ArticleEJNMMI research2012
A dimerized urea-based inhibitor of the prostate-specific membrane antigen for 68Ga-PET imaging of prostate cancer.
Article in EJNMMI research, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 70 papers.
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Who cites it
70 citing papers in PubMed, 165 citations in OpenAlex.
- Sarcosine-Based Pharmacokinetic Optimization and Fluorescent Dye Library Evaluation of Dual-Labeled PSMA Inhibitors for Fluorescence-Guided Surgery.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Lutetium-177 Radiolabeled Gold Nanoparticles for Prostate Cancer Theranostics.Nanomaterials (Basel, Switzerland) · 2026Article
- Preclinical Evaluation Study ofChemical & biomedical imaging · 2026Article
- A heterodimeric radioligand labeled with gallium-68 targeting fibroblast activation protein.EJNMMI research · 2025Article
- A comparison of routine [EJNMMI radiopharmacy and chemistry · 2024Article
- Development of a homotrimeric PSMA radioligand based on the NOTI chelating platform.EJNMMI radiopharmacy and chemistry · 2024Article
- [Diagnostics (Basel, Switzerland) · 2024Article
- The importance of tyrosines in multimers of cyclic RGD nonapeptides: towards αvβ6-integrin targeted radiotherapeutics.RSC medicinal chemistry · 2024Article
- Reliability and practicability of PSMA-RADS 1.0 for structured reporting of PSMA-PET/CT scans in prostate cancer patients.European radiology · 2024Article
- Synthesis,International journal of molecular sciences · 2023Article
- Preclinical Evaluation of a PSMA-Targeting Homodimer with an Optimized Linker for Imaging of Prostate Cancer.Molecules (Basel, Switzerland) · 2023Article
- A Dimeric FAP-Targeting Small-Molecule Radioconjugate with High and Prolonged Tumor Uptake.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2022Article
- Radiosynthesis and Preclinical Evaluation of Bispecific PSMA/FAP Heterodimers for Tumor Imaging.Pharmaceuticals (Basel, Switzerland) · 2022Article
- A New Class of PSMA-617-Based Hybrid Molecules for Preoperative Imaging and Intraoperative Fluorescence Navigation of Prostate Cancer.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Metamorphosis of prostate specific membrane antigen (PSMA) inhibitors.Biophysical reviews · 2022Review
- Imaging of Tumor-Associated Vascular Prostate-Specific Membrane Antigen in Woodchuck Model of Hepatocellular Carcinoma.Gastro hep advances · 2022Article
- Refined Chelator Spacer Moieties Ameliorate the Pharmacokinetics of PSMA-617.Frontiers in chemistry · 2022Article
- Radiolabeled PSMA Inhibitors.Cancers · 2021Review
- Pharmacokinetic studies of [European journal of nuclear medicine and molecular imaging · 2021Article
- Hybrid Chelator-Based PSMA Radiopharmaceuticals: Translational Approach.Molecules (Basel, Switzerland) · 2021Article
10 more citing papers are in PubMed but not listed here.
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Authors and funding
8 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
unlabelled
backgroundAlternative positron-emission tomography (PET) probes like labeled inhibitors of the prostate-specific membrane antigen (PSMA) are of emerging clinical impact as they show the ability to image small lesions of recurrent prostate cancer. Here, the dimerization of the pharmacophore Glu-ureido-Lys via the 68Ga chelator N,N'-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N'-diacetic acid (HBED-CC) was investigated to further improve the binding characteristics and pharmacokinetics.
methodsThe peptidomimetic structures were synthesized by solid-phase chemistry, and the resulting products were coupled with the respective 2,3,5,6-tetrafluorophenol esters of HBED-CC to form the monomeric reference and the dimeric Glu-ureido-Lys derivative. The binding properties were analyzed in competitive binding, internalization, and cell surface retention experiments. PET images and biodistribution data were obtained 1 h after injection in BALB/c nu/nu mice bearing LNCaP tumor xenografts.
resultsCell binding data revealed significant better binding properties of the dimer (IC50 = 3.9 ± 1.8 nM; IC50 (monomer) = 12.1 ± 2.1 nM). The inhibition potency investigated by the enzyme-based NAALADase assay confirmed these results. Specific internalization in LNCaP cells was demonstrated for both, the monomer and dimer. As shown by efflux measurements, the dimeric compound was more effectively retained on the cell surface, resulting in advanced in vivo properties (T/BMonomer = 9.2; T/BDimer = 26.5).
conclusionsThe dimeric [68Ga]7 is a promising imaging agent for PSMA-expressing tumors as it shows higher tumor uptake while observing more favorable background clearance. As compared to the respective monomer, the higher affinity and prolonged tumor retention additionally represent promising features and warrant further evaluation regarding 68Ga-PET imaging of PSMA expression.
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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.