Enhanced intracellular delivery using arginine-rich peptides by the addition of penetration accelerating sequences (Pas)

Kentaro Takayama, Ikuhiko Nakase, Hiroyuki Michiue, Toshihide Takeuchi, Kazuhito Tomizawa, Hideki Matsui, Shiroh Futaki

Research output: Contribution to journalArticle

71 Citations (Scopus)

Abstract

Cell penetrating peptides (CPPs), including arginine-rich peptides, are attractive tools for the intracellular delivery of various bioactive molecules with a low membrane permeability. We showed that the accelerated intracellular delivery of arginine-rich peptides was achieved by the addition of a short peptide segment (penetration accelerating sequence, Pas) to arginine-rich CPPs. The cytosolic release of the Pas-attached arginine-rich CPPs was observed within 5 min after the treatment of the cells with the peptides even in the presence of serum. Effectiveness of the Pas segment in the intracellular delivery of bioactive peptides using arginine-rich CPPs was exemplified through the enhanced growth inhibition activity of the malignant glioma cells by a retro-inverso peptide derived from the p53 C-terminal 22-amino-acid segment (positions 361-382).

Original languageEnglish
Pages (from-to)128-133
Number of pages6
JournalJournal of Controlled Release
Volume138
Issue number2
DOIs
Publication statusPublished - Sep 1 2009

Keywords

  • Arginine-rich peptide
  • Cell penetrating peptide
  • Intracellular delivery
  • Retro-inverso peptide
  • p53 C-terminal segment

ASJC Scopus subject areas

  • Pharmaceutical Science

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