MA‐NOTMP: A Triazacyclononane Trimethylphosphinate Based Bifunctional Chelator for Gallium Radiolabelling of Biomolecules |
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Authors: | Sophie Poty Dr. Pauline Désogère Dr. Jakub Šimeček Dr. Claire Bernhard Dr. Victor Goncalves Dr. Christine Goze Dr. Frédéric Boschetti Dr. Johannes Notni Prof. Dr. Hans J. Wester Prof. Dr. Franck Denat |
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Affiliation: | 1. ICMUB UMR6302, CNRS, Université Bourgogne Franche‐Comté, 21000 Dijon (France);2. Lehrstuhl für Pharmazeutische Radiochemie, Technische Universit?t, München, Walther‐Meissner‐Str.?3, 85748 Garching (Germany);3. Chematech, 9?Av. Alain Savary, BP?47870 21000 Dijon cedex (France) |
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Abstract: | In the past few years, gallium‐68 has demonstrated significant potential as a radioisotope for positron emission tomography (PET), and the optimization of chelators for gallium coordination is a major goal in the development of radiopharmaceuticals. Methylaminotriazacyclononane trimethylphosphinate (MA‐NOTMP), a new C‐functionalized triazacyclononane derivative with phosphinate pendant arms, presents excellent coordination properties for 68Ga (low ligand concentration, labelling at low pH even at room temperature). A “ready‐to‐be‐grafted” bifunctional chelating agent (p‐NCS‐Bz‐MA‐NOTMP) was prepared to allow 68Ga labelling of sensitive biological vectors. Conjugation to a bombesin(7–14) derivative was performed, and preliminary in vitro experiments demonstrated the potential of MA‐NOTMP in the development of radiopharmaceuticals. This new chelator is therefore of major interest for labelling sensitive biomolecules, and further in vivo experiments will soon be performed. |
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Keywords: | bombesin gallium phosphinates radiolabelling triazacyclononane |
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