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MA‐NOTMP: A Triazacyclononane Trimethylphosphinate Based Bifunctional Chelator for Gallium Radiolabelling of Biomolecules
Author(s) -
Poty Sophie,
Désogère Pauline,
Šimeček Jakub,
Bernhard Claire,
Goncalves Victor,
Goze Christine,
Boschetti Frédéric,
Notni Johannes,
Wester Hans J.,
Denat Franck
Publication year - 2015
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201500198
Subject(s) - bifunctional , chemistry , chelation , biomolecule , gallium , labelling , combinatorial chemistry , ligand (biochemistry) , in vivo , phosphinate , in vitro , radiochemistry , biochemistry , organic chemistry , receptor , microbiology and biotechnology , fire retardant , biology , catalysis
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.