Fiche publication
Date publication
septembre 2015
Journal
ChemMedChem
Auteurs
Membres identifiés du Cancéropôle Est :
Pr DENAT Franck
,
Dr GONCALVES Victor
Tous les auteurs :
Poty S, Désogère P, Šimeček J, Bernhard C, Goncalves V, Goze C, Boschetti F, Notni J, Wester HJ, Denat F
Lien Pubmed
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 (68) Ga (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 (68) Ga 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.
Mots clés
Animals, Aza Compounds, chemistry, Bombesin, chemistry, Cerebral Cortex, metabolism, Chelating Agents, chemical synthesis, Chemistry Techniques, Synthetic, Gallium Radioisotopes, chemistry, Heterocyclic Compounds, 1-Ring, chemistry, Hydrogen-Ion Concentration, Isotope Labeling, methods, Organophosphorus Compounds, chemistry, Phosphinic Acids, chemistry, Piperidines, chemistry, Radiopharmaceuticals, chemistry, Rats, Receptors, Bombesin, metabolism, Temperature
Référence
ChemMedChem. 2015 Sep;10(9):1475-9
