Solid-phase synthesis of 89 polyamine-based cationic lipids for DNA delivery to mammalian cells
Yingyongnarongkul, Boon-ek, Howarth, Mark, Elliott, Tim and Bradley, Mark (2004) Solid-phase synthesis of 89 polyamine-based cationic lipids for DNA delivery to mammalian cells Chemistry - A European Journal, 10, (2), pp. 463-473. (doi:10.1002/chem.200305232).
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The ability of non-viral gene delivery systems to overcome extracellular and intracellular barriers is a critical issue for future clinical applications of gene therapy. In recent years much effort has been focused on the development of a variety of DNA carriers, and cationic liposomes have become the most common non-viral gene delivery system. Solid-phase synthesis was used to produce three libraries of polyamine-based cationic lipids with diverse hydrophobic tails. These were characterised, and structure-activity relationships were determined for DNA binding and transfection ability of these compounds when formulated as cationic liposomes. Two of the cationic lipids produced high-efficiency transfection of human cells. Surprisingly, these two compounds were from the library with two headgroups and one aliphatic tail, a compound class regarded as detergent-like and little investigated for transfection. These cationic lipids are promising reagents for gene delivery and illustrate the potential of solid-phase synthesis methods for lipoplex discovery.
|Digital Object Identifier (DOI):||doi:10.1002/chem.200305232|
|Keywords:||cationic lipids, combinatorial chemistry, gene therapy, non-viral vector, solid-phase synthesisgene-transfer, liposome complexes, biologic activity, amino-groups, transfection, vectors, efficient, deprotection, guanidines, mechanism|
|Subjects:||Q Science > QD Chemistry
Q Science > QH Natural history > QH426 Genetics
R Medicine > RM Therapeutics. Pharmacology
|Date Deposited:||16 Feb 2006|
|Last Modified:||18 Feb 2017 17:46|
Funded by: BBSRC (UNSPECIFIED)
UNSPECIFIED to UNSPECIFIED
|Further Information:||Google Scholar|
|RDF:||RDF+N-Triples, RDF+N3, RDF+XML, Browse.|
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