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PLoS One. 2013 Jun 11;8(6):e66084. doi: 10.1371/journal.pone.0066084. Print 2013.

A cancer specific cell-penetrating peptide, BR2, for the efficient delivery of an scFv into cancer cells.

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  • 1Department of Biological Sciences, Korea Advanced Institute of Science and Technology, Daejeon, Korea.

Abstract

Cell-penetrating peptides (CPPs) have proven very effective as intracellular delivery vehicles for various therapeutics. However, there are some concerns about non-specific penetration and cytotoxicity of CPPs for effective cancer treatments. Herein, based on the cell-penetrating motif of an anticancer peptide, buforin IIb, we designed several CPP derivatives with cancer cell specificity. Among the derivatives, a 17-amino acid peptide (BR2) was found to have cancer-specificity without toxicity to normal cells. After specifically targeting cancer cells through interaction with gangliosides, BR2 entered cells via lipid-mediated macropinocytosis. Moreover, BR2 showed higher membrane translocation efficiency than the well-known CPP Tat (49-57). The capability of BR2 as a cancer-specific drug carrier was demonstrated by fusion of BR2 to a single-chain variable fragment (scFv) directed toward a mutated K-ras (G12V). BR2-fused scFv induced a higher degree of apoptosis than Tat-fused scFv in K-ras mutated HCT116 cells. These results suggest that the novel cell-penetrating peptide BR2 has great potential as a useful drug delivery carrier with cancer cell specificity.

PMID:
23776609
[PubMed - indexed for MEDLINE]
PMCID:
PMC3679022
Free PMC Article
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