文献类型：期刊文献

英文题名：Fluorescent In Situ Targeting Probes for Rapid Imaging of Ovarian-Cancer-Specific γ-Glutamyltranspeptidase

作者：Wang, Feiyi[1,2];Zhu, Ying[3];Zhou, Li[4];Pan, Liang[3];Cui, Zhifen[3];Fei, Qiang[1,2];Luo, Sihang[1,2];Pan, Dun[3];Huang, Qing[3];Wang, Rui[4];Zhao, Chunchang[1,2];Tian, He[1,2];Fan, Chunhai[3]

机构：[1]E China Univ Sci & Technol, Key Lab Adv Mat, Shanghai 200237, Peoples R China;[2]E China Univ Sci & Technol, Inst Fine Chem, Shanghai 200237, Peoples R China;[3]Chinese Acad Sci, Shanghai Inst Appl Phys, CAS Key Lab Interfacial Phys & Technol, Shanghai Synchrotron Radiat Facil,Div Phys Biol &, Shanghai 201800, Peoples R China;[4]E China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China

年份：2015

卷号：54

期号：25

起止页码：7349

外文期刊名：ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

收录：;EI(收录号：20151900821663);WOS:【SCI-EXPANDED(收录号:WOS:000356390300023)】；

基金：We 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).

语种：英文

外文关键词：aromatic hydrocarbon transfer; enzymes; fluorescence; photophysics; tumor cells

摘要：gamma-Glutamyltranspeptidase (GGT) is a tumor biomarker that selectively catalyzes the cleavage of glutamate overexpressed on the plasma membrane of tumor cells. Here, we developed two novel fluorescent in situ targeting (FIST) probes that specifically target GGT in tumor cells, which comprise 1) a GGT-specific substrate unit (GSH), and 2) a boron-dipyrromethene (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 rapid, irreversible aromatic hydrocarbon transfer between the sulfur and nitrogen atoms accompanied by switching of photophysical properties.