Site-Specific ⁶⁸Ga Radiolabeling of Trastuzumab Fab via Methionine for ImmunoPET Imaging.

ABSTRACT: Bioconjugates of antibodies and their derivatives radiolabeled with β⁺-emitting radionuclides can be utilized for diagnostic PET imaging. Site-specific attachment of radioactive cargo to antibody delivery vectors provides homogeneous, well-defined immunoconjugates. Recent studies have demonstrated the utility of oxaziridine chemistry for site-specific labeling of methionine residues. Herein, we applied this approach to site-specifically radiolabel trastuzumab-derived Fab immunoconjugates with ⁶⁸Ga, which can be used for in vivo PET imaging of HER2-positive breast cancer tumors. Initially, a reactive azide was introduced to a single solvent-accessible methionine residue in both the wild-type Fab and an engineered derivative containing methionine residue M74, utilizing

SUBMITTER: Yue TTC 

PROVIDER: S-EPMC10587866 | biostudies-literature | 2023 Oct

REPOSITORIES: biostudies-literature