University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK.
Chem Soc Rev. 2015 Jan 7;44(1):91-102. doi: 10.1039/c4cs00246f. Epub 2014 Sep 8.
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.
肽键是一种约束短肽的策略，通常使其形成α-螺旋构象。通过将两个氨基酸的侧链共价连接，从而形成肽大环。基于不同的环化化学原理，有越来越多的订书钉技术。在本教程综述中，我们根据其合成和在生物系统中的适用性对肽键的关键实例进行分类和分析。
