Cookies on this website

We use cookies to ensure that we give you the best experience on our website. If you click 'Accept all cookies' we'll assume that you are happy to receive all cookies and you won't see this message again. If you click 'Reject all non-essential cookies' only necessary cookies providing core functionality such as security, network management, and accessibility will be enabled. Click 'Find out more' for information on how to change your cookie settings.

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.

Original publication

DOI

10.1002/chem.200305232

Type

Journal article

Journal

Chemistry (Weinheim an der Bergstrasse, Germany)

Publication Date

01/2004

Volume

10

Pages

463 - 473

Addresses

Department of Chemistry, University of Southampton, Southampton SO17 1BJ, UK.

Keywords

Cell Line, Humans, Cations, Guanidine, Polyamines, Lipids, DNA, Transfection, Cell Survival, Binding Sites, Molecular Structure, Structure-Activity Relationship, Genetic Vectors, Plasmids