Peptide Ribonucleic Acid (PRNA)–Arginine Hybrids. Effects of Arginine Residues Alternatingly Introduced to PRNA Backbone on Aggregation, Cellular Uptake, and Cytotoxicity

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Author(s)

    • Sugai Hiroka
    • Institute of Multidisciplinary Research for Advanced Materials, Tohoku University
    • Yokota Takanori
    • Department of Neurology and Neurological Science, Tokyo Medical and Dental University
    • Wada Takehiko
    • Institute of Multidisciplinary Research for Advanced Materials, Tohoku University
    • Sakamoto Seiji
    • Institute of Multidisciplinary Research for Advanced Materials, Tohoku University
    • Inagaki Masahito
    • Institute of Multidisciplinary Research for Advanced Materials, Tohoku University
    • Araki Yasuyuki
    • Institute of Multidisciplinary Research for Advanced Materials, Tohoku University
    • Ishibashi Satoru
    • Department of Neurology and Neurological Science, Tokyo Medical and Dental University

Abstract

<p>Intracellular delivery is crucial not only in achieving effective oligonucleotide therapeutics but also for a wide variety of therapeutic strategies. In this study to elucidate the effects of the number of incorporated arginine residues on cell membrane permeability, we designed a series of peptide ribonucleic acids (PRNAs) that alternatingly incorporated 4, 8, or 12 arginine residues (<b>P<sub>R</sub>R1</b>-<b>3</b>) in the PRNA backbone for experimental verifications. Indeed, the cellular uptake efficiency and the aggregation properties turned out to be critical functions of the number of incorporated arginine residues. Thus, the optimized <b>P<sub>R</sub>R2</b> that incorporates 8 arginines showed the most efficient cellular uptake ability, much higher than that of octaarginine, without accompanying cytotoxicity or aggregation.</p>

Journal

  • Chemistry Letters

    Chemistry Letters 47(3), 381-384, 2018

    The Chemical Society of Japan

Codes

  • NII Article ID (NAID)
    130006434142
  • Text Lang
    ENG
  • ISSN
    0366-7022
  • Data Source
    J-STAGE 
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