Journal
RSC ADVANCES
Volume 5, Issue 116, Pages 96194-96200Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c5ra20359g
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Funding
- British Heart Foundation [NH/12/1/29382]
- Leeds Teaching Hospitals Charitable Foundation [3T92/1203]
- British Heart Foundation [NH/12/1/29382] Funding Source: researchfish
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The development of novel protein-targeted MRI contrast agents crucially depends on the ability to derivatise suitable targeting moieties with a high payload of relaxation enhancer (e.g., gadolinium(III) complexes such as Gd-DOTA), without losing affinity for the target proteins. Here, we report robust synthetic procedures for the preparation of trivalent Gd-DOTA reagents with various chemical handles for site-specific modification of biomolecules. The reagents were shown to successfully label proteins through isothiocyanate ligation or through site-specific thiol-maleimide ligation and strain-promoted azide-alkyne cycloaddition.
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