Show simple item record

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

hal.structure.identifierInstitut des Sciences Moléculaires [ISM]
dc.contributor.authorCORNILLEAU, Thomas
dc.contributor.authorSIMONSEN, M.
hal.structure.identifierChimie et Biologie des Membranes et des Nanoobjets [CBMN]
dc.contributor.authorVANG, Maylou
hal.structure.identifierChimie et Biologie des Membranes et des Nanoobjets [CBMN]
dc.contributor.authorTAIB MAAMAR, Nada
hal.structure.identifierChimie et Biologie des Membranes et des Nanoobjets [CBMN]
dc.contributor.authorDESSOLIN, Jean
dc.contributor.authorAUDRAIN, H.
hal.structure.identifierInstitut des Sciences Moléculaires [ISM]
dc.contributor.authorHERMANGE, Philippe
hal.structure.identifierInstitut des Sciences Moléculaires [ISM]
dc.contributor.authorFOUQUET, Eric
dc.date.accessioned2020-07-09T14:17:02Z
dc.date.available2020-07-09T14:17:02Z
dc.date.issued2017-11
dc.identifier.issn1043-1802
dc.identifier.urihttps://oskar-bordeaux.fr/handle/20.500.12278/10338
dc.description.abstractEnThe 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.
dc.title.enLast-Step Pd-Mediated C-11 CO Labeling of a Moxestrol-Conjugated o-lodobenzyl Alcohol: From Model Experiments to in Vivo Positron Emission Tomography Studies
dc.typeArticle de revue
dc.identifier.doi10.1021/acs.bioconjchem.7b00583
dc.subject.halChimie/Matériaux
bordeaux.journalBioconjugate Chemistry
bordeaux.page2887-2894
bordeaux.volume28
bordeaux.hal.laboratoriesInstitut de Chimie & de Biologie des Membranes & des Nano-objets (CBMN) - UMR 5248*
bordeaux.hal.laboratoriesInstitut de Chimie & de Biologie des Membranes & des Nano-objets (CBMN, UMR 5248)
bordeaux.issue11
bordeaux.institutionUniversité de Bordeaux
bordeaux.institutionBordeaux INP
bordeaux.COinSctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=Bioconjugate%20Chemistry&rft.date=2017-11&rft.volume=28&rft.issue=11&rft.spage=2887-2894&rft.epage=2887-2894&rft.eissn=1043-1802&rft.issn=1043-1802&rft.au=CORNILLEAU,%20Thomas&SIMONSEN,%20M.&VANG,%20Maylou&TAIB%20MAAMAR,%20Nada&DESSOLIN,%20Jean&rft.genre=article


Files in this item

FilesSizeFormatView

There are no files associated with this item.

This item appears in the following Collection(s)

Show simple item record