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. 2019 Aug 7;55(64):9499-9502.
doi: 10.1039/c9cc05042f.

Macrocyclisation and functionalisation of unprotected peptides via divinyltriazine cysteine stapling

Naomi S Robertson  1 , Stephen J Walsh, Elaine Fowler, Masao Yoshida, Sam M Rowe, Yuteng Wu, Hannah F Sore, Jeremy S Parker, David R Spring
Affiliations

Macrocyclisation and functionalisation of unprotected peptides via divinyltriazine cysteine stapling

Naomi S Robertson et al. Chem Commun (Camb). .

Abstract

We report a novel divinyltriazine linker for the stapling of two cysteine residues to form macrocyclic peptides from their unprotected linear counterparts. The stapling reaction occurred rapidly under mild conditions on a range of unprotected peptide sequences. The resulting constrained peptides displayed greater stability in a serum stability assay when compared to their linear counterparts.

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