ArticleEJNMMI radiopharmacy and chemistry2019
Comparison of desferrioxamine and NODAGA for the gallium-68 labeling of exendin-4.
Article in EJNMMI radiopharmacy and chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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10 citing papers in PubMed, 15 citations in OpenAlex.
- High-yield, standardised automated radiosynthesis process for routine clinical insulinoma PET with [⁶⁸Ga]Ga-NODAGA-exendin-4.EJNMMI radiopharmacy and chemistry · 2026Article
- Development of an automated radiosynthesis for [EJNMMI radiopharmacy and chemistry · 2026Article
- Site-SpecificBioconjugate chemistry · 2023Article
- Theranostic in GLP-1R molecular imaging: challenges and emerging opportunities.Frontiers in molecular biosciences · 2023Review
- Modern Developments in Bifunctional Chelator Design for Gallium Radiopharmaceuticals.Molecules (Basel, Switzerland) · 2022Review
- Comparison of the Tissue Distribution of a Long-Circulating Glucagon-like Peptide-1 Agonist Determined by Positron Emission Tomography and Quantitative Whole-Body Autoradiography.ACS pharmacology & translational science · 2022Article
- Cold Kit Labeling: The Future ofFrontiers in medicine · 2022Review
- HER3 PET Imaging:Cancers · 2021Article
- [International journal of molecular sciences · 2021Article
- Radiolabelling of the octadentate chelators DFO* and oxoDFO* with zirconium-89 and gallium-68.Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry · 2020Article
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4 authors at 3 institutions in 2 countries.
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Abstract
introductionRadiolabeled exendin-4 (Ex4) derivatives are used to target the glucagon-like peptide-1 receptor (GLP-1R) for the clinical diagnosis of insulinomas, a rare type of neuroendocrine tumor. Gallium-68 is an ideal diagnostic nuclide for this application and a study evaluating an exendin-4-NODAGA conjugate is currently underway. However, in complexion with the chelator DFO, its in vivo stability has been a matter of dispute. The aim of this work was to directly compare [
methodsIn our approach, we directly compared N'-[5-(acetyl-hydroxy-amino)pentyl]-N-[5-[3-(5-aminopentyl-hydroxy-carbamoyl)propanoylamino]pentyl]-N-hydroxy-butane diamide (desferriox-amine B, DFO) and 2-(4,7-bis (carboxymethyl)-1,4,7-triazonan-1-yl) pentanedioic acid (NODAGA) conjugated to exendin-4 in vitro and in vivo. We radiolabeled the peptides with gallium-68, followed by HPLC quality control. In vitro characterization was performed in CHL cells overexpressing the GLP-1R and in vivo studies were conducted with CD1 nu/nu mice carrying tumors derived from these cells.
resultsWe found that both peptides could be radiolabeled with a molar activity of about 9.33 MBq/nmol without further purification. They internalized equally well into GLP-1R-expressing cells and their IC CONCLUSION AND RELEVANCE: DFO is a suitable chelator for the radiolabeling of exendin-4 derivatives with gallium-68 for in vitro and preclinical in vivo studies. DFO performed better in vivo due to its significantly lower kidney accumulation (p < 0.0001). It was also found to be stable in vivo in mice, contrary to earlier reports. Based on our results, the DFO chelating system in combination with exendin-4 would be an interesting option for clinical imaging of insulinomas.
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