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A Class Of Cationic Triblock Amphiphilic Oligopeptides As Efficient Gene-delivery Vectors

机译:一类阳离子三嵌段两亲寡肽作为有效的基因传递载体。

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Cationic oligopeptides fabricated from natural amino acids have been widely explored as nonviral vectors for gene delivery, due to their biodegradability, greater biocompatibility, ease of production, and compositional control compared to polymeric carriers. Existing oligopeptide designs consist mainly of ⅰ) cationic arginine, either as a homopolymer or conjugated to a hydrophobic compound, or ⅱ) cationic lysine, which is either functionalized with endosomolytic agents, for example pH-sensitive histidine moieties, melittin peptide, adenovirus, and the influenza virus hemagglutinin subunit HA-2, or incorporated with several cysteine residues and one tryptophan residue, to improve transfection ability. Here, we design novel short triblock amphiphilic oligopeptides based on pure amino acids, which combine all the above features and can also form micellar particles in an aqueous medium. We then systematically demonstrate that the functionality of each block is essential for achieving high transfection efficiency at levels comparable or even superior to those of polyethylenimine (PEI).
机译:与聚合载体相比,由天然氨基酸制成的阳离子寡肽由于具有生物可降解性,更大的生物相容性,易于生产和成分控制等优点,已被广泛用作基因传递的非病毒载体。现有的寡肽设计主要由以下组成:ⅰ)作为均聚物或与疏水化合物偶联的阳离子精氨酸,或ⅱ)内溶酶(例如pH敏感的组氨酸部分,蜂毒肽,腺病毒和流感病毒血凝素亚基HA-2,或掺入几个半胱氨酸残基和一个色氨酸残基,以提高转染能力。在这里,我们设计了基于纯氨基酸的新型短三嵌段两亲性寡肽,它们结合了上述所有特征,并且还可以在水性介质中形成胶束颗粒。然后,我们系统地证明,每个嵌段的功能对于以与聚乙烯亚胺(PEI)相当甚至更高的水平实现高转染效率至关重要。

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