MA-NOTMP: A Triazacyclononane Trimethylphosphinate Based Bifunctional Chelator for Gallium Radiolabelling of Biomolecules

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TitreMA-NOTMP: A Triazacyclononane Trimethylphosphinate Based Bifunctional Chelator for Gallium Radiolabelling of Biomolecules
Type de publicationJournal Article
Year of Publication2015
AuteursPoty S, Desogere P, Simecek J, Bernhard C, Goncalves V, Goze C, Boschetti F, Notni J, Wester HJ, Denat F
JournalCHEMMEDCHEM
Volume10
Pagination1475-1479
Date PublishedSEP
Type of ArticleArticle
ISSN1860-7179
Mots-clésbombesin, 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.

DOI10.1002/cmdc.201500198