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Peptide to Peptoid Substitutions Increase Cell Permeability in Cyclic Hexapeptides

机译:肽到类肽取代增加环六肽的细胞通透性

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摘要

The effect of peptide-to-peptoid substitutions on the passive membrane permeability of an N-methylated cyclic hexapeptide is examined. In general, substitutions maintained permeability but increased conformational heterogeneity. Diversification with nonproteinogenic side chains increased permeability up to 3-fold. Additionally, the conformational impact of peptoid substitutions within a beta-turn are explored. Based on these results, the strategic incorporation of peptoid residues into cyclic peptides can maintain or improve cell permeability, while increasing access to diverse side-chain functionality.
机译:研究了肽到类肽取代对N-甲基化环六肽的被动膜通透性的影响。通常,取代保持渗透性,但构象异质性增加。非蛋白侧链的多样化将通透性提高了3倍。另外,探索了β-转角内类肽取代的构象影响。基于这些结果,将类肽残基策略性地并入环状肽中可以维持或改善细胞的通透性,同时增加了获得各种侧链功能的机会。

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