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Title 

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

 

효율적 scFv 암세포 전달을 위한 암세포 특이적 세포침투 펩타이드, BR2

Authors 

K J LimBong Hyun SungJ R ShinY W LeeD J KimK S YangS C Kim

Publisher 

Public Library of Science

Issue Date 

2013

Citation 

Plos One, vol. 8, no. 6, pp. e66084-e66084

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.

ISSN 

1932-6203

Link 

http://dx.doi.org/10.1371/journal.pone.0066084

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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