ArticleEuropean journal of nuclear medicine and molecular imaging2008
Targeting of a CCK(2) receptor splice variant with (111)In-labelled cholecystokinin-8 (CCK8) and (111)In-labelled minigastrin.
Article in European journal of nuclear medicine and molecular imaging, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 46 citations in OpenAlex.
- Development of INER-PP-F11N as the Peptide-Radionuclide Conjugate Drug Against CCK2 Receptor-Overexpressing Tumors.International journal of molecular sciences · 2025Article
- Peptide-based drugs in immunotherapy: current advances and future prospects.Medical oncology (Northwood, London, England) · 2025Review
- Peptide-Based Agents for Cancer Treatment: Current Applications and Future Directions.International journal of molecular sciences · 2023Review
- Peptides as multifunctional players in cancer therapy.Experimental & molecular medicine · 2023Review
- Peptide Radioligands in Cancer Theranostics: Agonists and Antagonists.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Nonpeptidic Z360-Analogs Tagged with Trivalent Radiometals as Anti-CCKPharmaceutics · 2022Article
- Preliminary Study of a 1,5-Benzodiazepine-Derivative Labelled with Indium-111 for CCK-2 Receptor Targeting.Molecules (Basel, Switzerland) · 2021Article
- [Molecular pharmaceutics · 2020Article
- Cholecystokinin-2 Receptor Targeting with Radiolabeled Peptides: Current Status and Future Directions.Current medicinal chemistry · 2020Review
- Utilizing Peptide Ligand GPCRs to Image and Treat Pancreatic Cancer.Biomedicines · 2018Review
- Characterization ofScientific reports · 2018Article
- Article
- Tumor antigens as proteogenomic biomarkers in invasive ductal carcinomas.BMC medical genomics · 2014Article
- Article
- Preclinical evaluation of radiolabeled DOTA-derivatized cyclic minigastrin analogs for targeting cholecystokinin receptor expressing malignancies.Molecular imaging and biology · 2012Article
- A single nucleotide polymorphism of the cholecystokinin-B receptor predicts risk for pancreatic cancer.Cancer biology & therapy · 2012Article
- Radiolabelled peptides for oncological diagnosis.European journal of nuclear medicine and molecular imaging · 2012Review
- Radiolabeled CCK/gastrin peptides for imaging and therapy of CCK2 receptor-expressing tumors.Amino acids · 2011Review
- Comparison of the binding and internalization properties of 12 DOTA-coupled and ¹¹¹In-labelled CCK2/gastrin receptor binding peptides: a collaborative project under COST Action BM0607.European journal of nuclear medicine and molecular imaging · 2011Article
- 68Ga-labelled exendin-3, a new agent for the detection of insulinomas with PET.European journal of nuclear medicine and molecular imaging · 2010Article
Corrections and comments
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Authors and funding
10 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeRadiolabelled cholecystokinin (CCK) and gastrin-derived peptides potentially can be used for peptide receptor radionuclide therapy (PRRT). Recently, a splice variant version of the CCK2R has been identified, designated CCK2i4svR. Constitutive expression of this receptor has been demonstrated in human colorectal cancer and in pancreatic cancer, but not in normal tissue. So far, it has never been shown whether radiolabelled peptides can target the CCK2i4svR in vivo. In this paper, we investigated the potential of sulfated (111)In-labelled DOTA-CCK8 (sCCK8), a pan-CCKR-binding peptide, and [(111)In]DOTA-minigastrin (MG0), a CCK2R selective peptide, for the targeting of the CCK2i4svR. MATERIALS AND
methodsThe receptor binding affinity of [(111)In]DOTA-sCCK8 and [(111)In]DOTA-MG0 for the CCK2R and CCK2i4svR was determined using stably transfected HEK293 cell lines, expressing either CCK2R or CCK2i4svR. Tumour targeting was studied in HEK293-CCK2i4svR tumour-bearing athymic mice.
results[(111)In]DOTA-sCCK8 as well as [(111)In]DOTA-MG0 specifically bound both CCK2R and CCK2i4svR with affinities in the low nanomolar range. In vivo experiments revealed that accumulation of both peptides in CCK2i4svR-positive tumours was similar (3.21 +/- 0.77 and 3.01 +/- 0.67%ID/g, sCCK8 and MG0, respectively, 24 h p.i.). Kidney retention of [(111)In]DOTA-MG0 (32.4 +/- 7.5%ID/g, 24 h p.i.) was markedly higher than that of [(111)In]DOTA-sCCK8 (2.75 +/- 0.31%ID/g, 24 h p.i.).
conclusionWe demonstrated that the CCK2i4svR is a potential target for PRRT using a radiolabelled sulfated CCK8 peptide. As this receptor is expressed on colorectal and pancreatic tumours, but not in normal tissue, these tumours are potentially new targets for PRRT with CCK8 and gastrin analogs.
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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.