Pretargeted imaging using bioorthogonal chemistry in mice

Following the successful application of in vivo chemistry in chemical biology there has been growing interest in extending the application scope to non-invasive molecular imaging and therapy in living animals and eventually humans. A typical example of such an application is pretargeted radioimmuno-imaging and -therapy: the tumor targeting of a tagged antibody followed by administration and binding of a small radiolabeled probe to the tag of the tumor-bound antibody. In this review, we describe the requirements to take the step to non-invasive applications in animals, summarize recent achievements in this field, and we offer a perspective on future developments.