The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.
Proton Sponge Trick for pH-Sensitive Disassembly of Polyethylenimine-Based siRNA Delivery Systems
Abstract
Small interfering RNAs offer novel opportunities to inhibit gene expression in a highly selective and efficient manner but depend on cytosolic translocation with synthetic delivery systems. The polyethylenimine (PEI) is widely used for plasmid DNA transfection. However, the water-soluble PEI does not form siRNA polyplexes stable enough in extracellular media for effective delivery. We previously showed that rendering PEI insoluble in physiological media, without modifying drastically its overall cationic charge density, by simple conjugation with natural hydrophobic alpha-amino acids, can lead to effective siRNA delivery in mammalian cells. In here, we comprehensively investigated the mechanism behind the excellent efficacy of the leading PEIY vector. Our data revealed that the underlining proton sponge property is key to the effectiveness of the tyrosine-polyethylenimine conjugate as it may allow both endosomal rupture and siRNA liberation via an optimal pH-sensitive dissolution of the PEIY self-aggregates. Altogether, these results should facilitate the development of novel and more sophisticated siRNA delivery systems.
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Cites
RNAi-mediated gene silencing in non-human primates
Zimmermann, T. S., Lee, A. C. H., Akinc, A., Bramlage, B., Bumcrot, D., Fedoruk, M. N., Harborth, J., Heyes, J. A., Jeffs, L. B., John, M., et al. (2006) · Nature · doi:10.1038/nature04688 · Cited by 1,357
Cited by
Nucleic Acid Therapeutics Using Polyplexes: A Journey of 50 Years (and Beyond)
Lächelt, U., & Wagner, E. (2015) · Chemical Reviews · doi:10.1021/cr5006793 · Cited by 600
Chen, C., Law, W., Aalinkeel, R., Nair, B., Kopwitthaya, A., Mahajan, S. D., Reynolds, J. L., Zou, J., Schwartz, S. A., Prasad, P. N., et al. (2012) · Advanced Healthcare Materials · doi:10.1002/adhm.201200094 · Cited by 82
Naik, S., Shreya, A. B., Raychaudhuri, R., Pandey, A., Lewis, S. A., Hazarika, M., Bhandary, S. V., Rao, B. S. S., & Mutalik, S. (2021) · Life Sciences · doi:10.1016/j.lfs.2020.118712 · Cited by 33
Metadata
- Authors
- Creusat, G., Rinaldi, A.-S., Weiss, E., Elbaghdadi, R., Remy, J.-S., Mulherkar, R., & Zuber, G.
- Venue
- Bioconjugate Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2010-04-16
- Volume
- 21
- Issue
- 5
- Pages
- 994-1002
- ISSN
- 1043-1802 (ISSN-L)
- 1520-4812
- OpenAlex
- W2079424629
- Cited by
- 170
- References
- 1
- FWCI
- 5.08
- Type
- journal article
- Language
- en
- Open access
- closed
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- Creusat, G., Rinaldi, A.-S., Weiss, E., Elbaghdadi, R., Remy, J.-S., Mulherkar, R., & Zuber, G. (2010). Proton Sponge Trick for pH-Sensitive Disassembly of Polyethylenimine-Based siRNA Delivery Systems. Bioconjugate Chemistry. https://doi.org/10.1021/bc100010k
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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