A Small‐Molecule FRET Reporter for the Real‐Time Visualization of Cell‐Surface Proteolytic Enzyme Functions |
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| Authors: | Jing Mu Dr Fang Liu Muhammad Shafiq Rajab Meng Shi Shuang Li Chiching Goh Prof Lei Lu Prof Qing‐Hua Xu Prof Bin Liu Dr Lai Guan Ng Prof Bengang Xing |
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| Affiliation: | 1. Division of Chemistry and Biological Chemistry, School of Physical & Mathematical Sciences, Nanyang Technological University, Singapore, 637371 (Singapore);2. School of Biological Sciences, Nanyang Technological University, Singapore, 637551 (Singapore);3. Department of Chemistry, National University of Singapore, Singapore 117543 (Singapore);4. Singapore Immunology Network (SIgN), A*STAR (Agency for Science, Technology and Research), Biopolis, Singapore, 138648 (Singapore);5. Department of Chemical Biomolecular Engineering, National University of Singapore, Singapore 117576 (Singapore) |
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| Abstract: | Real‐time imaging of cell‐surface‐associated proteolytic enzymes is critical to better understand their performances in both physiological and pathological processes. However, most current approaches are limited by their complexity and poor membrane‐anchoring properties. Herein, we have designed and synthesized a unique small‐molecule fluorescent probe, which combines the principles of passive exogenous membrane insertion and Förster resonance energy transfer (FRET) to image cell‐surface‐localized furin‐like convertase activities. The membrane‐associated furin‐like enzymatic cleavage of the peptide probe leads to an increased fluorescence intensity which was mainly localized on the plasma membrane of the furin‐expressed cells. This small‐molecule fluorescent probe may serve as a unique and reliable reporter for real‐time visualization of endogenous cell‐surfaceassociated proteolytic furin‐like enzyme functions in live cells and tissues using one‐photon and two‐photon microscopy. |
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| Keywords: | fluorescence microscopy FRET imaging agents proteolytic enzymes two‐photon imaging |
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