Macrocyclisation and functionalisation of unprotected peptides via divinyltriazine cysteine stapling.
Accepted version
Peer-reviewed
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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.
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0304 Medicinal and Biomolecular Chemistry
Journal Title
Chem Commun (Camb)
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Journal ISSN
1359-7345
1364-548X
1364-548X
Volume Title
55
Publisher
Royal Society of Chemistry (RSC)
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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)
Engineering and Physical Sciences Research Council (EP/J016012/1)
Royal Society (WM150022)
Engineering and Physical Sciences Research Council (1800602)
AstraZeneca