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Synthesis and in vitro evaluation of an antiangiogenic cancer-specific dual-targeting 177Lu-Au-nanoradiopharmaceutical

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Abstract

The aim of this research was to synthesize and chemically characterize a cancer-specific 177Lu-Au-nanoradiopharmaceutical based on gold nanoparticles (NPs), the nuclear localization sequence (NLS)-Arg-Gly-Asp peptide and an aptamer (HS-pentyl-pegaptanib) to target both the α(v)β(3) integrin and the vascular endothelial growth factor (VEGF) overexpressed in the tumor neovasculature, as well as to evaluate by the tube formation assay, the nanosystem capability to inhibit angiogenesis. 177Lu-NP-RGD-NLS-Aptamer was obtained with a radiochemical purity of 99 ± 1%. Complete inhibition of tube formation (angiogenesis) was demonstrated when endothelial cells (EA.hy926), cultured in a 3D-extracellular matrix support, were treated with the developed nanosystem.

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Acknowledgements

This study was supported by the Mexican National Council of Science and Technology (CONACYT-SEP-CB-2014-01-242443). This research was carried out as part of the activities of the “Laboratorio Nacional de Investigación y Desarrollo de Radiofármacos, CONACyT”.

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Correspondence to Guillermina Ferro-Flores.

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González-Ruíz, A., Ferro-Flores, G., Azorín-Vega, E. et al. Synthesis and in vitro evaluation of an antiangiogenic cancer-specific dual-targeting 177Lu-Au-nanoradiopharmaceutical. J Radioanal Nucl Chem 314, 1337–1345 (2017). https://doi.org/10.1007/s10967-017-5465-x

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  • DOI: https://doi.org/10.1007/s10967-017-5465-x

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