期刊
CHEMISTRY-A EUROPEAN JOURNAL
卷 23, 期 13, 页码 3034-3041出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201604946
关键词
cell permeability; conformation analysis; cyclic peptides; cyclopropane; NMR spectroscopy
资金
- Creation of Innovation Centers for Advanced Interdisciplinary Research Areas Program, Ministry of Education, Culture, Sports, Science, and Technology, Japan
- Shionogi Co., Ltd.
- Grants-in-Aid for Scientific Research [15H02495] Funding Source: KAKEN
The conformation of cyclic peptides is closely related to their physicochemical and biological properties, but their rational design to obtain a conformation with the desired properties is difficult. Herein, we present a new strategy by using conformationally restricted cyclopropane tethers (CPTs) to control the conformation and improve the cell permeability of cyclic peptides regardless of the amino acid sequence. Newly designed cis-or trans-CPTs with three-dimensional structural diversity were introduced into a model cyclic peptide, and the relationship between the conformation of the cyclic peptides and their cell permeability was analyzed. Peptides containing a CPT exhibited conformational diversity due to the characteristic steric feature of cyclopropane, among which peptides containing a CPT, cis-NfCf had remarkably higher cell permeability than peptides containing other CPTs-even superior to that of cyclosporine A, a known permeable cyclic peptide.
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