Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers

Dan Fang; Rui Wang; Xinyi Yu; Yuan Tian

doi:10.3791/64293

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Chemistry

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JoVE Journal Chemistry

Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers

构建环状细胞穿透肽以增强生物屏障的穿透力

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10:12 min

September 19, 2022

DOI: 10.3791/64293-v

Dan Fang¹, Rui Wang¹, Xinyi Yu¹, Yuan Tian¹

¹Sichuan Engineering Research Center for Biomimetic Synthesis of Natural Drugs, School of Life Science and Engineering,Southwest Jiaotong University

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该协议描述了具有芳香交联的环细胞穿透肽的合成以及它们跨生物屏障的渗透性的评估。

癌症治疗的一个严重障碍是由于生理障碍，治疗药物对更深的肿瘤细胞的访问有限。因此，强烈希望开发能够治疗生物屏障的新型分子转运蛋白以提高药物递送效率。该程序的目的是合成环状细胞穿透肽以增强细胞间的渗透。

该方法的优点是肽环化可以通过与半胱氨酸和树脂的取代反应轻松实现，而无需任何金属催化剂。与亲水性内酰胺或三唑交联相比，芳香交联的掺入改善了肽的整体疏水性，从而增强了其渗透性。首先，在通风橱中组装手动肽合成装置。

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撤稿第187期细胞穿透肽环肽生物屏障细胞通透性