The aim of this research was to evaluate the <em>in vitro</em> potential of <sup>177</sup>Lu-labeled gold nanoparticles conjugated to cyclo-[RGDfK(C)] peptides (<sup>177</sup>Lu-AuNP-c[RGDfK(C)]) as a plasmonic photothermal therapy and targeted radiotherapy system in MCF7 breast cancer cells. Peptides were conjugated to AuNPs (20 nm) by spontaneous reaction with the thiol group of cysteine (C). After laser irradiation, the presence of c[RGDfK(C)]-AuNP in cells caused a significant increase in the temperature of the medium (50.5 °C, compared to 40.3 °C without AuNPs) resulting in a significant decrease in MCF7 cell viability down to 9 %. After treatment with <sup>177</sup>-AuNP-c[RGDfK(C)], the MCF7 cell proliferation was significantly inhibited.
Gold nanoparticles (AuNPs) have been proposed for a variety of medical applications such as localized heat sources for cancer treatment and drug delivery systems. The conjugation of peptides to AuNPs produces stable multimeric systems with target-specific molecular recognition. Lutetium- 177 ((177)Lu) has been successfully used in peptide radionuclide therapy. Recently, (177)Lu-AuNPs conjugated to different peptides have been proposed as a new class of theranostic radiopharmaceuticals. These radioconjugates may function simultaneously as molecular imaging agents, radiotherapy systems and thermal-ablation systems. This article covers advancements in the design, synthesis, physicochemical characterization, molecular recognition assessment and preclinical therapeutic efficacy of gold nanoparticles radiolabeled with (177)Lu and conjugated to RGD (-Arg-Gly-Asp-), Lys(3)-Bombesin and Tat(49-57) peptides.
Different kit formulations for the direct labeling of MoAb-IOR CEAl and its F(ab')2 fragments with Rhenium-188, using EHDP as a weak competing ligand, were developed. The influence of reaction conditions such as pH, temperature, weak ligand concentration and stannous Chloride concentration during the preparation of '""Re-MoAb radioimmunoconjugates, were investigated in detail in order to obtain high radiochemical yields. Results showed that under different reaction conditions, radiochemical purities Over 95% were obtained in 1 to 2 h periods after addition of perrhenate Solution eluted from the ""W/'®®Re generator to a kit formulation. The procedure reported herein demonstrated the overall usefulness for the preparation of pure "®Re-antibody fragments.
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