ArticleMolecular imaging and biology2015
Radiofluorination of PSMA-HBED via Al(18)F(2+) Chelation and Biological Evaluations In Vitro.
Article in Molecular imaging and biology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 51 citations in OpenAlex.
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- Fluorine-18 Labeled Urea-Based Ligands Targeting Prostate-Specific Membrane Antigen (PSMA) with Increased Tumor and Decreased Renal Uptake.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Radiolabeled PSMA Inhibitors.Cancers · 2021Review
- The aluminium-[EJNMMI radiopharmacy and chemistry · 2021Review
- One-pot and one-step automated radio-synthesis of [EJNMMI radiopharmacy and chemistry · 2021Article
- Intra-individual dynamic comparison ofScientific reports · 2020Article
- Rhenium(i) complexation-dissociation strategy for synthesising fluorine-18 labelled pyridine bidentate radiotracers.RSC advances · 2020Article
- Optimization of PET protocol and interrater reliability ofEJNMMI research · 2020Article
- Radiolabelled Peptides for Positron Emission Tomography and Endoradiotherapy in Oncology.Pharmaceuticals (Basel, Switzerland) · 2020Review
- A Comprehensive Review of Non-Covalent Radiofluorination Approaches Using Aluminum [Molecules (Basel, Switzerland) · 2019Review
- One-StepJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2019Article
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- Peripheral ganglia in healthy rats as target structures for the evaluation of PSMA imaging agents.BMC cancer · 2019Article
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- Synthesis and preclinical evaluation of novelEJNMMI research · 2018Article
- Synthesis of an AlEJNMMI radiopharmacy and chemistry · 2018Article
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6 authors at 1 institution in 1 country.
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No grant is acknowledged in the PubMed record.
Abstract
purposeGa-68-labeled prostate-specific membrane antigen (PSMA) ligands have been used clinically for positron emission tomography (PET) imaging of prostate cancer. However, F-18-labeled compounds offer several advantages, including the potential for delayed imaging, high starting activities enabling multidose preparation, and improved spatial resolution in PET. For F-18 labeling of peptides conjugated with a suitable chelator, a fast and feasible method is the use of [Al(18)F](2+). In the present study, the radiofluorinations of a well-known PSMA ligand Glu-NH-CO-NH-Lys(Ahx)-HBED-CC (PSMA-HBED) via [Al(18)F](2+) were performed with respect to various reaction parameters, along with the biological evaluations in a cell experiment. PROCEDURES: [Al(18)F]PSMA-HBED was prepared by adding Na[(18)F]F into a vial containing 0.026 μmol peptide (in 0.05 M NaOAc buffer) and 0.03 μmol AlCl3⋅6H2O (in 0.05 M NaOAc buffer). Then, it was stirred at different temperatures from 1 to 30 min. Afterwards, purification was carried out by solid phase extraction. Biological evaluations were performed in PSMA-positive cell lines LNCaP C4-2, along with a negative control using PC-3 cell lines.
resultsThe best labeling results (81 ± 0.5 %, n = 4) were observed with 0.026 μmol peptide (30 °C, 5 min). For preclinical experiments, the production of [Al(18)F]PSMA-HBED at 35 °C including purification by solid phase extraction (SPE) succeeded within 45 min, resulting in a radiochemical yield of 49 ± 1.2 % (decay-corrected, n = 6, radiochemical purity ≥98 %) at EOS. The labeled peptide revealed serum stability for 4 h as well as a promising binding coefficient (K D) value of 10.3 ± 2.2 nM in cell experiments with PSMA-positive LNCaP C4-2 cells.
conclusionAn efficient and one-pot method for the radiosynthesis of [Al(18)F]PSMA-HBED was developed (0.26 μmol of precursor at 35 °C). In cell culture studies, the K D suggests [Al(18)F]PSMA-HBED as a potential PSMA ligand for future investigations in vivo and clinical applications afterwards.
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