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A biocompatible stapling reaction for in situ generation of constrained peptides

Morewood, Richard; Nitsche, Christoph


Constrained peptides are promising next-generation therapeutics. Peptide stapling is a particularly attractive technique to generate constrained macrocycles with improved biological activity and metabolic stability. We introduce a biocompatible two-component stapling approach based on the reagent 2,6-dicyanopyridine and a pseudo-cysteine amino acid. Stapling can proceed either directly on-resin during solid-phase synthesis or following isolation of the linear peptide. The stapling reaction is...[Show more]

CollectionsANU Research Publications
Date published: 2020-11-04
Type: Journal article
Source: Chemical science
DOI: 10.1039/d0sc05125j
Access Rights: Open Access


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