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 exter-nal triggers at the tumor sites to release imaging agents and cytotoxic drugs, thus offering many advan-tages 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. (c) 2023 Published by Elsevier B.V.

Automated summary

Theranostics has attracted great attention for its ability to combine real-time cancer diagnosis with efficient treatment. Activatable dual-functional molecular agents can be synthesized by combining imaging agents, therapeutic agents, stimuli-responsive linkers, and/or targeting molecules. These agents can be activated by overexpressed physiological stimuli or external triggers at tumor sites to release imaging agents and cytotoxic drugs, offering advantages such as a high signal-to-noise ratio, low toxicity, and improved therapeutic effects. This review summarizes recent advances in dual-functional molecular agents for cancer theranostics, including molecular designs, synthetic strategies, activatable mechanisms, and biomedical applications, as well as discussing challenges and opportunities in this field.