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An Activatable AIEgen Probe for High‐Fidelity Monitoring of Overexpressed Tumor Enzyme Activity and Its Application to Surgical Tumor Excision
Author(s) -
Li Haidong,
Yao Qichao,
Xu Feng,
Li Yueqing,
Kim Dayeh,
Chung Jeewon,
Baek Gain,
Wu Xiaofeng,
Hillman Prima Fitria,
Lee Eun Young,
Ge Haoying,
Fan Jiangli,
Wang Jingyun,
Nam SangJip,
Peng Xiaojun,
Yoon Juyoung
Publication year - 2020
Publication title -
angewandte chemie
Language(s) - English
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.202001675
Subject(s) - alkaline phosphatase , in vivo , chemistry , fluorescence , enzyme , fluorophore , ex vivo , biophysics , quinoline , molecular probe , covalent bond , microbiology and biotechnology , biochemistry , in vitro , biology , dna , optics , organic chemistry , physics
Monitoring fluctuations in enzyme overexpression facilitates early tumor detection and excision. An AIEgen probe (DQM‐ALP) for the imaging of alkaline phosphatase (ALP) activity was synthesized. The probe consists of a quinoline‐malononitrile (QM) core decorated with hydrophilic phosphate groups as ALP‐recognition units. The rapid liberation of DQM‐OH aggregates in the presence of ALP resulted in aggregation‐induced fluorescence. The up‐regulation of ALP expression in tumor cells was imaged using DQM‐ALP. The probe permeated into 3D cervical and liver tumor spheroids for imaging spatially heterogeneous ALP activity with high spatial resolution on a two‐photon microscopy platform, providing the fluorescence‐guided recognition of sub‐millimeter tumorigenesis. DQM‐ALP enabled differentiation between tumor and normal tissue ex vivo and in vivo, suggesting that the probe may serve as a powerful tool to assist surgeons during tumor resection.