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Macrocyclisation and functionalisation of unprotected peptides via divinyltriazine cysteine stapling.

Accepted version
Peer-reviewed

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Type

Article

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Authors

Robertson, Naomi S 
Walsh, Stephen J 
Fowler, Elaine 
Yoshida, Masao 
Rowe, Sam M 

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.

Description

Keywords

0304 Medicinal and Biomolecular Chemistry

Journal Title

Chem Commun (Camb)

Conference Name

Journal ISSN

1359-7345
1364-548X

Volume Title

55

Publisher

Royal Society of Chemistry (RSC)

Rights

All rights reserved
Sponsorship
Engineering and Physical Sciences Research Council (EP/P020291/1)
Engineering and Physical Sciences Research Council (EP/J016012/1)
Royal Society (WM150022)
Engineering and Physical Sciences Research Council (1800602)
AstraZeneca