Novel cell penetrating peptides with multiple motifs composed of RGD and its analogs

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Title
Novel cell penetrating peptides with multiple motifs composed of RGD and its analogs
Author(s)
A A Mokhtarieh; Semi Kim; Yunhee Lee; Bong Hyun Chung; Myung Kyu Lee
Bibliographic Citation
Biochemical and Biophysical Research Communications, vol. 432, no. 2, pp. 359-364
Publication Year
2013
Abstract
Cell penetrating peptides (CPPs) have been used to transport macromolecules into cells. Most CPPs have properties such as a strong polycationic charge, amphipathic basic, and hydrophobicity. In this study, we designed the peptides with multiple motifs composed of RGD and its analogs to induce integrin-mediated endocytosis as well as endosomal escape by forming an amphipathic helix in acidic endosomes. These peptides were proved less toxic to animal cells than those without acidic residues. Unexpectedly, peptide conjugated liposomes could penetrate into cells regardless of integrins. The replacement of all aspartic acids by glutamic acids did not prevent the peptide-mediated liposome uptake, and the higher basic and leucine contents enhanced the gene silencing activity of siRNA encapsulated in the liposomes. The peptide is considered to be a new type of CPP which can be used for drug delivery.
Keyword
Cell penetrating peptide (CPP)CPP-mediated liposome uptakeGene silencingPeptide cytotoxicityRGD motif
ISSN
0006-291X
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bbrc.2013.01.096
Type
Article
Appears in Collections:
Division of Biomedical Research > Microbiome Convergence Research Center > 1. Journal Articles
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