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Article

[68Ga]Ga-DFO-c(RGDyK): Synthesis and Evaluation of Its Potential for Tumor Imaging in Mice

1
Department of Organic Chemistry, Faculty of Science, Palacky University, 77900 Olomouc, Czech Republic
2
Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacky University, 77900 Olomouc, Czech Republic
*
Authors to whom correspondence should be addressed.
Academic Editors: Menotti Ruvo and Nunzianna Doti
Int. J. Mol. Sci. 2021, 22(14), 7391; https://doi.org/10.3390/ijms22147391
Received: 14 May 2021 / Revised: 6 July 2021 / Accepted: 6 July 2021 / Published: 9 July 2021
Angiogenesis has a pivotal role in tumor growth and the metastatic process. Molecular imaging was shown to be useful for imaging of tumor-induced angiogenesis. A great variety of radiolabeled peptides have been developed to target αvβ3 integrin, a target structure involved in the tumor-induced angiogenic process. The presented study aimed to synthesize deferoxamine (DFO)-based c(RGD) peptide conjugate for radiolabeling with gallium-68 and perform its basic preclinical characterization including testing of its tumor-imaging potential. DFO-c(RGDyK) was labeled with gallium-68 with high radiochemical purity. In vitro characterization including stability, partition coefficient, protein binding determination, tumor cell uptake assays, and ex vivo biodistribution as well as PET/CT imaging was performed. [68Ga]Ga-DFO-c(RGDyK) showed hydrophilic properties, high stability in PBS and human serum, and specific uptake in U-87 MG and M21 tumor cell lines in vitro and in vivo. We have shown here that [68Ga]Ga-DFO-c(RGDyK) can be used for αvβ3 integrin targeting, allowing imaging of tumor-induced angiogenesis by positron emission tomography. View Full-Text
Keywords: deferoxamine; RGD peptides; integrins; radiodiagnostics; PET imaging deferoxamine; RGD peptides; integrins; radiodiagnostics; PET imaging
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MDPI and ACS Style

Krajcovicova, S.; Daniskova, A.; Bendova, K.; Novy, Z.; Soural, M.; Petrik, M. [68Ga]Ga-DFO-c(RGDyK): Synthesis and Evaluation of Its Potential for Tumor Imaging in Mice. Int. J. Mol. Sci. 2021, 22, 7391. https://doi.org/10.3390/ijms22147391

AMA Style

Krajcovicova S, Daniskova A, Bendova K, Novy Z, Soural M, Petrik M. [68Ga]Ga-DFO-c(RGDyK): Synthesis and Evaluation of Its Potential for Tumor Imaging in Mice. International Journal of Molecular Sciences. 2021; 22(14):7391. https://doi.org/10.3390/ijms22147391

Chicago/Turabian Style

Krajcovicova, Sona, Andrea Daniskova, Katerina Bendova, Zbynek Novy, Miroslav Soural, and Milos Petrik. 2021. "[68Ga]Ga-DFO-c(RGDyK): Synthesis and Evaluation of Its Potential for Tumor Imaging in Mice" International Journal of Molecular Sciences 22, no. 14: 7391. https://doi.org/10.3390/ijms22147391

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