Copper (II) synergistic AS1411 conjunction with chemical decaging reactions for selective fluorescence imaging and prodrug activation in living systems

Chemotherapy remains an effective treatment for cancer today. However, it remains a huge challenge due to side effects. In the current study, we first introduce aptamer-linked chemical decaging reactions combine with endogenous copper ions or Cu-chelates to regulate the release of prodrugs in pathological conditions. For the proof-of-concept study, we use aptamers with rhodamine to target imaging of nucleolin overexpressing cancer cells, where nucleolin aptamers not only act as targets, but surprisingly also cooperate with copper ions to accelerate the release of fluorescent moieties. We construct activatable prodrugs models nucleic acid aptamers and conventional chemotherapy to target nucleolin overexpressing cancer cells, in which reduced drug toxicity can be activated by adding copper ions. We envision that the integration of binding aptamer and catalytic reactions based on small molecules has a promising application in the field of cancer treatment.