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

Author

Listed:
  • Valentina Bagnacani

    (Università degli Studi di Parma, Parco Area delle Scienze 17/a)

  • Valentina Franceschi

    (Università degli Studi di Parma, Via del Taglio 6)

  • Michele Bassi

    (Università degli Studi di Parma, Parco Area delle Scienze 17/a)

  • Michela Lomazzi

    (Università degli Studi di Parma, Parco Area delle Scienze 17/a)

  • Gaetano Donofrio

    (Università degli Studi di Parma, Via del Taglio 6)

  • Francesco Sansone

    (Università degli Studi di Parma, Parco Area delle Scienze 17/a)

  • Alessandro Casnati

    (Università degli Studi di Parma, Parco Area delle Scienze 17/a)

  • Rocco Ungaro

    (Università degli Studi di Parma, Parco Area delle Scienze 17/a)

Abstract

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.

Suggested Citation

  • Valentina Bagnacani & Valentina Franceschi & Michele Bassi & Michela Lomazzi & Gaetano Donofrio & Francesco Sansone & Alessandro Casnati & Rocco Ungaro, 2013. "Arginine clustering on calix[4]arene macrocycles for improved cell penetration and DNA delivery," Nature Communications, Nature, vol. 4(1), pages 1-7, June.
  • Handle: RePEc:nat:natcom:v:4:y:2013:i:1:d:10.1038_ncomms2721
    DOI: 10.1038/ncomms2721
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