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.

今天，化疗仍然是一种有效的癌症治疗方法。然而，由于副作用，它仍然是一个巨大的挑战。在目前的研究中，我们首先引入了适体连接的化学去壳反应与内源性铜离子或铜螯合物相结合，以调节病理条件下前药的释放。对于概念验证研究，我们使用带有罗丹明的适体来靶向核仁蛋白过度表达的癌细胞的成像，其中核仁蛋白适体不仅作为靶标，而且令人惊讶地还与铜离子合作以加速荧光部分的释放。我们构建了可激活的前药模型核酸适体和常规化疗以靶向核仁蛋白过表达的癌细胞，其中通过添加铜离子可以激活降低的药物毒性。