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Issue 64, 2019
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Macrocyclisation and functionalisation of unprotected peptides via divinyltriazine cysteine stapling

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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.

Graphical abstract: Macrocyclisation and functionalisation of unprotected peptides via divinyltriazine cysteine stapling

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Publication details

The article was received on 01 Jul 2019, accepted on 15 Jul 2019 and first published on 15 Jul 2019


Article type: Communication
DOI: 10.1039/C9CC05042F
Chem. Commun., 2019,55, 9499-9502

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    Macrocyclisation and functionalisation of unprotected peptides via divinyltriazine cysteine stapling

    N. S. Robertson, S. J. Walsh, E. Fowler, M. Yoshida, S. M. Rowe, Y. Wu, H. F. Sore, J. S. Parker and D. R. Spring, Chem. Commun., 2019, 55, 9499
    DOI: 10.1039/C9CC05042F

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