ArticleEuropean journal of nuclear medicine and molecular imaging2011
Development of a potent DOTA-conjugated bombesin antagonist for targeting GRPr-positive tumours.
Article in European journal of nuclear medicine and molecular imaging, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 76 papers.
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Who cites it
76 citing papers in PubMed, 198 citations in OpenAlex.
- Comparison ofJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2023Trial
- 68Ga-NOTA-Aca-BBN(7-14) PET/CT in Healthy Volunteers and Glioma Patients.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2016Trial
- GRPR-Targeted Radionuclide Conjugates: A Molecular Evolution Perspective.Chemistry & biodiversity · 2026Review
- Radionuclide-based pharmaceuticals for breast cancer imaging: state of the art.EJNMMI radiopharmacy and chemistry · 2026Review
- A true theranostic pair -European journal of nuclear medicine and molecular imaging · 2026Article
- Exploring the theranostic potential of two metabolically stable GRPR-targeting peptides labelled with Ga-68 for PET imaging.EJNMMI radiopharmacy and chemistry · 2026Article
- Preclinical Evaluation of aACS pharmacology & translational science · 2026Article
- The gastrin-releasing peptide receptor in oncology: a comprehensive review of recent advances in targeted radionuclide theranostics.Frontiers in oncology · 2026Review
- FunctionalACS bio & med chem Au · 2025Article
- Studies on the impact of modifications at the Gln-Trp site in RM2-based GRPR ligands.EJNMMI research · 2025Article
- A preclinical study on the influence of linkers in [EJNMMI research · 2025Article
- Emerging PET Imaging Agents and Targeted Radioligand Therapy: A Review of Clinical Applications and Trials.Tomography (Ann Arbor, Mich.) · 2025Review
- Towards Dual-Tracer SPECT for Prostate Cancer Imaging Using [Pharmaceuticals (Basel, Switzerland) · 2025Article
- [Physical and engineering sciences in medicine · 2025Article
- Evaluation of maSSS/maSES-PEG2-RM26 for their potential therapeutic use after labeling with Re-188. Could their [EJNMMI radiopharmacy and chemistry · 2025Article
- Radiopharmaceuticals and their applications in medicine.Signal transduction and targeted therapy · 2025Review
- Gastrin-releasing peptide receptor (GRPR) as a novel biomarker and therapeutic target in prostate cancer.Annals of medicine · 2024Review
- Synthesis and Preclinical Evaluation of a Bispecific PSMA-617/RM2 Heterodimer Targeting Prostate Cancer.ACS medicinal chemistry letters · 2024Article
- Preclinical Investigation of [Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2024Article
- Bimodal MRI/Fluorescence Nanoparticle Imaging Contrast Agent Targeting Prostate Cancer.Nanomaterials (Basel, Switzerland) · 2024Article
16 more citing papers are in PubMed but not listed here.
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Authors and funding
9 authors at 4 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeRadiolabelled somatostatin-based antagonists show a higher uptake in tumour-bearing mouse models than agonists of similar or even distinctly higher receptor affinity. Very similar results were obtained with another family of G protein-coupled receptor ligands, the bombesin family. We describe a new conjugate, RM2, with the chelator DOTA coupled to D-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH(2) via the cationic spacer 4-amino-1-carboxymethyl-piperidine for labelling with radiometals such as (111)In and (68)Ga.
methodsRM2 was synthesized on a solid support and evaluated in vitro in PC-3 cells. IC(50) and K(d) values were determined. The antagonist potency was evaluated by immunofluorescence-based internalization and Ca(2+) mobilization assays. Biodistribution studies were performed in PC-3 and LNCaP tumour-bearing mice with (111)In-RM2 and (68)Ga-RM2, respectively. PET/CT studies were performed on PC-3 and LNCaP tumour-bearing nude mice with (68)Ga-RM2.
resultsRM2 and (111)In-RM2 are high-affinity and selective ligands for the GRP receptor (7.7 ± 3.3 nmol/l for RM2; 9.3 ± 3.3 nmol/l for (nat)In-RM2). The potent antagonistic properties were confirmed by an immunofluorescence-based internalization and Ca(2+) mobilization assays. (68)Ga- and (111)In-RM2 showed high and specific uptake in both the tumour and the pancreas. Uptake in the tumour remained high (15.2 ± 4.8%IA/g at 1 h; 11.7 ± 2.4%IA/g at 4 h), whereas a relatively fast washout from the pancreas and the other abdominal organs was observed. Uptake in the pancreas decreased rapidly from 22.6 ± 4.7%IA/g at 1 h to 1.5 ± 0.5%IA/g at 4 h.
conclusionRM2 was shown to be a potent GRPr antagonist. Pharmacokinetics and imaging studies indicate that (111)In-RM2 and (68)Ga-RM2 are ideal candidates for clinical SPECT and PET studies.
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