Jeong Woo-jin, Lim Yong-beom
Translational Research Center for Protein Function Control and Department of Materials Science & Engineering, Yonsei University , Seoul 120-749, Korea.
Bioconjug Chem. 2014 Nov 19;25(11):1996-2003. doi: 10.1021/bc500367z. Epub 2014 Oct 7.
In this study, we developed macrocyclic peptide building blocks that formed self-assembled peptide vesicles with molecular recognition capabilities. Macrocyclic peptides were significantly different from conventional amphiphiles, in that they could self-assemble into vesicles at very high hydrophilic-to-total mass ratios. The flexibility of the hydrophobic self-assembly segment was critical for vesicle formation. The unique features of this peptide vesicle system include a homogeneous size distribution, unusually small size, and robust structural and thermal stability. The peptide vesicles successfully entrapped a hydrophilic model drug, released the payload very slowly, and were internalized by cells in a highly efficient manner. Moreover, the peptide vesicles exhibited molecular recognition capabilities, in that they selectively bound to target RNA through surface-displayed peptides. This study demonstrates that self-assembled peptide vesicles can be used as strong intracellular delivery vehicles that recognize specific biomacromolecular targets.
在本研究中，我们开发了具有分子识别能力的大环肽构建模块，其能形成自组装肽囊泡。大环肽与传统两亲分子显著不同，因为它们能在非常高的亲水质量与总质量比下自组装成囊泡。疏水自组装片段的柔韧性对囊泡形成至关重要。该肽囊泡系统的独特特征包括均一的尺寸分布、异常小的尺寸以及强大的结构和热稳定性。肽囊泡成功包封了一种亲水性模型药物，非常缓慢地释放药物载荷，并能高效地被细胞内化。此外，肽囊泡表现出分子识别能力，即它们通过表面展示的肽选择性地结合靶RNA。本研究表明，自组装肽囊泡可用作识别特定生物大分子靶标的强大细胞内递送载体。
