Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 54, Issue 38, Pages 11133-11137Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201504884
Keywords
cell-penetrating peptides; disulfide-mediated dimerization; foldamers; gene delivery; transfection
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Funding
- RTRA International Center for Frontier Research in Chemistry
- DGA
- Conseil Regional d'Aquitaine
- CNRS
- Univ. Bordeaux
- Conseil Regional d'Aquitaine [20091102003]
- ANR (TRANSPEP) [ANR-07-PCVI-0018]
- Agence Nationale de la Recherche (ANR) [ANR-07-PCVI-0018] Funding Source: Agence Nationale de la Recherche (ANR)
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Despite significant advances in foldamer chemistry, tailored delivery systems based on foldamer architectures, which provide a high level of control over secondary structure, are curiously rare among non-viral technologies for transporting nucleic acids into cells. A potent pH-responsive, bioreducible cell-penetrating foldamer (CPF) was developed through covalent dimerization of a short (8-mer) amphipathic oligourea sequence bearing histidine-type units. This CPF exhibits a high capacity to assemble with pDNA and mediates efficient delivery of nucleic acids into the cell. Furthermore, it does not adversely affect cellular viability and was shown to compare favorably with a cognate peptide transfection agent based on His-rich sequences.
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