Journal article
M. Deri, S. Ponnala, B. Zeglis, G. Pohl, J. Dannenberg, Jason S. Lewis, L. Francesconi
Journal of medicinal chemistry, 2014
Journal of medicinal chemistry, 2014
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APA
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Deri, M., Ponnala, S., Zeglis, B., Pohl, G., Dannenberg, J., Lewis, J. S., & Francesconi, L. (2014). Alternative Chelator for 89Zr Radiopharmaceuticals: Radiolabeling and Evaluation of 3,4,3-(LI-1,2-HOPO). Journal of Medicinal Chemistry.
Chicago/Turabian
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Deri, M., S. Ponnala, B. Zeglis, G. Pohl, J. Dannenberg, Jason S. Lewis, and L. Francesconi. “Alternative Chelator for 89Zr Radiopharmaceuticals: Radiolabeling and Evaluation of 3,4,3-(LI-1,2-HOPO).” Journal of medicinal chemistry (2014).
MLA
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Deri, M., et al. “Alternative Chelator for 89Zr Radiopharmaceuticals: Radiolabeling and Evaluation of 3,4,3-(LI-1,2-HOPO).” Journal of Medicinal Chemistry, 2014.
BibTeX Click to copy
@article{m2014a,
title = {Alternative Chelator for 89Zr Radiopharmaceuticals: Radiolabeling and Evaluation of 3,4,3-(LI-1,2-HOPO)},
year = {2014},
journal = {Journal of medicinal chemistry},
author = {Deri, M. and Ponnala, S. and Zeglis, B. and Pohl, G. and Dannenberg, J. and Lewis, Jason S. and Francesconi, L.}
}
Abstract
Zirconium-89 is an effective radionuclide for antibody-based positron emission tomography (PET) imaging because its physical half-life (78.41 h) matches the biological half-life of IgG antibodies. Desferrioxamine (DFO) is currently the preferred chelator for 89Zr4+; however, accumulation of 89Zr in the bones of mice suggests that 89Zr4+ is released from DFO in vivo. An improved chelator for 89Zr4+ could eliminate the release of osteophilic 89Zr4+ and lead to a safer PET tracer with reduced background radiation dose. Herein, we present an octadentate chelator 3,4,3-(LI-1,2-HOPO) (or HOPO) as a potentially superior alternative to DFO. The HOPO ligand formed a 1:1 Zr-HOPO complex that was evaluated experimentally and theoretically. The stability of 89Zr-HOPO matched or surpassed that of 89Zr-DFO in every experiment. In healthy mice, 89Zr-HOPO cleared the body rapidly with no signs of demetalation. Ultimately, HOPO has the potential to replace DFO as the chelator of choice for 89Zr-based PET imaging agents.
