School of Chemical and Biomedical Engineering, Nanyang Technological University, Singapore, 637457, Singapore.
Angew Chem Int Ed Engl. 2018 Jun 25;57(26):7804-7808. doi: 10.1002/anie.201803321. Epub 2018 May 23.
Theranostics provides opportunities for precision cancer therapy. However, theranostic probes that simultaneously turn on their diagnostic signal and pharmacological action only in respond to a targeted biomarker have been less exploited. We herein report the synthesis of a macrotheranostic probe that specifically activates its near-infrared fluorescence (NIRF), photoacoustic (PA), and photothermal signals in the presence of a cancer-overexpressed enzyme for imaging-guided cancer therapy. Superior to the small-molecule counterpart probe, the macrotheranostic probe has ideal biodistribution and renal clearance, permitting passive targeting of tumors, in situ activation of multimodal signals, and effective photothermal ablation. Our study thus provides a macromolecular approach towards activatable multimodal phototheranostics.
治疗诊断学为精准癌症治疗提供了机会。然而，能够针对靶向生物标志物同时开启诊断信号和药理作用的治疗诊断探针仍较少被开发。在此，我们报告了一种大分子治疗诊断探针的合成，该探针在存在过表达的癌症酶时特异性激活其近红外荧光（NIRF）、光声（PA）和光热信号，用于成像引导的癌症治疗。与小分子对应物探针相比，大分子治疗诊断探针具有理想的生物分布和肾脏清除率，允许肿瘤的被动靶向、多模态信号的原位激活和有效的光热消融。因此，我们的研究为可激活的多模态光热治疗诊断提供了一种大分子方法。
