Cysteine-Free Peptide and Glycopeptide Ligation by Direct Aminolysis

摘要

Native chemical ligation (NCL) is an extremely useful technique for the synthesis of peptide and protein targets. The method, which relies on the chemoselective condensation of a C-terminal peptide thioester with a peptide containing an N-terminal cysteine residue to afford a native peptide bond, has been implemented successfully in the total synthesis of hundreds of proteins to date. Furthermore, NCL has also been applied effectively to the synthesis of glycoproteins. Although NCL has proved to be an extremely powerful technique, certain limitations still exist.