Site-specific conjugation allows modulation of click reaction stoichiometry for pretargeted SPECT imaging.

ABSTRACT: Antibody pretargeting is a promising strategy for improving molecular imaging, wherein the separation in time of antibody targeting and radiolabeling can lead to rapid attainment of high contrast, potentially increased sensitivity, and reduced patient radiation exposure. The inverse electron demand Diels-Alder 'click' reaction between trans-cyclooctene (TCO) conjugated antibodies and radiolabeled tetrazines presents an ideal platform for pretargeted imaging due to rapid reaction kinetics, bioorthogonality, and potential for optimization of both slow and fast clearing components. Herein, we evaluated a series of anti-human epidermal growth factor receptor 2 (HER2) pretargeting antibodies containing distinct molar ratios of site-specifically incorporated TCO. The effect of stoichiometry on t

SUBMITTER: Mandikian D 

PROVIDER: S-EPMC6284555 | biostudies-literature | 2018 Nov-Dec

REPOSITORIES: biostudies-literature