ArticleJournal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry2016
Promising bifunctional chelators for copper 64-PET imaging: practical (64)Cu radiolabeling and high in vitro and in vivo complex stability.
Article in Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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26 citing papers in PubMed, 45 citations in OpenAlex.
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- Development of NOTA-based antibody-fragment labeling agent that reduces early renal radioactivity levels.EJNMMI radiopharmacy and chemistry · 2026Article
- CDCA-Derived NE3TA Conjugate for Liver-SelectiveACS omega · 2026Article
- Chemical Tools to Characterize the Coordination Chemistry of Radionuclides for Radiopharmaceutical Applications.Chemical reviews · 2025Review
- A Cursory Gaze at Solitary Radiopharmaceutical Chelators Incorporating Macrocyclic and Acyclic Moieties.Pharmaceutics · 2025Review
- Molecular targets and the emerging role of copper radionuclides in prostate cancer theranostics.EJNMMI research · 2025Review
- Radiolabeling and evaluation ofScientific reports · 2025Article
- Optimizing antibody PET imaging: a comparative preclinical analysis of nanobody and minibody-like PET tracers.European journal of nuclear medicine and molecular imaging · 2025Article
- Physicochemical Properties and Route of Systemic Delivery Control the In Vivo Dynamics and Breakdown of Radiolabeled Gold Nanostars.Small (Weinheim an der Bergstrasse, Germany) · 2023Article
- Molecular imaging of chemokine-like receptor 1 (CMKLR1) in experimental acute lung injury.Proceedings of the National Academy of Sciences of the United States of America · 2023Article
- Aβ-Targeting Bifunctional Chelators (BFCs) for Potential Therapeutic and PET Imaging Applications.International journal of molecular sciences · 2022Review
- Chelation of Theranostic Copper Radioisotopes with S-Rich Macrocycles: From Radiolabelling of Copper-64 to In Vivo Investigation.Molecules (Basel, Switzerland) · 2022Article
- The Chemical Scaffold of Theranostic Radiopharmaceuticals: Radionuclide, Bifunctional Chelator, and Pharmacokinetics Modifying Linker.Molecules (Basel, Switzerland) · 2022Review
- Pyridine-containing octadentate ligand NE3TA-PY for formation of neutral complex withJournal of inorganic biochemistry · 2021Article
- Radiolabelling of Extracellular Vesicles for PET and SPECT imaging.Nanotheranostics · 2021Review
- New Bifunctional Chelator 3p-ACS omega · 2020Article
- Article
- Evaluation of Pan-SSTRs Targeted Radioligand [ACS medicinal chemistry letters · 2020Article
- Site-specific antibody fragment conjugates for targeted imaging.Methods in enzymology · 2020Article
- Site-Specific Immuno-PET Tracer to Image PD-L1.Molecular pharmaceutics · 2019Article
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8 authors at 2 institutions in 1 country.
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Abstract
Positron emission tomography (PET) using copper-64 is a sensitive and non-invasive imaging technique for diagnosis and staging of cancer. A bifunctional chelator that can present rapid radiolabeling kinetics and high complex stability with (64)Cu is a critical component for targeted PET imaging. Bifunctional chelates 3p-C-NE3TA, 3p-C-NOTA, and 3p-C-DE4TA were evaluated for complexation kinetics and stability with (64)Cu in vitro and in vivo. Hexadentate 3p-C-NOTA and heptadentate 3p-C-NE3TA possess a smaller TACN-based macrocyclic backbone, while nonadentate 3p-C-DE4TA is constructed on a larger CYCLEN-based ring. The frequently explored chelates of (64)Cu, octadentate C-DOTA and hexadentate C-NOTA were also comparatively evaluated. Radiolabeling kinetics of bifunctional chelators with (64)Cu was assessed under mild conditions. All bifunctional chelates instantly bound to (64)Cu in excellent radiolabeling efficiency at room temperature. C-DOTA was less efficient in binding (64)Cu than all other chelates. All (64)Cu-radiolabeled bifunctional chelates remained stable in human serum without any loss of (64)Cu for 2 days. When challenged by an excess amount of EDTA, (64)Cu complexes of C-NOTA, 3p-C-NE3TA and 3p-C-NOTA were shown to be more stable than (64)Cu-C-DOTA and (64)Cu-3p-C-DE4TA. (64)Cu complexes of the new chelates 3p-C-NE3TA and 3p-C-NOTA displayed comparable in vitro and in vivo complex stability to (64)Cu-C-NOTA. In vivo biodistribution result indicates that the (64)Cu-radiolabeled complexes of 3p-C-NOTA and 3p-C-NE3TA possess excellent in vivo complex stability, while (64)Cu-3p-C-DE4TA was dissociated as evidenced by high renal and liver retention in mice. The results of in vitro and in vivo studies suggest that the bifunctional chelates 3p-C-NE3TA and 3p-C-NOTA offer excellent chelation chemistry with (64)Cu for potential PET imaging applications.
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