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Issue 1, 2015
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Peptide stapling techniques based on different macrocyclisation chemistries

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Abstract

Peptide stapling is a strategy for constraining short peptides typically in an alpha-helical conformation. Stapling is carried out by covalently linking the side-chains of two amino acids, thereby forming a peptide macrocycle. There is an expanding repertoire of stapling techniques based on different macrocyclisation chemistries. In this tutorial review, we categorise and analyse key examples of peptide stapling in terms of their synthesis and applicability to biological systems.

Graphical abstract: Peptide stapling techniques based on different macrocyclisation chemistries

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Article information


Submitted
17 Jul 2014
First published
08 Sep 2014

Chem. Soc. Rev., 2015,44, 91-102
Article type
Tutorial Review
Author version available

Peptide stapling techniques based on different macrocyclisation chemistries

Y. H. Lau, P. de Andrade, Y. Wu and D. R. Spring, Chem. Soc. Rev., 2015, 44, 91
DOI: 10.1039/C4CS00246F

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