Abstract
Cerenkov radiation (CR) from radionuclides and megavoltage X-ray radiation can act as an in situ light source for deep cancer theranostics, overcoming the limitations of external light sources. Despite the blue-weighted emission and low quantum yield of CR, activatable probes-mediated CR can enhance the in-vivo diagnostic signals by Cerenkov resonance energy transfer and also can produce therapeutic effects by reactive species generation/drug release, greatly promoting the biomedical applications of CR. In this review, we describe the principles and sources of CR, construction of CR-activated probes and their application to tumor optical imaging and therapy. Finally, future prospects for the design and biomedical application of CR-activated probes are discussed.