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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Synthesis, characterization, and in vivo delivery of siRNA-squalene nanoparticles targeting fusion oncogene in papillary thyroid carcinoma
Journal of Medicinal Chemistry, Volume 54, No. 12, Year 2011
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Description
We report the conjugation of the natural lipid squalene (SQ) with a small interfering RNA (siRNA), against the junction oncogene RET/PTC1, usually found in papillary thyroid carcinoma (PTC). The acyclic isoprenoid chain of squalene has been covalently coupled with siRNA RET/PTC1 at the 3′-terminus of the sense strand via maleimide-sulfhydryl chemistry. Remarkably, the linkage of siRNA RET/PTC1 to squalene led to an amphiphilic molecule that self-organized in H2O as siRNA-SQ RET/PTC1 nanoparticles (NPs). The siRNA-SQ RET/PTC1 NPs, stable in H2O, were used for biological studies. In vitro, they did not show any cytotoxicity. Interestingly, in vivo, on a mice xenografted RET/PTC1 experimental model, RET/PTC1-SQ NPs were found to inhibit tumor growth and RET/PTC1 oncogene and oncoprotein expression after 2.5 mg/kg cumulative dose intravenous injections. In conclusion, these results showed that the "squalenoylation" offers a new noncationic plate-form for the siRNA delivery. © 2011 American Chemical Society.
Authors & Co-Authors
Raouane, Mouna
France, Chatenay-malabry
Institut Galien Paris-saclay
France, Villejuif
Institut de Cancerologie Gustave Roussy
Tunisia, Sousse
Faculty of Medicine Sousse
Desmaële, Didier
France, Chatenay-malabry
Institut Galien Paris-saclay
Gilbert-Sirieix, Marie
France, Villejuif
Institut de Cancerologie Gustave Roussy
Gueutin, Claire
France, Chatenay-malabry
Institut Galien Paris-saclay
Zouhiri, Fatima
France, Chatenay-malabry
Institut Galien Paris-saclay
Bourgaux, Claudie
France, Chatenay-malabry
Institut Galien Paris-saclay
Lepeltier, Elise
France, Chatenay-malabry
Institut Galien Paris-saclay
Gref, R.
France, Chatenay-malabry
Institut Galien Paris-saclay
Ben Salah, Ridha
Tunisia, Sousse
Faculty of Medicine Sousse
Clayman, Gary
United States, Houston
University of Texas Health Science Center at Houston
Massaad-Massade, Liliane
France, Villejuif
Institut de Cancerologie Gustave Roussy
Couvreur, P.
France, Chatenay-malabry
Institut Galien Paris-saclay
Statistics
Citations: 72
Authors: 12
Affiliations: 4
Identifiers
Doi:
10.1021/jm2000272
ISSN:
00222623
e-ISSN:
15204804
Research Areas
Cancer