New Bifunctional Chelators Incorporating Dibromomaleimide Groups for Radiolabeling of Antibodies with Positron Emission Tomography Imaging Radioisotopes.

ABSTRACT: Positron Emission Tomography (PET) imaging with antibody-based contrast agents frequently uses the radioisotopes [⁶⁴Cu]Cu²⁺ and [⁸⁹Zr]Zr⁴⁺. The macrobicyclic chelator commonly known as sarcophagine (sar) is ideal for labeling receptor-targeted biomolecules with [⁶⁴Cu]Cu²⁺. The siderophore chelator, desferrioxamine-B (dfo), has been widely used to incorporate [⁸⁹Zr]Zr⁴⁺ into antibodies. Here, we describe new bifunctional chelators of sar and dfo: these chelators have been functionalized with dibromomaleimides (dbm), that enable site-specific and highly stable attachment of molecular cargoes to reduced, solvent-accessible, interstrand native disulfide groups. The new sar-dbm and dfo-dbm derivatives can be

SUBMITTER: Farleigh M 

PROVIDER: S-EPMC8299457 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature