ArticlePharmaceutics2020
Heterodimeric Radiotracer Targeting PSMA and GRPR for Imaging of Prostate Cancer-Optimization of the Affinity towards PSMA by Linker Modification in Murine Model.
Article in Pharmaceutics, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers, 1 of them a synthesis that pooled it.
What it found
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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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
19 citing papers in PubMed, 1 synthesis or guideline pooled it, 31 citations in OpenAlex.
- Detection rate of gastrin-releasing peptide receptor (GRPr) targeted tracers for positron emission tomography (PET) imaging in primary prostate cancer: a systematic review and meta-analysis.Annals of nuclear medicine · 2024Pooled it
- The Role of Nuclear Medicine in Prostate Cancer.Diagnostics (Basel, Switzerland) · 2025Review
- Fibroblast activation protein targeting radiopharmaceuticals: From drug design to clinical translation.Acta pharmaceutica Sinica. B · 2025Review
- First-in-human experience with GRPR antagonist [EJNMMI research · 2025Article
- Synthesis and Preclinical Evaluation of a Bispecific PSMA-617/RM2 Heterodimer Targeting Prostate Cancer.ACS medicinal chemistry letters · 2024Article
- Influence of Molecular Design on the Tumor Targeting and Biodistribution of PSMA-Binding Tracers Labeled with Technetium-99m.International journal of molecular sciences · 2024Article
- Stabilizing Scaffold for Short Peptides Based on Knottins.Current cancer drug targets · 2024Article
- Recent Pre-Clinical Advancements in Nuclear Medicine: Pioneering the Path to a Limitless Future.Cancers · 2023Review
- The Application of Radiolabeled Targeted Molecular Probes for the Diagnosis and Treatment of Prostate Cancer.Korean journal of radiology · 2023Review
- Synthesis and Preclinical Evaluation of Three NovelMolecules (Basel, Switzerland) · 2023Article
- Article
- Application of targeted diagnosis of PSMA in the modality shift of prostate cancer diagnosis: a review.Frontiers in oncology · 2023Review
- Radiolabeled iron oxide nanoparticles functionalized with PSMA/BN ligands for dual-targeting of prostate cancer.Frontiers in nuclear medicine · 2023Article
- The Performance of FDA-Approved PET Imaging Agents in the Detection of Prostate Cancer.Biomedicines · 2022Review
- Development and Evaluation of a Peptide Heterodimeric Tracer Targeting CXCR4 and Integrin αPharmaceutics · 2022Article
- Design, Synthesis, and Evaluation of Linker-Optimised PSMA-Targeting Radioligands.Pharmaceutics · 2022Article
- Radiolabeled PSMA Inhibitors.Cancers · 2021Review
- Radiolabeled Bombesin Analogs.Cancers · 2021Review
- Molecular Imaging in Primary Staging of Prostate Cancer Patients: Current Aspects and Future Trends.Cancers · 2021Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
9 authors at 1 institution in 3 countries.
Funding
Abstract
Prostate-specific membrane antigen (PSMA) and gastrin-releasing peptide receptor (GRPR) are promising targets for molecular imaging of prostate cancer (PCa) lesions. Due to the heterogenic overexpression of PSMA and GRPR in PCa, a heterodimeric radiotracer with the ability to bind to both targets could be beneficial. Recently, our group reported the novel heterodimer BQ7800 consisting of a urea-based PSMA inhibitor, the peptide-based GRPR antagonist RM26 and NOTA chelator. The study reported herein, aimed to improve the affinity of BQ7800 towards PSMA by changing the composition of the two linkers connecting the PSMA- and GRPR-targeting motifs. Three novel heterodimeric analogues were synthesized by incorporation of phenylalanine in the functional linker of the PSMA-binding motif and/or shortening the PEG-linker coupled to RM26. The heterodimers were labeled with indium-111 and evaluated in vitro. In the competitive binding assay, BQ7812, featuring phenylalanine and shorter PEG-linker, demonstrated a nine-fold improved affinity towards PSMA. In the in vivo biodistribution study of [
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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.