MA‐NOTMP: A Triazacyclononane Trimethylphosphinate Based Bifunctional Chelator for Gallium Radiolabelling of Biomolecules. Issue 9 (1st June 2015)

• Record Type: Journal Article
• Authors: Poty, Sophie; Désogère, Pauline; Šimeček, Jakub; Bernhard, Claire; Goncalves, Victor; Goze, Christine; Boschetti, Frédéric; Notni, Johannes; Wester, Hans J.; Denat, Franck
• Is Part Of: ChemMedChem. Volume 10:Issue 9(2015:Sep.)
• Page Start: 1475
• Page End: 1479
• Publication Date: 2015-06-01
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.201500198
• Languages: English
• ISSNs: 1860-7179

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <p>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 (<italic>p</italic>‐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.</p> </abstract>