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首页> 外文期刊>Journal of Controlled Release: Official Journal of the Controlled Release Society >Intracellular protein delivery with a dimerizable amphiphile for improved complex stability and prolonged protein release in the cytoplasm of adherent cell lines
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Intracellular protein delivery with a dimerizable amphiphile for improved complex stability and prolonged protein release in the cytoplasm of adherent cell lines

机译：具有二聚体性两亲物的细胞内蛋白质递送，可改善复杂的稳定性并延长粘附细胞系细胞质中的蛋白质释放

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摘要

Direct delivery of functionally active proteins into cells represents an emerging strategy for laboratory investigation and therapeutic applications. For this purpose, we developed a novel amphiphile (CholCSper) consisting of cholesterol linked to carboxy-spermine by a cysteine. This amphiphile is dimerizable upon mild oxidation of the thiol to disulfide and it was used in formulation with DOPE to prepare an intracellular protein delivery system. The stabilization of the CholCSper assemblies by chemical conversion of CholCSper into its gemini amphiphile afforded the production of homogeneous assemblies with proteins whose sizes are easier to control. Furthermore, the cholesterol moiety has an effect on the density of the complexes formed with proteins and leads to a prolonged protein release in the cytoplasm of cells exposed to the protein carrier assemblies. (c) 2006 Elsevier B.V All rights reserved.
机译：将功能活性蛋白直接递送至细胞代表了实验室研究和治疗应用的新兴策略。为此，我们开发了一种新型两亲物（CholCSper），它由通过半胱氨酸与羧基精胺连接的胆固醇组成。该两亲物在硫醇轻度氧化为二硫键后可二聚，并与DOPE一起用于配制细胞内蛋白质递送系统。通过将CholCSper化学转化为双亲双亲分子来稳定CholCSper装配体，可以生产出大小均较容易控制的蛋白质均质装配体。此外，胆固醇部分对与蛋白质形成的复合物的密度有影响，并导致暴露于蛋白质载体组件的细胞的细胞质中蛋白质的释放延长。 （c）2006 Elsevier B.V保留所有权利。

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