Activatable dual-functional molecular agents for imaging-guided cancer therapy.

Theranostics has attracted great attention due to its ability to combine the real-time diagnosis of cancers with efficient treatment modalities. Activatable dual-functional molecular agents could be synthesized by covalently conjugating imaging agents, therapeutic agents, stimuli-responsive linkers and/or targeting molecules together. They could be selectively activated by overexpressed physiological stimuli or external triggers at the tumor sites to release imaging agents and cytotoxic drugs, thus offering many advantages for tumor imaging and therapy, such as a high signal-to-noise ratio, low systemic toxicity, and improved therapeutic effects. This review summarizes the recent advances of dual-functional molecular agents that respond to various physiological or external stimuli for cancer theranostics. The molecular designs, synthetic strategies, activatable mechanisms, and biomedical applications of these molecular agents are elaborated, followed by a brief discussion of the challenges and opportunities in this field.