Design, Synthesis, and Evaluation of Enhanced DNA Binding New Lipopolythioureas - Unité de pharmacologie chimique et génétique et d'imagerie Access content directly
Journal Articles Bioconjugate Chemistry Year : 2006

Design, Synthesis, and Evaluation of Enhanced DNA Binding New Lipopolythioureas

Abstract

Nonviral gene delivery is limited to a large extent by the cationic nature of most of the chemical vector. We have shown that lipopolythioureas interact with DNA. However, lipopolythioureas were not very efficient at transfecting cells, probably due to reduced interaction between the noncationic synthetic lipid and the cell membrane. Here, we report that liposomes made from a new thiourea lipid, DPPC, and a lipid bearing an RGD ligand allowed very efficient entry of the lipopolythioureas into integrin R v 3 expressing cells. In addition, we show that a stable interaction between DNA and lipopolythiourea could be obtain with two thiourea groups. Moreover, the addition of a hydrophilic terminus improves the formulation of these new DNA binding agents.
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hal-02512562 , version 1 (19-03-2020)

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Jeanne Leblond, Nathalie Mignet, Lucie Leseurre, Celine Largeau, Michel Bessodes, et al.. Design, Synthesis, and Evaluation of Enhanced DNA Binding New Lipopolythioureas. Bioconjugate Chemistry, inPress, ⟨10.1021/bc060110g⟩. ⟨hal-02512562⟩
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