Trivalent Gd-DOTA reagents for modification of proteins. Issue 116 (11th November 2015)

• Record Type: Journal Article
• Authors: Fisher, Martin J.; Williamson, Daniel J.; Burslem, George M.; Plante, Jeffrey P.; Manfield, Iain W.; Tiede, Christian; Ault, James R.; Stockley, Peter G.; Plein, Sven; Maqbool, Azhar; Tomlinson, Darren C.; Foster, Richard; Warriner, Stuart L.; Bon, Robin S.
• Is Part Of: RSC advances. Volume 5:Issue 116(2015)
• Page Start: 96194
• Page End: 96200
• Publication Date: 2015-11-11
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1039/c5ra20359g
• Languages: English
• ISSNs: 2046-2069

Abstract

Abstract : 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 without losing affinity for the target proteins. Abstract : 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.