ArticleNuclear medicine and biology2014
Synthesis and biological evaluation of copper-64 radiolabeled [DUPA-6-Ahx-(NODAGA)-5-Ava-BBN(7-14)NH2], a novel bivalent targeting vector having affinity for two distinct biomarkers (GRPr/PSMA) of prostate cancer.
Article in Nuclear medicine and biology, 2014. 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, 54 citations in OpenAlex.
- Design, Synthesis, and Preclinical Evaluation of Novel Dimeric RM2-Based Radioligands for GRPR-Targeted Breast Cancer Imaging.Molecular pharmaceutics · 2026Article
- A Siderophore-Antibiotic Heterodimer Imaging Agent EnablesJournal of medicinal chemistry · 2026Article
- Molecular targets and the emerging role of copper radionuclides in prostate cancer theranostics.EJNMMI research · 2025Review
- NOTA and NODAGA Radionuclide Complexing Agents: Versatile Approaches for Advancements in Radiochemistry.Molecules (Basel, Switzerland) · 2025Review
- Elevating theranostics: The emergence and promise of radiopharmaceutical cell-targeting heterodimers in human cancers.iRadiology · 2024Article
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- Radiolabeled PSMA Inhibitors.Cancers · 2021Review
- The Importance of 6-Aminohexanoic Acid as a Hydrophobic, Flexible Structural Element.International journal of molecular sciences · 2021Review
- Enzyme-responsive polymeric micelles of cabazitaxel for prostate cancer targeted therapy.Acta biomaterialia · 2020Article
- Current State of Radiolabeled Heterobivalent Peptidic Ligands in Tumor Imaging and Therapy.Pharmaceuticals (Basel, Switzerland) · 2020Review
- Heterodimeric Radiotracer Targeting PSMA and GRPR for Imaging of Prostate Cancer-Optimization of the Affinity towards PSMA by Linker Modification in Murine Model.Pharmaceutics · 2020Article
- Development of NovelBiomolecules · 2020Article
- New Frontiers in Molecular Imaging Using Peptide-Based Radiopharmaceuticals for Prostate Cancer.Frontiers in chemistry · 2020Review
- The Future of PSMA-Targeted Radionuclide Therapy: An Overview of Recent Preclinical Research.Pharmaceutics · 2019Review
- Bispecific GRPR-Antagonistic Anti-PSMA/GRPR Heterodimer for PET and SPECT Diagnostic Imaging of Prostate Cancer.Cancers · 2019Article
- Synthesis and Preclinical Evaluation of Radio-Iodinated GRPR/PSMA Bispecific Heterodimers for the Theranostics Application in Prostate Cancer.Pharmaceutics · 2019Article
- Recent applications of a single quadrupole mass spectrometer inJournal of fluorine chemistry · 2018Article
- Radiolabeled bombesin derivatives for preclinical oncological imaging.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2017Review
- The therapeutic and diagnostic potential of the prostate specific membrane antigen/glutamate carboxypeptidase II (PSMA/GCPII) in cancer and neurological disease.British journal of pharmacology · 2016Review
- Bombesin related peptides/receptors and their promising therapeutic roles in cancer imaging, targeting and treatment.Expert opinion on therapeutic targets · 2016Review
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Authors and funding
12 authors at 2 institutions in 1 country.
Funding
Abstract
unlabelledGastrin-releasing peptide receptors (GRPr) and prostate-specific membrane antigen (PSMA) are two identifying biomarkers expressed in very high numbers on prostate cancer cells and could serve as a useful tool for molecular targeting and diagnosis of disease via positron-emission tomography (PET). The aim of this study was to produce the multipurpose, bivalent [DUPA-6-Ahx-((64)Cu-NODAGA)-5-Ava-BBN(7-14)NH2] radioligand for prostate cancer imaging, where DUPA = (2-[3-(1,3-dicarboxypropyl)-ureido]pentanedioic acid), a small-molecule, PSMA-targeting probe, 6Ahx = 6-aminohexanoic acid, 5-Ava = 5-aminovaleric acid, NODAGA = [2-(4,7-biscarboxymethyl)-1,4,7-(triazonan-1-yl)pentanedioic acid] (a derivative of NOTA (1,4,7-triazacyclononane-1,4,7-triacetic acid)), and BBN(7-14)NH2 = bombesin, a GRPr-specific peptide targeting probe.
methodsThe PSMA/GRPr dual targeting ligand precursor [DUPA-6-Ahx-K-5-Ava-BBN(7-14)NH2], was synthesized by solid-phase and manual peptide synthesis, after which NODAGA was added via manual conjugation to the ε-amine of lysine (K). The new bivalent GRPr/PSMA targeting vector was purified by reversed-phase high performance liquid chromatography (RP-HPLC), characterized by electrospray-ionization mass spectrometry (ESI-MS), and metallated with (64)CuCl2 and (nat)CuCl2. The receptor binding affinity was evaluated in human, prostate, PC-3 (GRPr-positive) and LNCaP (PSMA-positive) cells and the tumor-targeting efficacy determined in severe combined immunodeficient (SCID) and athymic nude mice bearing PC-3 and LNCaP tumors. Whole-body maximum intensity microPET/CT images of PC-3/LNCaP tumor-bearing mice were obtained 18 h post-injection (p.i.).
resultsCompetitive binding assays in PC-3 and LNCaP cells indicated high receptor binding affinity for the [DUPA-6-Ahx-((nat)Cu-NODAGA)-5-Ava-BBN(7-14)NH2] conjugate. MicroPET scintigraphy in PC-3/LNCaP tumor-bearing mice indicated that xenografted tumors were visible at 18h p.i. with collateral, background radiation also being observed in non-target tissue.
conclusionsDUPA-6-Ahx-((64)Cu-NODAGA)-5-Ava-BBN(7-14)NH2] targeting vector, as described herein, is the first example of a dual GRPr-/PSMA-targeting radioligand for molecular of imaging prostate tumors. Detailed in vitro studies and microPET molecular imaging investigations of [DUPA-6-Ahx-((64)Cu-NODAGA)-5-Ava-BBN(7-14)NH2 in tumor-bearing mice indicate that further studies are necessary to optimize uptake and retention of tracer in GRPr- and PSMA-positive tissues.
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