1. Synthesis and characterization of monophosphinic acid DOTA derivative: A smart tool with functionalities for multimodal imaging
- Author
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Lionel Larbanoix, Ondrej Zemek, Sophie Laurent, Sébastien Boutry, Jan Kotek, Robert N. Muller, Coralie Sclavons, Luce Vander Elst, Satya Narayana Murthy Chilla, and Ivan Lukeš
- Subjects
Steric effects ,Stereochemistry ,Clinical Biochemistry ,Contrast Media ,Pharmaceutical Science ,Peptide ,Inner sphere electron transfer ,010402 general chemistry ,Multimodal Imaging ,01 natural sciences ,Biochemistry ,Heterocyclic Compounds, 1-Ring ,Mice ,Structure-Activity Relationship ,chemistry.chemical_compound ,In vivo ,Drug Discovery ,Animals ,DOTA ,Bifunctional ,Molecular Biology ,Multimodal imaging ,chemistry.chemical_classification ,Dose-Response Relationship, Drug ,Molecular Structure ,010405 organic chemistry ,Organic Chemistry ,Magnetic Resonance Imaging ,0104 chemical sciences ,chemistry ,Molecular Medicine ,Female ,Conjugate - Abstract
A new facile synthetic strategy was developed to prepare bifunctional monophosphinic acid Ln-DOTA derivatives, Gd-DO2AGAPNBn and Gd- DO2AGAPABn. 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 DO2AGAPNBn were appended in trans positions and are designed to conjugate identical or different vectors according to the potential applications. The conjugation of Gd-DO2AGAPABn with E3 peptide known to target apoptosis was successfully performed and in vivo MRI allowed cell death detection in a mouse model.
- Published
- 2017
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