ArticleTheranostics2011
F-Labeled GRPR Agonists and Antagonists: A Comparative Study in Prostate Cancer Imaging.
Article in Theranostics, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 41 papers, 1 of them a synthesis that pooled it.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
41 citing papers in PubMed, 1 synthesis or guideline pooled it, 82 citations in OpenAlex.
- Non-conventional and Investigational PET Radiotracers for Breast Cancer: A Systematic Review.Frontiers in medicine · 2022Pooled it
- 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
- Radionuclide-based pharmaceuticals for breast cancer imaging: state of the art.EJNMMI radiopharmacy and chemistry · 2026Review
- Synthesis and preclinical evaluation of gastrin releasing peptide receptor antagonist [EJNMMI radiopharmacy and chemistry · 2025Article
- Synthesis and Evaluation ofPharmaceuticals (Basel, Switzerland) · 2025Article
- Unnatural amino acid substitutions to improve in vivo stability and tumor uptake ofEJNMMI radiopharmacy and chemistry · 2024Article
- A prospective comparative study of [European journal of nuclear medicine and molecular imaging · 2023Article
- An Overview of In Vitro Assays ofDiagnostics (Basel, Switzerland) · 2023Review
- Article
- Review
- Production, Purification, and Applications of a Potential Theranostic Pair: Cobalt-55 and Cobalt-58m.Diagnostics (Basel, Switzerland) · 2021Review
- In Vitro Evaluation and Biodistribution Studies of HPMA Copolymers Targeting the Gastrin Releasing Peptide Receptor in Prostate Cancer.Pharmaceutical research · 2020Article
- Radiofluorinated GPC3-Binding Peptides for PET Imaging of Hepatocellular Carcinoma.Molecular imaging and biology · 2020Article
- A Comprehensive Review of Non-Covalent Radiofluorination Approaches Using Aluminum [Molecules (Basel, Switzerland) · 2019Review
- Comparative Study of Subcutaneous and Orthotopic Mouse Models of Prostate Cancer: Vascular Perfusion, Vasculature Density, Hypoxic Burden and BB2r-Targeting Efficacy.Scientific reports · 2019Article
- Targeting HER2-positive gastric cancer with a novelRSC advances · 2019Article
- Bombesin receptor-targeted liposomes for enhanced delivery to lung cancer cells.Beilstein journal of nanotechnology · 2019Article
- Prostate Cancer Theranostics Targeting Gastrin-Releasing Peptide Receptors.Molecular imaging and biology · 2018Review
- PET Using a GRPR AntagonistJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2018Article
- Positron Emission Tomography Imaging of Prostate Cancer with Ga-68-Labeled Gastrin-Releasing Peptide Receptor Agonist BBNBioconjugate chemistry · 2018Article
Corrections and comments
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Authors and funding
10 authors at 5 institutions in 3 countries.
Funding
Abstract
Radiolabeled bombesin analogs are promising probes for cancer imaging of gastrin-releasing peptide receptor (GRPR). In this study, we developed (18)F-labeled GRPR agonists and antagonists for positron emission tomography (PET) imaging of prostate cancer. GRPR antagonists ATBBN (D-Phe-Gln-Trp-Ala-Val-Gly-His-Leu-NHCH(2)CH(3)) and MATBBN (Gly-Gly-Gly-Arg-Asp-Asn-D-Phe-Gln-Trp-Ala-Val-Gly-His-Leu-NHCH(2)CH(3)), and agonists AGBBN (Gln-Trp-Ala-Val-Gly-His-Leu-MetNH(2)) and MAGBBN (Gly-Gly-Gly-Arg-Asp-Asn-Gln-Trp-Ala-Val-Gly-His-Leu-MetNH(2)) were radiolabeled with (18)F via 4-nitrophenyl 2-(18)F-fluoropropionate. The in vitro receptor binding, cell uptake, and efflux properties of the radiotracers were studied on PC-3 cells. An in vivo PET study was performed on mice bearing PC-3 tumors. Direct (18)F-labeling of known GRPR antagonist ATBBN and agonist AGBBN did not result in good tumor targeting or appropriate pharmacokinetics. Modification was made by introducing a highly hydrophilic linker Gly-Gly-Gly-Arg-Asp-Asn. Higher receptor binding affinity, much higher cell uptake and slower washout were observed for the agonist (18)F-FP-MAGBBN over the antagonist (18)F-FP-MATBBN. Both tracers showed good tumor/background contrast, with the agonist (18)F-FP-MAGBBN having significantly higher tumor uptake than the antagonist (18)F-FP-MATBBN (P < 0.01). In conclusion, Gly-Gly-Gly-Arg-Asp-Asn linker significantly improved the pharmacokinetics of the otherwise hydrophobic BBN radiotracers. (18)F-labeled BBN peptide agonists may be the probes of choice for prostate cancer imaging due to their relatively high tumor uptake and retention as compared with the antagonist counterparts.
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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.