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首页> 外文期刊>ACS combinatorial science >Comparison of Cell Permeability of Cyclic Peptoids and Linear Peptoids
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Comparison of Cell Permeability of Cyclic Peptoids and Linear Peptoids

机译：循环拟肽和线性拟骨膜细胞渗透性的比较

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摘要

Cyclic peptoids are emerging as an attractive class of peptidomimetics. Compared to their linear counterparts, cyclic peptoids should have increased conformational rigidity and preorganized structures, enabling them to bind more tightly to target proteins without major entropy penalty. Because cyclic peptoids lack the amide protons in their backbones like linear peptoids, it is perceived that cyclic peptoids are seemingly cell permeable as much as linear peptoids. However, no systematic investigation for cell permeability of cyclic peptoids has been reported yet. Here, we, for the first time, demonstrate that cyclic peptoids are far more cell permeable than linear counterparts irrespective of their size and side chains. This study highlights that cyclic peptoids, along with combinatorial library and high -throughput screening technologies, will serve as a rich source of protein binding molecules, particularly targeting intracellular proteins, given their excellent cell permeability in addition to their conformational rigidity and proteolytic stability.
机译：循环拟肽是作为一种吸引人的肽模拟物而涌现。与它们的线性对应物相比，循环拟肽应具有增加的构象刚性和预组织结构，使它们能够更加紧密地粘合到靶蛋白没有主要熵障碍。因为循环拟肽在其骨干中缺乏酰胺质子，如线性拟骨膜，所以它被认为是循环拟肽似乎是细胞的可渗透，如线性拟肽。然而，还没有报道对细胞栓塞的细胞渗透性的系统性研究。在这里，我们首次证明循环拟骨肽比线性对应物不管其尺寸和侧链无关。本研究突出了循环肽，以及组合文库和高杆间筛选技术，将作为其优异的细胞渗透性，除了它们的构象刚性和蛋白水解稳定性之外，作为其优异的细胞渗透性，将作为富含蛋白质结合分子的富含蛋白质结合分子的富源，特别是细胞内蛋白质。

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