MA-NOTMP: A Triazacyclononane Trimethylphosphinate Based Bifunctional Chelator for Gallium Radiolabelling of Biomolecules
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Titre | MA-NOTMP: A Triazacyclononane Trimethylphosphinate Based Bifunctional Chelator for Gallium Radiolabelling of Biomolecules |
Type de publication | Journal Article |
Year of Publication | 2015 |
Auteurs | Poty S, Desogere P, Simecek J, Bernhard C, Goncalves V, Goze C, Boschetti F, Notni J, Wester HJ, Denat F |
Journal | CHEMMEDCHEM |
Volume | 10 |
Pagination | 1475-1479 |
Date Published | SEP |
Type of Article | Article |
ISSN | 1860-7179 |
Mots-clés | bombesin, gallium, phosphinates, Radiolabelling, triazacyclononane |
Résumé | 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 Ga-68 (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 Ga-68 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. |
DOI | 10.1002/cmdc.201500198 |