Peptide ribonucleic acid (PRNA)Arginine Hybrids. Effects of arginine residues alternatingly introduced to PRNA backbone on aggregation, cellular uptake, and cytotoxicity

Hiroka Sugai, Ikuhiko Nakase, Seiji Sakamoto, Akihiro Nishio, Masahito Inagaki, Masaki Nishijima, Asako Yamayoshi, Yasuyuki Araki, Satoru Ishibashi, Takanori Yokota, Yoshihisa Inoue, Takehiko Wada

Research output: Contribution to journalArticlepeer-review

1 Citation (Scopus)

Abstract

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 (PRR1-3) 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 PRR2 that incorporates 8 arginines showed the most efficient cellular uptake ability, much higher than that of octaarginine, without accompanying cytotoxicity or aggregation.

Original languageEnglish
Pages (from-to)381-384
Number of pages4
JournalChemistry Letters
Volume47
Issue number3
DOIs
Publication statusPublished - 2018 Jan 1

Keywords

  • Cell membrane permeability
  • Oligoarginine
  • Peptide ribonucleic acid (PRNA)

ASJC Scopus subject areas

  • Chemistry(all)

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