| Efficient nucleic acid transduction with lipoplexes containing novel piperazine- and polyamine-conjugated cholesterol derivatives. | |
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MedLine Citation:
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PMID: 19028097 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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To advance the use of cationic lipids for non-viral nucleic acid vector formulation, a panel of novel nitrogen heterocycle cholesteryl derivatives containing a biodegradable carbamate linker was synthesised. Optimally acting piperazine and cyclen compounds had nucleic acid-binding and lipoplex nanoparticle formation properties that were suitable for their use as non-viral vectors. It was found that the lipoplexes formed were capable of efficient non-toxic nucleic acid delivery to cells in culture. The chemical structure of individual cationic lipids, which is likely to influence lipoplex formation, affected efficiency of DNA or RNA transfection. The results indicated that the cyclen containing compound possessing two cholesteryl moieties resulted in efficient siRNA-mediated target gene silencing but was a poor reagent for DNA transfection. |
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Authors:
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Rafique Ul Islam; Justin Hean; Willem A L van Otterlo; Charles B de Koning; Patrick Arbuthnot |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2008-11-06 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 19 ISSN: 1464-3405 ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2009 Jan |
Date Detail:
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Created Date: 2008-12-26 Completed Date: 2009-01-28 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: England |
Other Details:
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Languages: eng Pagination: 100-3 Citation Subset: IM |
Affiliation:
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Department of Molecular Medicine and Haematology, Antiviral Gene Therapy Research Unit, University of the Witwatersrand Medical School, Private Bag 3, WITS, South Africa. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Cations Cells / metabolism Cholesterol Esters / chemistry* DNA / pharmacokinetics Heterocyclic Compounds / chemistry* Humans Lipids / chemistry Piperazines / chemistry* Polyamines / chemistry* RNA / pharmacokinetics RNA, Small Interfering / pharmacokinetics Transduction, Genetic / methods* |
| Chemical | |
Reg. No./Substance:
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0/Cations; 0/Cholesterol Esters; 0/Heterocyclic Compounds; 0/Lipids; 0/Piperazines; 0/Polyamines; 0/RNA, Small Interfering; 294-90-6/cyclen; 63231-63-0/RNA; 9007-49-2/DNA |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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