[68Ga]Ga-DFO-c(RGDyK): synthesis and evaluation of its potential for tumor imaging in mice

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F21%3A73608285" target="_blank" >RIV/61989592:15310/21:73608285 - isvavai.cz</a>
Result on the web
<a href="https://www.mdpi.com/1422-0067/22/14/7391/htm" target="_blank" >https://www.mdpi.com/1422-0067/22/14/7391/htm</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3390/ijms22147391" target="_blank" >10.3390/ijms22147391</a>

Result language
angličtina
Original language name
[68Ga]Ga-DFO-c(RGDyK): synthesis and evaluation of its potential for tumor imaging in mice
Original language description
Angiogenesis has a pivotal role in tumor growth and 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, 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.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10401 - Organic chemistry

Project
<a href="/en/project/EF16_019%2F0000868" target="_blank" >EF16_019/0000868: Molecular, cellular and clinical approach to healthy ageing</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year
2021
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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