Department of Chemical and Biomolecular Engineering, National University of Singapore, 4 Engineering Drive 4, 117585, Singapore, Singapore.
State Key Laboratory of Medicinal Chemical Biology, Key Laboratory of Bioactive Materials, Ministry of Education and College of Life Sciences, Nankai University, Tianjin, 300071, China.
Angew Chem Int Ed Engl. 2018 Aug 6;57(32):10182-10186. doi: 10.1002/anie.201805446. Epub 2018 Jul 18.
Bio-orthogonal tumor labeling is more effective in delivering imaging agents or drugs to a tumor site than active targeting strategy owing to covalent ligation. However, to date, tumor-specific imaging through bio-orthogonal labeling largely relies on body clearance to differentiate target from the intrinsic probe signal owing to the lack of light-up probes for in vivo bio-orthogonal labeling. Now the first light-up probe based on a fluorogen with aggregation-induced emission for in vivo bio-orthogonal fluorescence turn-on tumor labeling is presented. The probe has low background fluorescence in aqueous media, showing negligible non-specific interaction with normal tissues. Once it reacts with azide groups introduced to tumor cells through metabolic engineering, the probe fluorescence is lightened up very quickly, enabling rapid tumor-specific imaging. The photosensitizing ability was also used to realize effective image-guided photodynamic tumor therapy.
生物正交肿瘤标记物由于共价键的连接，比主动靶向策略更有效地将成像剂或药物递送到肿瘤部位。然而，迄今为止，由于缺乏用于体内生物正交标记的光激活探针，通过生物正交标记进行肿瘤特异性成像在很大程度上依赖于机体清除，以区分靶标与固有探针信号。现在，首次提出了基于具有聚集诱导发射的荧光团的光激活探针用于体内生物正交荧光开启肿瘤标记。该探针在水介质中具有低背景荧光，与正常组织几乎没有非特异性相互作用。一旦它与通过代谢工程引入肿瘤细胞的叠氮基团反应，探针的荧光就会迅速增强，从而实现快速的肿瘤特异性成像。光致敏能力也被用于实现有效的图像引导光动力肿瘤治疗。
