Arginine clustering on calix[4]arene macrocycles for improved cell penetration and DNA delivery.

Arginine clustering on calix[4]arene macrocycles for improved cell penetration and DNA delivery.
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DOI:
10.1038/ncomms2721
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发表时间:
2013
影响因子:
16.6
通讯作者:
--
中科院分区:
综合性期刊1区
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--
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细胞穿透肽广泛用作分子转运蛋白,用于各种货物(包括蛋白质和核酸)在细胞内的内化。富含精氨酸的肽和与货物共价连接或简单混合的寡聚精氨酸起着特殊的作用。在这里,我们报告细胞渗透剂,其中精氨酸单位聚集在大环支架。代替使用长肽,将四个单个精氨酸单元共价连接到杯[4]芳烃的上边缘或下边缘,保持锥形构象,构建“平行”环状阵列。这些新的大环载体在多种细胞系中显示出高效率的DNA递送和转染。 富含精氨酸的肽充当用于在细胞中内化货物的递送系统。在这里,精氨酸单元在大环支架上以平行阵列聚集产生了一种在DNA递送和转染方面具有高效的载体。
Cell-penetrating peptides are widely used as molecular transporters for the internalization inside cells of various cargo, including proteins and nucleic acids. A special role is played by arginine-rich peptides and oligoarginines covalently linked or simply mixed with the cargo. Here we report cell-penetrating agents in which arginine units are clustered on a macrocyclic scaffold. Instead of using long peptides, four single arginine units were covalently attached to either the upper or lower rim of a calix[4]arene, kept in the cone conformation building a ‘parallel’ cyclic array. These new macrocyclic carriers show high efficiency in DNA delivery and transfection in a variety of cell lines. Arginine-rich peptides act as delivery systems for the internalization of cargoes in cells. Here, the clustering of arginine units in a parallel array on a macrocyclic scaffold produces a vector with high efficiency in DNA delivery and transfection.
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