Recently，Prof. Chunchang Zhao et al published a paper on Angew. Chem. Int. Ed (http://onlinelibrary.wiley.com/doi/10.1002/ange.201502899/abstract.), tilted “Fluorescent In Situ Targeting Probes for Rapid Imaging of Ovarian Cancer-Specific g-Glutamyltranspeptidase”. The work, collaborated with Prof. Rui Wang and Prof. Chunhai Fan, was finished by Feiyi Wang etc.

    γ-Glutamyltranspeptidase (GGT) is a well-known tumor biomarker, which selectively catalyzes the cleavage of glutamate that is overexpressed on the plasma membrane of tumor cells but not on that of normal cells. In this paper, the autors developed two novel fluorescent in-situ targeting (FIST) probes that specifically target GGT in tumor cells. These probes are designed to comprise (1) a GGT-specific substrate unit (GSH), and (2) a BODIPY moiety for fluorescent signalling. In the presence of GGT, sulfur-substituted BODIPY was converted to amino-substituted BODIPY, resulting in dramatic fluorescence variations. By exploiting this enzyme-triggered photophysical property, we employed these FIST probes to monitor the GGT activity in living cells, which showed remarkable differentiation between ovarian cancer cells and normal cells. These probes represent two first-generation chemodosimeters featuring enzyme-mediated a rapid, irreversible SN aromatic hydrocarbon transfer accompanied with the switching of photophysical properties. Such translation should thus open new opportunities for novel enzyme-activatable probes.
    Gratefully acknowledge the financial support by the National Science Foundation of China (grant numbers 21172071, 21190033, 21372083, 21375139, 21390414, and 91313302), and the Ministry of Science and Technology (grant numbers 2013CB933802 and 2012CB825805).