![2-morpholino-2-[2-(trifluoromethyl)pyrimidin-5-yl]ethanamine structure](https://static.chemtradehub.com/structs/119/1192570-20-9-2810.webp "2-morpholino-2-[2-(trifluoromethyl)pyrimidin-5-yl]ethanamine structure")
2-morpholino-2-[2-(trifluoromethyl)pyrimidin-5-yl]ethanamine
CAS Number:
1192570-20-9
Molecular Formula:
C11H15F3N4O
Cyclisation strategies for stabilising peptides with irregular conformations
Literature Information
Publication Date
2021-04-28
DOI
10.1039/D1MD00098E
Impact Factor
0
Authors
Quynh Ngoc Vu, Reginald Young, Haritha Krishna Sudhakar, Tianyi Gao, Tiancheng Huang, Yaw Sing Tan, Yu Heng Lau
View Original
Abstract
Cyclisation is a common synthetic strategy for enhancing the therapeutic potential of peptide-based molecules. While there are extensive studies on peptide cyclisation for reinforcing regular secondary structures such as α-helices and β-sheets, there are remarkably few reports of cyclising peptides which adopt irregular conformations in their bioactive target-bound state. In this review, we highlight examples where cyclisation techniques have been successful in stabilising irregular conformations, then discuss how the design of cyclic constraints for irregularly structured peptides can be informed by existing β-strand stabilisation approaches, new computational design techniques, and structural principles extracted from cyclic peptide library screening hits. Through this analysis, we demonstrate how existing peptide cyclisation techniques can be adapted to address the synthetic design challenge of stabilising irregularly structured binding motifs.
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