Nature Communications (Jan 2022)
Extendable stapling of unprotected peptides by crosslinking two amines with o-phthalaldehyde
Abstract
Methods for peptide stapling, or covalently linking amino acid residues to create a non-linear structure, mostly rely on cysteine residues, which imposes a significant practical limitation. Here the authors disclose a method to chemoselectively macrocyclize two free-amine-containing residues in mild, peptide-relevant conditions, using a commercially available reagent.