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Synthesis and characterization of monophosphinic acid DOTA derivative: A smart tool with functionalities for multimodal imaging
SNM. Chilla, O. Zemek, J. Kotek, S. Boutry, L. Larbanoix, C. Sclavons, LV. Elst, I. Lukes, RN. Muller, S. Laurent,
Bioorganic & medicinal chemistry.
2017 ;
25 (16) :
4297-4303.
[pub] 20170615
Jazyk angličtina Země Anglie, Velká Británie
Typ dokumentu časopisecké články
Perzistentní odkaz
https://www.medvik.cz/link/bmc17030717
- MeSH
- heterocyklické sloučeniny monocyklické chemická syntéza chemie MeSH
- kontrastní látky chemická syntéza chemie MeSH
- magnetická rezonanční tomografie MeSH
- molekulární struktura MeSH
- multimodální zobrazování * MeSH
- myši MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- vztahy mezi strukturou a aktivitou MeSH
- zvířata MeSH
- Check Tag
- myši MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
A new facile synthetic strategy was developed to prepare bifunctional monophosphinic acid Ln-DOTA derivatives, Gd-DO2AGAP(NBn) and Gd- DO2AGAP(ABn). The relaxivities of the Gd-complexes are enhanced compared to Gd-DOTA. Monophosphinic acid arm of these Gd-complexes affords enhancement of inner sphere water exchange rate due to its steric bulkiness. The different functionalities of DO2AGAP(NBn) were appended in trans positions and are designed to conjugate identical or different vectors according to the potential applications. The conjugation of Gd-DO2AGAP(ABn) with E3 peptide known to target apoptosis was successfully performed and in vivo MRI allowed cell death detection in a mouse model.
Centre for Microscopy and Molecular Imaging Rue Adrienne Bolland 8 6041 Charleroi Gosselies Belgium
Department of Inorganic Chemistry Universita Karlova Hlavova 2030 128 40 Prague 2 Czech Republic
Citace poskytuje Crossref.org
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- $a Chilla, Satya Narayana Murthy $u Department of General, Organic and Biomedical Chemistry, NMR and Molecular Imaging Laboratory, University of Mons, Avenue Maistriau, 19, Mendeleïev Building, 7000 Mons, Belgium. Electronic address: satya.chilla@umons.ac.be.
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- $a A new facile synthetic strategy was developed to prepare bifunctional monophosphinic acid Ln-DOTA derivatives, Gd-DO2AGAP(NBn) and Gd- DO2AGAP(ABn). The relaxivities of the Gd-complexes are enhanced compared to Gd-DOTA. Monophosphinic acid arm of these Gd-complexes affords enhancement of inner sphere water exchange rate due to its steric bulkiness. The different functionalities of DO2AGAP(NBn) were appended in trans positions and are designed to conjugate identical or different vectors according to the potential applications. The conjugation of Gd-DO2AGAP(ABn) with E3 peptide known to target apoptosis was successfully performed and in vivo MRI allowed cell death detection in a mouse model.
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- $a Boutry, Sébastien $u Department of General, Organic and Biomedical Chemistry, NMR and Molecular Imaging Laboratory, University of Mons, Avenue Maistriau, 19, Mendeleïev Building, 7000 Mons, Belgium; Centre for Microscopy and Molecular Imaging (CMMI), Rue Adrienne Bolland, 8, 6041 Charleroi-Gosselies, Belgium.
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