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 calixarene, 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 clustering on calixarene macrocycles for improved cell penetration and DNA delivery / V. Bagnacani; V. Franceschi; M. Bassi; M. Lomazzi; G. Donofrio; F. Sansone; A. Casnati; R. Ungaro. - In: NATURE COMMUNICATIONS. - ISSN 2041-1723. - 4(2013). [10.1038/ncomms2721]
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