ArticleContrast media & molecular imaging
Radiolabelled GLP-1 analogues for in vivo targeting of insulinomas.
Article in Contrast media & molecular imaging. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 48 citations in OpenAlex.
- Peptide Radioligands in Cancer Theranostics: Agonists and Antagonists.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Role of Exendin-4 Functional Imaging in Diagnosis of Insulinoma: A Systematic Review.Life (Basel, Switzerland) · 2023Review
- Conjugation to a cell-penetrating peptide drives the tumour accumulation of the GLP1R antagonist exendin(9-39).European journal of nuclear medicine and molecular imaging · 2023Article
- Small peptide-based GLP-1R ligands: an approach to reduce the kidney uptake of radiolabeled GLP-1R-targeting agents?EJNMMI radiopharmacy and chemistry · 2021Article
- NHS-Functionalized THP Derivative for Efficient Synthesis of Kit-Based Precursors forBiomedicines · 2021Article
- Non-invasive Beta-cell Imaging: Visualization, Quantification, and Beyond.Frontiers in endocrinology · 2021Review
- Receptor-Targeted Photodynamic Therapy of Glucagon-Like Peptide 1 Receptor-Positive Lesions.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2020Article
- 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
- Advances in GLP-1 receptor targeting radiolabeled agent development and prospective of theranostics.Theranostics · 2020Review
- Exendin-4 analogs in insulinoma theranostics.Journal of labelled compounds & radiopharmaceuticals · 2019Review
- Molecular imaging of β-cells: diabetes and beyond.Advanced drug delivery reviews · 2019Review
- Pancreatic imaging using an antibody fragment targeting the zinc transporter type 8: a direct comparison with radio-iodinated Exendin-4.Acta diabetologica · 2018Article
- Preclinical evaluation of PAC1 targeting with radiolabeled Maxadilan.Scientific reports · 2017Article
- 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
- Strain Differences Determine the Suitability of Animal Models for Noninvasive In Vivo Beta Cell Mass Determination with Radiolabeled Exendin.Molecular imaging and biology · 2016Article
- A Synthetic Heterobivalent Ligand Composed of Glucagon-Like Peptide 1 and Yohimbine Specifically Targets β Cells Within the Pancreas.Molecular imaging and biology · 2015Article
- Beta cell specific probing with fluorescent exendin-4 is progressively reduced in type 2 diabetic mouse models.Islets · 2015Article
- Evaluation of ¹¹¹in-labelled exendin-4 derivatives containing different meprin β-specific cleavable linkers.PloS one · 2015Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
Internalizing agonists are usually selected for peptide receptor targeting. There is increasing evidence that non-internalizing receptor antagonists can be used for this purpose. We investigated whether the glucagon-like peptide-1 receptor (GLP-1R) antagonist exendin(9-39) can be used for in vivo targeting of GLP-1R expressing tumours and compared the in vitro and in vivo characteristics with the GLP-1R agonists exendin-3 and exendin-4. The binding and internalization kinetics of labelled [Lys(40) (DTPA)]exendin-3, [Lys(40) (DTPA)]exendin-4 and [Lys(40) (DTPA)]exendin(9-39) were determined in vitro using INS-1 cells. The in vivo targeting properties of [Lys(40) ((111) In-DTPA)]exendin-3, [Lys(40) ((111) In-DTPA)]exendin-4 and [Lys(40) ((111) In-DTPA)]exendin(9-39) were examined in BALB/c nude mice with subcutaneous INS-1 tumours. (nat) In-labelled [Lys(40) (DTPA)]exendin-3, [Lys(40) (DTPA)]exendin-4 and [Lys(40) (DTPA)]exendin(9-39) exhibited similar IC(50) values (13.5, 14.4 and 13.4 n m, respectively) and bound to 26 × 10(3) , 41 × 10(3) and 37 × 10(3) receptors per cell, respectively. [Lys(40) ((111) In-DTPA)]exendin-3 and [Lys(40) ((111) In-DTPA)]exendin-4 showed rapid in vitro binding and internalization kinetics, whereas [Lys(40) ((111) In-DTPA)]exendin(9-39) showed lower binding and minimal internalization in vitro. In mice, high specific uptake of [Lys(40) ((111) In-DTPA)]exendin-3 [25.0 ± 6.0% injected dose (ID) g(-1) ] in the tumour was observed at 0.5 h post-injection (p.i.) with similar uptake up to 4 h p.i. [Lys(40) ((111) In-DTPA)]exendin-4 showed higher tumour uptake at 1 and 4 h p.i. (40.8 ± 7.0 and 41.9 ± 7.2% ID g(-1), respectively). Remarkably, [Lys(40) ((111) In-DTPA)]exendin(9-39) showed only low specific uptake in the tumour at 0.5 h p.i. (3.2 ± 0.7% ID g(-1)), rapidly decreasing over time. In conclusion, the GLP-1R agonists [Lys(40) (DTPA)]exendin-3 and [Lys(40) (DTPA)]exendin-4 labelled with (111) In could be useful for in vivo GLP-1R targeting, whereas [Lys(40) (DTPA)]exendin(9-39) is not suited for in vivo targeting of the GLP-1R.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.