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Solid-phase synthesis of 89 polyamine-based cationic lipids for DNA delivery to mammalian cells

Solid-phase synthesis of 89 polyamine-based cationic lipids for DNA delivery to mammalian cells
Solid-phase synthesis of 89 polyamine-based cationic lipids for DNA delivery to mammalian cells
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.
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
0947-6539
463-473
Yingyongnarongkul, Boon-ek
9fd5bdf6-d2f0-4b32-b1f2-72f1931d9605
Howarth, Mark
75054a4c-d313-4a69-ba86-8a08104ca300
Elliott, Tim
16670fa8-c2f9-477a-91df-7c9e5b453e0e
Bradley, Mark
562b9add-34c4-4620-bfa1-c7c83a0f0900
Yingyongnarongkul, Boon-ek
9fd5bdf6-d2f0-4b32-b1f2-72f1931d9605
Howarth, Mark
75054a4c-d313-4a69-ba86-8a08104ca300
Elliott, Tim
16670fa8-c2f9-477a-91df-7c9e5b453e0e
Bradley, Mark
562b9add-34c4-4620-bfa1-c7c83a0f0900

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).

Record type: Article

Abstract

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.

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More information

Published date: 23 January 2004
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

Identifiers

Local EPrints ID: 20348
URI: http://eprints.soton.ac.uk/id/eprint/20348
ISSN: 0947-6539
PURE UUID: 18d14388-eedd-46b9-821d-f20561a96298
ORCID for Tim Elliott: ORCID iD orcid.org/0000-0003-1097-0222

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Date deposited: 16 Feb 2006
Last modified: 17 Jul 2017 16:29

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Contributors

Author: Boon-ek Yingyongnarongkul
Author: Mark Howarth
Author: Tim Elliott ORCID iD
Author: Mark Bradley

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