ArticleEuropean journal of nuclear medicine and molecular imaging2010
68Ga-labelled exendin-3, a new agent for the detection of insulinomas with PET.
Article in European journal of nuclear medicine and molecular imaging, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 66 papers.
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Who cites it
66 citing papers in PubMed, 144 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
- 68 Ga-NODAGA-EXENDIN-4 PET/CT in the Detection or the Exclusion of Occult Sporadic Insulinomas.Clinical nuclear medicine · 2025Article
- Engineered GLP-1R-targeting nanoplatforms: multimodal therapeutics in human diseases.Journal of nanobiotechnology · 2025Review
- [EJNMMI research · 2025Article
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- GLP- 1R status using validated monoclonal antibody in 689 cases of neuroendocrine neoplasm and its correlation with somatostatin receptor scintigraphy, insulin production, and histological grades.Virchows Archiv : an international journal of pathology · 2025Article
- Characterization of the Pancreatic Neuroendocrine Neoplasm Immune Microenvironment.Cancer medicine · 2025Review
- Characterization and comparison of insulinoma tumor model and pancreatic damage caused by the tumor, and identification of possible markers.Molecular biology reports · 2024Article
- Theranostic in GLP-1R molecular imaging: challenges and emerging opportunities.Frontiers in molecular biosciences · 2023Review
- Article
- Translational challenges in pancreatic neuroendocrine tumor immunotherapy.Biochimica et biophysica acta. Reviews on cancer · 2021Review
- Small peptide-based GLP-1R ligands: an approach to reduce the kidney uptake of radiolabeled GLP-1R-targeting agents?EJNMMI radiopharmacy and chemistry · 2021Article
- Non-invasive Beta-cell Imaging: Visualization, Quantification, and Beyond.Frontiers in endocrinology · 2021Review
- Targeted Optical Imaging of the Glucagonlike Peptide 1 Receptor Using Exendin-4-IRDye 800CW.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2020Article
- Innovative imaging of insulinoma: the end of sampling? A review.Endocrine-related cancer · 2020Review
- Advances in GLP-1 receptor targeting radiolabeled agent development and prospective of theranostics.Theranostics · 2020Review
- Noninvasive longitudinal quantification of β-cell mass with [FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2019Article
- A Comprehensive Review of Non-Covalent Radiofluorination Approaches Using Aluminum [Molecules (Basel, Switzerland) · 2019Review
- First-in-class positron emission tomography tracer for the glucagon receptor.EJNMMI research · 2019Article
- Molecular imaging of β-cells: diabetes and beyond.Advanced drug delivery reviews · 2019Review
6 more citing papers are in PubMed but not listed here.
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5 authors at 2 institutions in 1 country.
Funding
Abstract
purposeInsulinomas are neuroendocrine tumours derived from pancreatic beta-cells. The glucagon-like peptide 1 receptor (GLP-1R) is expressed with a high incidence (>90%) and high density in insulinomas. Glucagon-like peptide 1 (GLP-1), the natural ligand of GLP-1R, is rapidly degraded in vivo. A more stable agonist of GLP-1R is exendin-3. We investigated imaging of insulinomas with DOTA-conjugated exendin-3 labelled with (68)Ga.
methodsTargeting of insulinomas with [Lys(40)(DOTA)]exendin-3 labelled with either (111)In or (68)Ga was investigated in vitro using insulinoma tumour cells (INS-1). [Lys(40)((111)In-DTPA)]Exendin-3 was used as a reference in this study. In vivo targeting was investigated in BALB/c nude mice with subcutaneous INS-1 tumours. PET imaging was performed using a preclinical PET/CT scanner.
resultsIn vitro exendin-3 specifically bound and was internalized by GLP-1R-positive cells. In BALB/c nude mice with subcutaneous INS-1 tumours a high uptake of [Lys(40)((111)In-DTPA)]exendin-3 in the tumour was observed (33.5 +/- 11.6%ID/g at 4 h after injection). Uptake was specific, as determined by coinjection of an excess of unlabelled [Lys(40)]exendin-3 (1.8 +/- 0.1%ID/g). The pancreas also exhibited high and specific uptake (11.3 +/- 1.0%ID/g). High uptake was also found in the kidneys (144 +/- 24%ID/g) and this uptake was not receptor-mediated. In this murine tumour model optimal targeting of the GLP-1R expressing tumour was obtained at exendin doses < or =0.1 microg. Remarkably, tumour uptake of (68)Ga-labelled [Lys(40)(DOTA)]exendin-3 was lower (8.9 +/- 3.1%ID/g) than tumour uptake of (111)In-labelled [Lys(40)(DTPA)]exendin-3 (25.4 +/- 7.2%ID/g). The subcutaneous tumours were clearly visualized by small-animal PET imaging after injection of 3 MBq of [Lys(40)((68)Ga-DOTA)]exendin-3.
conclusion[Lys(40)((68)Ga-DOTA)]Exendin-3 specifically accumulates in insulinomas, although the uptake is lower than that of [Lys(40)((111)In-DTPA)]exendin-3. Therefore, [Lys(40)((68)Ga-DOTA)]exendin-3 is a promising tracer to visualize insulinomas with PET.
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