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首页> 外文期刊>Chemistry: A European journal >Highly Conformationally Restricted Cyclopropane Tethers with Three-Dimensional Structural Diversity Drastically Enhance the Cell Permeability of Cyclic Peptides
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Highly Conformationally Restricted Cyclopropane Tethers with Three-Dimensional Structural Diversity Drastically Enhance the Cell Permeability of Cyclic Peptides

机译：具有三维结构多样性的高度兼容性限制的环丙烷，大大提高了环肽的细胞渗透性

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摘要

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.
机译：环状肽的构象与其物理化学和生物学特性密切相关，但它们的合理设计难以获得具有所需特性的构象。 在此，我们通过使用构象限制的环丙烷TETH（CPT）来控制一种新的策略来控制锥形肽的构象并改善环肽的细胞渗透性，而不管氨基酸序列。 将具有三维结构分集的新设计的CIS-或反式CPT被引入模型循环肽，分析了环状肽的构象与其细胞渗透性之间的关系。 由于环丙烷的特征空间特征，含有CPT的肽表现出构象的多样性，其中含有CPT的肽，CIS-NFCF具有比含有其他CPTS的肽更高的细胞渗透性 - 甚至优于环孢菌素A，一种已知的可渗透环肽 。

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