Peptide stapling techniques based on different macrocyclisation chemistries

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 differen...

Full description

Saved in:
Bibliographic Details
Published in:Chemical Society reviews 2015-01, Vol.44 (1), p.91-12
Main Authors: Lau, Yu Heng, de Andrade, Peterson, Wu, Yuteng, Spring, David R
Format: Article
Language:English
Subjects:
Click Chemistry
Cyclization
Cycloaddition Reaction
Lactams - chemistry
Peptides - chemistry
Photochemical Processes
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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. This review analyses how the choice of macrocyclisation chemistry can influence the biological properties and applications of stapled peptides.
ISSN:0306-0012
1460-4744
DOI:10.1039/c4cs00246f