Abstract
A variety of bioorthogonal chemical tools have been developed and widely used in the study of biological phenomena in situ. Tetrazine bioorthogonal chemistry exhibits ultrafast reaction kinetics, excellent biocompatibility, and precise optical regulatory capabilities. Fluorogenic tetrazine bioorthogonal probes have achieved particularly diverse applications in bioimaging and disease diagnosis and treatment. This Viewpoint briefly introduces the characteristics and advantages of tetrazine bioorthogonal chemistry, some design strategies of fluorogenic tetrazine probes, and the status of applications of these tools to in vivo imaging, as well as disease diagnosis and treatment. Finally, we discuss challenges and propose future trends in the field of fluorogenic tetrazine probes. This Viewpoint offers insights into the development of new bioorthogonal tools for chemical biology research and for the design of new drugs.