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pH-responsive PepFect cell-penetrating peptides
Stockholm University, Faculty of Science, Department of Neurochemistry.
Stockholm University, Faculty of Science, Department of Neurochemistry.
Stockholm University, Faculty of Science, Department of Neurochemistry. University of Tartu, Estonia.
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Number of Authors: 5
2016 (English)In: International Journal of Pharmaceutics, ISSN 0378-5173, E-ISSN 1873-3476, Vol. 501, no 1-2, 32-38 p.Article in journal (Refereed) Published
Abstract [en]

A series of cell-penetrating PepFect peptide analogues was developed by substitutions of the galanin-derived N-terminal sequence. Histidine modifications were incorporated in order to make the peptides pH-responsive. The peptides were all able to form non-covalent complexes with an oligonucleotide cargo by co-incubation in buffer. The complexes were characterized by dynamic light scattering and circular dichroism, and an assay to evaluate the peptide-cargo affinity was developed. Cellular bioactivity was studied in HeLa cells using a luciferase-based splice correction assay. In addition, the membrane interactions of the peptides in large unilammelar vesicles was studied using a calcein leakage assay. The effects of substitutions were found to be dependent of the non-modified, C-terminal sequence of the peptides; for analogues of PepFect 3 we observed an increase in membrane activity and bioactivity for histidine-containing analogues, whereas the same modifications introduced to PepFect 14 lead to a decreased bioactivity. Peptides modified with a leucine/histidine sequence were found to be pH responsive, complexes formed from these peptides were small at pH 7 and grew under acidic conditions. The most promising of the novel PepFect 3 analogues, PepFect 132 has a significantly higher bioactivity and membrane activity than the parent peptide PepFect 3.

Place, publisher, year, edition, pages
2016. Vol. 501, no 1-2, 32-38 p.
Keyword [en]
Cell-penetrating peptide, Oligonucleotide delivery, Calcein leakage, PepFect, Cellular uptake, pH-responsive
National Category
Chemical Sciences Pharmaceutical Sciences
Research subject
Neurochemistry with Molecular Neurobiology
URN: urn:nbn:se:su:diva-128503DOI: 10.1016/j.ijpharm.2016.01.055ISI: 000370845300004PubMedID: 26821060OAI: diva2:918409
Available from: 2016-04-11 Created: 2016-03-30 Last updated: 2016-09-16Bibliographically approved
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Regberg, JakobVasconcelos, LuisLangel, ÜloHällbrink, Mattias
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