文献类型：期刊文献

英文题名：A "One-to-Multi" Activatable Near-infrared Fluorescent Probe for the Sensitive Imaging of γ-Glutamyl Transpeptidase Activity in Living Mice

作者：Ding, Yiru[1];Chen, Youyan[1];Dou, Huanke[1];Zhang, Zhengwei[2,3];Xie, Hexin[1]

机构：[1]East China Univ Sci & Technol, Frontiers Sci Ctr Materiobiol & Dynam Chem,Sch Pha, Shanghai Frontier Sci Res Base Optogenet Tech Cell, State Key Lab Bioreactor EngnShanghai Key Lab New, Shanghai 200237, Peoples R China;[2]Fudan Univ, Huashan Hosp, Dept Nucl Med, Shanghai 200235, Peoples R China;[3]Fudan Univ, Huashan Hosp, PET Ctr, Shanghai 200235, Peoples R China

年份：2025

卷号：20

期号：22

外文期刊名：CHEMISTRY-AN ASIAN JOURNAL

收录：;EI(收录号：20253318988900);WOS:【SCI-EXPANDED(收录号:WOS:001549055600001)】；

基金：Y.D. and Y.C. are contributed equally to this work. The authors greatly appreciate financial support from the NSFC (22077031), Fundamental Research Funds for the Central Universities, and Shanghai Frontier Science Research Base of Optogenetic Techniques for Cell Metabolism (Shanghai Municipal Education Commission, grant 2021 Sci & Tech 03-28).

语种：英文

外文关键词：Fluorescent probe; In vivo imaging; Quinone methide; gamma-glutamyl transpeptidase

摘要：gamma-Glutamyl transpeptidase (GGT) is a membrane-bounded enzyme closely involved in a wide range of physiological and pathological processes. While numerous fluorescent probes have been developed to image GGT activity noninvasively, in vivo applications remain challenging. A key limitation lies in GGT's localization: activated fluorophores diffuse rapidly from sites of activation, significantly reducing contrast of image in living systems. To overcome this, we adopted the "one-to-multi" design to develop a novel NIR fluorescent probe for GGT. This probe, upon a single GGT activation, triggers a cascade of effects, including markedly reduced aqueous solubility, enhanced cellular permeability, covalent self-immobilization at the target site, and enhancement in near-infrared (NIR) fluorescence intensity. This design allows real-time and sensitive imaging of GGT activity in live cells and achieves high contrast in vivo imaging with long-lasting signal retention at tumor sites in living mice.