their incorporation into pseudosubstrate- and bisubstrate-based kinase inhibitors
Van Ameijde, Jeroen,Poot, Alex J.,Van Wandelen, Loek T. M.,Wammes, Angelique E. M.,Ruijtenbeek, Rob,Rijkers, Dirk T. S.,Liskamp, Rob M. J.
, p. 1629 - 1639 (2010)
Efficient strategies for the introduction of arginine residues featuring acetylene or azide moieties in their side chains are described. The substituents are introduced in a way that maintains the basicity of the guanidine moiety. The methodology can be used e.g. for non-invasive labeling of arginine-containing peptides. Its applicability is demonstrated by the introduction of 'click' handles into a Protein Kinase C (PKC) pseudosubstrate peptide, and the subsequent preparation and evaluation of a novel bisubstrate-based inhibitor based on such a peptide.
