ArticleEuropean journal of nuclear medicine and molecular imaging2014
Radiolabelled GLP-1 receptor antagonist binds to GLP-1 receptor-expressing human tissues.
Article in European journal of nuclear medicine and molecular imaging, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 26 citations in OpenAlex.
- Distribution of glucagon-like peptide 1 receptor and insulin in phaeochromocytomas.Endocrine connections · 2026Article
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- Non-Alcoholic Fatty Liver Disease (NAFLD) Is an Independent Risk Factor for Developing New-Onset Diabetes After Acute Pancreatitis: A Multicenter Retrospective Cohort Study in Chinese Population.Frontiers in endocrinology · 2022Article
- Reply: From Mice to Humans: The Exocrine Pancreas Does Not Matter in Human GLP-1 Receptor Imaging.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2021Article
- Non-invasive Beta-cell Imaging: Visualization, Quantification, and Beyond.Frontiers in endocrinology · 2021Review
- Advances in GLP-1 receptor targeting radiolabeled agent development and prospective of theranostics.Theranostics · 2020Review
- The Effect of Exenatide on Thyroid-Stimulating Hormone and Thyroid Volume.European thyroid journal · 2019Article
- Blocking of Glucagonlike Peptide-1 Receptors in the Exocrine Pancreas Improves Specificity for β-Cells in a Mouse Model of Type 1 Diabetes.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2019Article
- Molecular imaging of β-cells: diabetes and beyond.Advanced drug delivery reviews · 2019Review
- Targets and probes for non-invasive imaging of β-cells.European journal of nuclear medicine and molecular imaging · 2017Review
- Current Status of Radiopharmaceuticals for the Theranostics of Neuroendocrine Neoplasms.Pharmaceuticals (Basel, Switzerland) · 2017Review
- Article
- (111)In-exendin uptake in the pancreas correlates with the β-cell mass and not with the α-cell mass.Diabetes · 2015Article
- The future of nuclear medicine imaging of neuroendocrine tumors: on a clear day one might see forever....European journal of nuclear medicine and molecular imaging · 2014Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeRadiolabelled glucagon-like peptide 1 (GLP-1) receptor agonists have recently been shown to successfully image benign insulinomas in patients. For the somatostatin receptor targeting of tumours, however, it was recently reported that antagonist tracers were superior to agonist tracers. The present study therefore evaluated various forms of the (125)iodinated-Bolton-Hunter (BH)-exendin(9-39) antagonist tracer for the in vitro visualization of GLP-1 receptor-expressing tissues in rats and humans and compared it with the agonist tracer (125)I-GLP-1(7-36)amide.
methodsReceptor autoradiography studies with (125)I-GLP-1(7-36)amide agonist or (125)I-BH-exendin(9-39) antagonist radioligands were performed in human and rat tissues.
resultsThe antagonist (125)I-BH-exendin(9-39) labelled at lysine 19 identifies all human and rat GLP-1 target tissues and GLP-1 receptor-expressing tumours. Binding is of high affinity and is comparable in all tested tissues in its binding properties with the agonist tracer (125)I-GLP-1(7-36)amide. For comparison, (125)I-BH-exendin(9-39) with the BH labelled at lysine 4 did identify the GLP-1 receptor in rat tissues but not in human tissues.
conclusionThe GLP-1 receptor antagonist exendin(9-39) labelled with (125)I-BH at lysine 19 is an excellent GLP-1 radioligand that identifies human and rat GLP-1 receptors in normal and tumoural tissues. It may therefore be the molecular basis to develop suitable GLP-1 receptor antagonist radioligands for in vivo imaging of GLP-1 receptor-expressing tissues in patients.
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