Department of Chemical and Biomolecular Engineering , National University of Singapore , 4 Engineering Drive 4 , Singapore 117585.
Nanotheranostics Laboratory, School of Medicine, Institutes for Life Sciences , South China University of Technology , Guangzhou , China 510006.
Anal Chem. 2018 Jun 5;90(11):6718-6724. doi: 10.1021/acs.analchem.8b00547. Epub 2018 May 10.
Metabolic glycoengineering of unnatural glycans with bio-orthogonal chemical groups and a subsequent click reaction with fluorescent probes have been widely used in monitoring various bioprocesses. Herein, we developed a dual-responsive metabolic precursor that could specifically generate unnatural glycans with azide groups on the membrane of targeted cancer cells with high selectivity. Moreover, a water-soluble fluorescent light-up probe with aggregation-induced emission (AIE) was synthesized, which turned its fluorescence on upon a click reaction with azide groups on the cancer cell surface, enabling special cancer cell imaging with low background signal. Furthermore, the probe can generate O upon light irradiation, fulfilling its dual role as an imaging and therapeutic agent for cancer cells. Therefore, the concepts of the cancer-cell-specific metabolic precursor cRGD-S-AcManNAz and the AIE light-up probe are promising in bio-orthogonal labeling and cancer-specific imaging and therapy.
利用具有生物正交化学基团的非天然糖进行代谢糖基工程，并随后与荧光探针发生点击反应，已被广泛用于监测各种生物过程。在此，我们开发了一种双重响应的代谢前体，它可以在高选择性的靶向癌细胞的膜上特异性地产生带有叠氮基团的非天然聚糖。此外，我们还合成了一种具有聚集诱导发射（AIE）的水溶性荧光点亮探针，它可以与癌细胞表面的叠氮基团发生点击反应，从而使荧光点亮，实现低背景信号的特殊癌细胞成像。此外，该探针在光照下可以产生 O，实现了其作为癌症细胞成像和治疗双重作用的探针。因此，具有细胞特异性的代谢前体 cRGD-S-AcManNAz 和 AIE 点亮探针的概念在生物正交标记和癌症特异性成像和治疗方面具有广阔的应用前景。
