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Solid‐Phase Synthesis of 89 Polyamine‐Based Cationic Lipids for DNA Delivery to Mammalian Cells
Author(s) -
Yingyongnarongkul Boonek,
Howarth Mark,
Elliott Tim,
Bradley Mark
Publication year - 2004
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.200305232
Subject(s) - transfection , cationic polymerization , gene delivery , cationic liposome , liposome , polyamine , intracellular , chemistry , dna , genetic enhancement , biochemistry , biophysics , microbiology and biotechnology , biology , gene , organic chemistry
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.