ArticleBioconjugate chemistry2015
p-SCN-Bn-HOPO: A Superior Bifunctional Chelator for (89)Zr ImmunoPET.
Article in Bioconjugate chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 58 papers.
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Who cites it
58 citing papers in PubMed.
- 89Zr-Trastuzumab PET/CT for Detection of Human Epidermal Growth Factor Receptor 2-Positive Metastases in Patients With Human Epidermal Growth Factor Receptor 2-Negative Primary Breast Cancer.Clinical nuclear medicine · 2017Trial
- Detection of HER2-Positive Metastases in Patients with HER2-Negative Primary Breast Cancer Using 89Zr-Trastuzumab PET/CT.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2016Trial
- Metal coordination at biological interfaces: Mechanisms, therapeutics, and translation.Materials today. Bio · 2026Review
- Oxidative Stability and Redox Coupling in 3,4,3-LI(1,2-HOPO)ACS electrochemistry · 2026Article
- Synthesis and Evaluation of D8W, an Octadentate Desferrioxamine Analogue with Enhanced Water Solubility Designed forMolecular pharmaceutics · 2026Article
- Coordination Chemistry of Emerging Meitner-Auger Electron-Emitting Radiometals for Targeted Radionuclide Therapy.Coordination chemistry reviews · 2025Article
- Isopeptidic Desferrioxamine Analogues: The Role of Hydroxamate Spacing for Chelation of ZrChemMedChem · 2025Article
- [ACS omega · 2025Article
- Novel Molecular Classification of Breast Cancer with PET Imaging.Medicina (Kaunas, Lithuania) · 2024Review
- Click Chemistry Enables [Bioconjugate chemistry · 2024Article
- Zirconium 89 and Copper 64 for ImmunoPET: From Antibody Bioconjugation and Radiolabeling to Molecular Imaging.Pharmaceutics · 2024Review
- Good practices forEJNMMI radiopharmacy and chemistry · 2024Review
- Bifunctional octadentate pseudopeptides as Zirconium-89 chelators for immuno-PET applications.EJNMMI radiopharmacy and chemistry · 2024Article
- Preparation of a Zirconium-89 Labeled Clickable DOTA Complex and Its Antibody Conjugate.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Sc-HOPO: A Potential Construct for Use in Radioscandium-Based Radiopharmaceuticals.Inorganic chemistry · 2023Article
- Metal-Ligand Interactions in Scandium Complexes with Radiopharmaceutical Applications.Inorganic chemistry · 2023Article
- Investigation of Two Zr-p-NOEuropean journal of inorganic chemistry · 2023Article
- Siderocalin fusion proteins enable a newRSC chemical biology · 2023Article
- Evaluation ofACS omega · 2023Article
- Probing Unexpected Reactivity in Radiometal Chemistry: Indium-111-Mediated Hydrolysis of Hybrid Cyclen-Hydroxypyridinone Ligands.Inorganic chemistry · 2023Article
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Authors and funding
8 authors.
Funding
Abstract
Zirconium-89 has an ideal half-life for use in antibody-based PET imaging; however, when used with the chelator DFO, there is an accumulation of radioactivity in the bone, suggesting that the (89)Zr(4+) cation is being released in vivo. Therefore, a more robust chelator for (89)Zr could reduce the in vivo release and the dose to nontarget tissues. Evaluation of the ligand 3,4,3-(LI-1,2-HOPO) demonstrated efficient binding of (89)Zr(4+) and high stability; therefore, we developed a bifunctional derivative, p-SCN-Bn-HOPO, for conjugation to an antibody. A Zr-HOPO crystal structure was obtained showing that the Zr is fully coordinated by the octadentate HOPO ligand, as expected, forming a stable complex. p-SCN-Bn-HOPO was synthesized through a novel pathway. Both p-SCN-Bn-HOPO and p-SCN-Bn-DFO were conjugated to trastuzumab and radiolabeled with (89)Zr. Both complexes labeled efficiently and achieved specific activities of approximately 2 mCi/mg. PET imaging studies in nude mice with BT474 tumors (n = 4) showed good tumor uptake for both compounds, but with a marked decrease in bone uptake for the (89)Zr-HOPO-trastuzumab images. Biodistribution data confirmed the lower bone activity, measuring 17.0%ID/g in the bone at 336 h for (89)Zr-DFO-trastuzumab while (89)Zr-HOPO-trastuzumab only had 2.4%ID/g. We successfully synthesized p-SCN-Bn-HOPO, a bifunctional derivative of 3,4,3-(LI-1,2-HOPO) as a potential chelator for (89)Zr. In vivo studies demonstrate the successful use of (89)Zr-HOPO-trastuzumab to image BT474 breast cancer with low background, good tumor to organ contrast, and, importantly, very low bone uptake. The reduced bone uptake seen with (89)Zr-HOPO-trastuzumab suggests superior stability of the (89)Zr-HOPO complex.
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