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.

Item Type: Article
Digital Object Identifier (DOI): doi:10.1002/chem.200305232
ISSNs: 0947-6539 (print)
Related URLs:
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
ePrint ID: 20348
Date :
Date Event
23 January 2004Published
Date Deposited: 16 Feb 2006
Last Modified: 16 Apr 2017 22:59
Further Information:Google Scholar

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