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Int. J. Mol. Sci. 2017, 18(1), 116; doi:10.3390/ijms18010116

Hydroxypyridinone Chelators: From Iron Scavenging to Radiopharmaceuticals for PET Imaging with Gallium-68

1
Division of Imaging Sciences and Biomedical Engineering, King’s College London, Fourth Floor Lambeth Wing, St. Thomas’ Hospital, London SE1 7EH, UK
2
Institute of Pharmaceutical Science, King’s College London, Franklin-Wilkins Building, 150 Stamford Street, London SE1 9NH, UK
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Academic Editors: Jamal Zweit and Sundaresan Gobalakrishnan
Received: 2 November 2016 / Revised: 5 December 2016 / Accepted: 21 December 2016 / Published: 8 January 2017
(This article belongs to the Special Issue Cancer Molecular Imaging in the Era of Precision Medicine)

Abstract

Derivatives of 3,4-hydroxypyridinones have been extensively studied for in vivo Fe3+ sequestration. Deferiprone, a 1,2-dimethyl-3,4-hydroxypyridinone, is now routinely used for clinical treatment of iron overload disease. Hexadentate tris(3,4-hydroxypyridinone) ligands (THP) complex Fe3+ at very low iron concentrations, and their high affinities for oxophilic trivalent metal ions have led to their development for new applications as bifunctional chelators for the positron emitting radiometal, 68Ga3+, which is clinically used for molecular imaging in positron emission tomography (PET). THP-peptide bioconjugates rapidly and quantitatively complex 68Ga3+ at ambient temperature, neutral pH and micromolar concentrations of ligand, making them amenable to kit-based radiosynthesis of 68Ga PET radiopharmaceuticals. 68Ga-labelled THP-peptides accumulate at target tissue in vivo, and are excreted largely via a renal pathway, providing high quality PET images. View Full-Text
Keywords: hydroxypyridinone; deferiprone; gallium; iron overload; positron emission tomography; molecular imaging; bifunctional chelators hydroxypyridinone; deferiprone; gallium; iron overload; positron emission tomography; molecular imaging; bifunctional chelators
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Cusnir, R.; Imberti, C.; Hider, R.C.; Blower, P.J.; Ma, M.T. Hydroxypyridinone Chelators: From Iron Scavenging to Radiopharmaceuticals for PET Imaging with Gallium-68. Int. J. Mol. Sci. 2017, 18, 116.

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