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Enhanced Intracellular Delivery Using Arginine-Rich Peptides by the Addition of Penetration Accelerating Sequences (Pas)

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


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)

Topics: arginine-rich peptide, cell penetrating peptide, intracellular delivery, p53 C-terminal segment, retro-inverso peptide
Publisher: 'Elsevier BV'
Year: 2009
DOI identifier: 10.1016/j.jconrel.2009.05.019
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