Synthesis, Characterization, and in Vivo Delivery of siRNA-Squalene Nanoparticles Targeting Fusion Oncogene in Papillary Thyroid Carcinoma
Тип публикации: Journal Article
Дата публикации: 2011-05-18
SCImago Q1
Tоп 10% SCImago
WOS Q1
БС1
SJR: 1.726
CiteScore: 11.1
Impact factor: 7.3
ISSN: 00222623, 15204804
PubMed ID:
21561161
Drug Discovery
Molecular Medicine
Краткое описание
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 H(2)O as siRNA-SQ RET/PTC1 nanoparticles (NPs). The siRNA-SQ RET/PTC1 NPs, stable in H(2)O, 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.
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Raouane M. et al. Synthesis, Characterization, and in Vivo Delivery of siRNA-Squalene Nanoparticles Targeting Fusion Oncogene in Papillary Thyroid Carcinoma // Journal of Medicinal Chemistry. 2011. Vol. 54. No. 12. pp. 4067-4076.
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Raouane M., Desmaele D., Gilbert-Sirieix M., GUEUTIN C., Zouhiri F., Bourgaux C., Lepeltier E., Gref R., Ben Salah R., Clayman G., Massaad-Massade L., Couvreur P. Synthesis, Characterization, and in Vivo Delivery of siRNA-Squalene Nanoparticles Targeting Fusion Oncogene in Papillary Thyroid Carcinoma // Journal of Medicinal Chemistry. 2011. Vol. 54. No. 12. pp. 4067-4076.
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TY - JOUR
DO - 10.1021/jm2000272
UR - https://doi.org/10.1021/jm2000272
TI - Synthesis, Characterization, and in Vivo Delivery of siRNA-Squalene Nanoparticles Targeting Fusion Oncogene in Papillary Thyroid Carcinoma
T2 - Journal of Medicinal Chemistry
AU - Raouane, Mouna
AU - Desmaele, Didier
AU - Gilbert-Sirieix, Marie
AU - GUEUTIN, CLAIRE
AU - Zouhiri, Fatima
AU - Bourgaux, C.
AU - Lepeltier, Elise
AU - Gref, R
AU - Ben Salah, Ridha
AU - Clayman, Gary
AU - Massaad-Massade, Liliane
AU - Couvreur, Patrick
PY - 2011
DA - 2011/05/18
PB - American Chemical Society (ACS)
SP - 4067-4076
IS - 12
VL - 54
PMID - 21561161
SN - 0022-2623
SN - 1520-4804
ER -
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@article{2011_Raouane,
author = {Mouna Raouane and Didier Desmaele and Marie Gilbert-Sirieix and CLAIRE GUEUTIN and Fatima Zouhiri and C. Bourgaux and Elise Lepeltier and R Gref and Ridha Ben Salah and Gary Clayman and Liliane Massaad-Massade and Patrick Couvreur},
title = {Synthesis, Characterization, and in Vivo Delivery of siRNA-Squalene Nanoparticles Targeting Fusion Oncogene in Papillary Thyroid Carcinoma},
journal = {Journal of Medicinal Chemistry},
year = {2011},
volume = {54},
publisher = {American Chemical Society (ACS)},
month = {may},
url = {https://doi.org/10.1021/jm2000272},
number = {12},
pages = {4067--4076},
doi = {10.1021/jm2000272}
}
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MLA
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Raouane, Mouna, et al. “Synthesis, Characterization, and in Vivo Delivery of siRNA-Squalene Nanoparticles Targeting Fusion Oncogene in Papillary Thyroid Carcinoma.” Journal of Medicinal Chemistry, vol. 54, no. 12, May. 2011, pp. 4067-4076. https://doi.org/10.1021/jm2000272.
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