Bioorthogonal coupling reactions are a powerful tool to create protein
conjugates within living systems without interfering with the native biochemical
environment. This reaction class has been increasingly utilized over the past few years
in the development of new radiopharmaceuticals for medical imaging and radiotherapy.
Pretargeting strategies have particularly benefited, where tissue-specific antibodies are
first allowed to localize to their target site before a radiolabeled molecule is
administered that can covalently bond with the antibody. These radionuclide delivery
systems can enhance therapeutic efficacy, reducing radiation exposure and increasing
image quality. Current applications of bioorthogonal coupling reactions in pretargeted
molecular imaging and radioimmunotherapy will be reviewed.
Keywords: Antibody labeling, Bioorthogonal coupling, Click chemistry, Inverse
electron demand Diels-Alder, PET imaging, Pretargeting, Radiotherapy,
Radiotracer, Staudinger ligation, Strain-promoted cycloaddition.
