CORNILLEAU, Thomas; SIMONSEN, M.; VANG, Maylou; TAIB MAAMAR, Nada; DESSOLIN, Jean; AUDRAIN, H.; HERMANGE, Philippe; FOUQUET, Eric

doi:10.1021/acs.bioconjchem.7b00583

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CORNILLEAU, Thomas

Institut des Sciences Moléculaires [ISM]

SIMONSEN, M.

VANG, Maylou
Chimie et Biologie des Membranes et des Nanoobjets [CBMN]

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Bioconjugate Chemistry. 2017-11, vol. 28, n° 11, p. 2887-2894

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The fast, efficient, and functional group tolerant last-step radiolabeling of bioconjugates is crucial for positron emission tomography (PET) applications. In this context, o-iodobenzyl alcohol based structures were identified as ideal tags for an easy Pd-catalyzed carbonylation after bioconjugation, and a moxestrol-conjugated precursor was chosen as the model compound for the further studies. Despite scale and time constraints, conditions developed with [C-12]CO and [C-13]CO were easily transferred to the C-11 isotope, and the desired radioactive product was obtained in amounts up to 740 MBq with radiochemical purities higher than 99%. Radio-high-performance liquid chromatography analyses of rat blood samples demonstrated excellent in vivo stability within the time of the acquisition. MicroPET-magnetic resonance imaging showed excretion pathways similar to moxestrol, and molecular modeling was also performed to evaluate the potential ability of this conjugate to bind estrogen receptors alpha. Thus, being both synthetically and biologically suitable, this strategy clears the path to potential novel biotracers for preclinical PET imaging.< Réduire

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Last-Step Pd-Mediated C-11 CO Labeling of a Moxestrol-Conjugated o-lodobenzyl Alcohol: From Model Experiments to in Vivo Positron Emission Tomography Studies

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