Trivalent Gd-DOTA reagents for modification of 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.

SUBMITTER: Fisher MJ 

PROVIDER: S-EPMC4786947 | biostudies-literature |

REPOSITORIES: biostudies-literature