2015 Volume 30 Issue 5 Pages 446-453
High-energy ionizing radiation is among the potential external triggers for precise control of the function and drug efficacy in living organisms, because the radiation reaction for activation of biomaterials can be regulated spatially and temporally without any additives. Herein, we demonstrated a radiation-activated prodrugs, the activities of which can be blocked by chemical modification, while their intrinsic activities are recovered by X-irradiation. Our studies illustrated that azidomethyl, indolequinone and disulfide groups have favorable functionalities for caging molecules and materials. We applied the prodrug strategy to antitumor agents, nucleic acid medicine and drug-encapsulating nanocarriers.