ArticleTheranostics2016
Evaluation of a 3-hydroxypyridin-2-one (2,3-HOPO) Based Macrocyclic Chelator for (89)Zr(4+) and Its Use for ImmunoPET Imaging of HER2 Positive Model of Ovarian Carcinoma in Mice.
Article in Theranostics, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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
29 citing papers in PubMed, 55 citations in OpenAlex.
- Preclinical Evaluation of a Radiolabeled Anti-PSMA Dimeric Aptamer in a Murine Model of Human Prostate Cancer.Molecules (Basel, Switzerland) · 2026Article
- Evaluation ofACS omega · 2023Article
- Probing Unexpected Reactivity in Radiometal Chemistry: Indium-111-Mediated Hydrolysis of Hybrid Cyclen-Hydroxypyridinone Ligands.Inorganic chemistry · 2023Article
- Toward OptimizedPharmaceutics · 2022Article
- Hydroxypyridinones as a Very Promising Platform for Targeted Diagnostic and Therapeutic Radiopharmaceuticals.Molecules (Basel, Switzerland) · 2021Review
- The Race for Hydroxamate-Based Zirconium-89 Chelators.Cancers · 2021Review
- Article
- Advances in Development of Radiometal Labeled Amino Acid-Based Compounds for Cancer Imaging and Diagnostics.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Exploring the Application of Bifunctional Metal Chelators in Treating Triple-Negative Breast Cancer.Frontiers in bioengineering and biotechnology · 2021Article
- Polyazamacrocycle Ligands FacilitateInorganic chemistry · 2020Article
- A High-Denticity Chelator Based on Desferrioxamine for Enhanced Coordination of Zirconium-89.Inorganic chemistry · 2020Article
- Imaging of Fibroblast Activation Protein Alpha Expression in a Preclinical Mouse Model of Glioma Using Positron Emission Tomography.Molecules (Basel, Switzerland) · 2020Article
- ImmunoPET: Concept, Design, and Applications.Chemical reviews · 2020Review
- Direct comparison of the in vitro and in vivo stability of DFO, DFO* and DFOcyclo* forEuropean journal of nuclear medicine and molecular imaging · 2019Article
- Article
- Preparation of Zirconium-89 Solutions for Radiopharmaceutical Purposes: Interrelation Between Formulation, Radiochemical Purity, Stability and Biodistribution.Molecules (Basel, Switzerland) · 2019Article
- A comprehensively revised strategy that improves the specific activity and long-term stability of clinically relevantDalton transactions (Cambridge, England : 2003) · 2018Article
- PET Imaging of Receptor Tyrosine Kinases in Cancer.Molecular cancer therapeutics · 2018Review
- Chemical aspects of metal ion chelation in the synthesis and application antibody-based radiotracers.Journal of labelled compounds & radiopharmaceuticals · 2018Review
- Recent Advances in Zirconium-89 Chelator Development.Molecules (Basel, Switzerland) · 2018Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
10 authors at 3 institutions in 2 countries.
Funding
Abstract
A novel octadentate 3-hydroxypyridin-2-one (2,3-HOPO) based di-macrocyclic ligand was evaluated for chelation of (89)Zr; subsequently, it was used as a bi-functional chelator for preparation of (89)Zr-labeled antibodies. Quantitative chelation of (89)Zr(4+) with the octadentate ligand forming (89)ZrL complex was achieved under mild conditions within 15 minutes. The (89)Zr-complex was stable in vitro in presence of DTPA, but a slow degradation was observed in serum. In vivo, the hydrophilic (89)Zr-complex showed prevalently renal excretion; and an elevated bone uptake of radioactivity suggested a partial release of (89)Zr(4+) from the complex. The 2,3-HOPO based ligand was conjugated to the monoclonal antibodies, HER2-specific trastuzumab and an isotypic anti-gD antibody, using a p-phenylene bis-isothiocyanate linker to yield products with an average loading of less than 2 chelates per antibody. Conjugated antibodies were labeled with (89)Zr under mild conditions providing the PET tracers in 60-69% yield. Despite the limited stability in mouse serum; the PET tracers performed very well in vivo. The PET imaging in mouse model of HER2 positive ovarian carcinoma showed tumor uptake of (89)Zr-trastuzumab (29.2 ± 12.9 %ID/g) indistinguishable (p = 0.488) from the uptake of positive control (89)Zr-DFO-trastuzumab (26.1 ± 3.3 %ID/g). In conclusion, the newly developed 3-hydroxypyridin-2-one based di-macrocyclic chelator provides a viable alternative to DFO-based heterobifunctional ligands for preparation of (89)Zr-labeled monoclonal antibodies for immunoPET studies.
Indexed as
Identifiers
What OpenQuestion holds
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.