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• W2169455898 abstract "Developing efficient cellular delivery vectors is crucial for designing novel therapeutic agents to enhance their plasma membrane permeability and metabolic stability in cells. Previously, we engineered cell penetrating peptide vectors named as lipo-oligoarginine peptides (LOAPs) by conjugating a proper combination of fatty acid and oligoarginine that translocated into cell easily without adverse effect on cell viability. In the present study, we report a systemic evaluation of cellular uptake and metabolic stability of LOAPs in Jurkat cells by introducing different combination of D-Arg residues in the peptide backbone. The cellular uptake and intracellular fate, cell viability, and metabolic stability and proteolytic degradation patterns of various LOAPs consisted of different combination of L- and D-Arg sequences were confirmed by flow cytometry, cytotoxicity assay, and analytical RP-HPLC with MALDI-TOF mass. All investigated LOAPs penetrated the cell efficiently with low cellular toxicity. The LOAPs having D-Arg residues at their N-termini seemed to have better metabolic stability than the LOAPs having C-terminal D-Arg residues. The metabolic degradation patterns were similar among all investigated LOAPs. The major hydrolytic site was between lauroyl group and β-Ala residue. Without the lipid chain, the oligoarginine peptide was pumped out ofcells easily. The results presented in this study suggest that structurally modified LOAPs could be used as a novel CPP design toward improved therapeutic application." @default.
• W2169455898 created "2016-06-24" @default.
• W2169455898 creator A5011709742 @default.
• W2169455898 creator A5086964876 @default.
• W2169455898 date "2011-01-01" @default.
• W2169455898 modified "2023-10-10" @default.
• W2169455898 title "Enhanced cellular uptake and metabolic stability of lipo-oligoarginine peptides" @default.
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• W2169455898 doi "https://doi.org/10.1002/bip.21681" @default.
• W2169455898 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3261498" @default.
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• W2169455898 hasPublicationYear "2011" @default.
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