Peptide stapling techniques based on different macrocyclisation chemistries

被引:450
作者
Lau, Yu Heng [1 ]
De Andrade, Peterson [1 ]
Wu, Yuteng [1 ]
Spring, David R. [1 ]
机构
[1] Univ Cambridge, Univ Chem Lab, Cambridge CB2 1EW, England
基金
英国工程与自然科学研究理事会; 英国医学研究理事会; 英国惠康基金; 英国生物技术与生命科学研究理事会;
关键词
CROSS-LINKING; SIDE-CHAIN; EFFICIENT SYNTHESIS; HELICAL STRUCTURES; ALPHA-HELICES; STABILIZATION; DERIVATIVES; INHIBITOR; STABILITY; ANALOGS;
D O I
10.1039/c4cs00246f
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
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.
引用
收藏
页码:91 / 102
页数:12
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