Furin-Triggered Peptide Self-Assembly Activates Coumarin Excimer Fluorescence for Precision Live-Cell Imaging

Monomer-to-excimer transition has become a valuable technique in fluorescence imaging because of its ability to enhance imaging contrast. However, from a practical perspective, the accuracy of excimer formation at target sites warrants further exploration. Enzyme-triggered peptide self-assembly prov...

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Main Authors: Peiyao Chen, Liling Meng, Yuting Wang, Xiaoya Yan, Meiqin Li, Yun Deng, Yao Sun
Format: Article
Language:English
Published: MDPI AG 2025-06-01
Series:Molecules
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Online Access:https://www.mdpi.com/1420-3049/30/11/2465
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author Peiyao Chen
Liling Meng
Yuting Wang
Xiaoya Yan
Meiqin Li
Yun Deng
Yao Sun
author_facet Peiyao Chen
Liling Meng
Yuting Wang
Xiaoya Yan
Meiqin Li
Yun Deng
Yao Sun
author_sort Peiyao Chen
collection DOAJ
description Monomer-to-excimer transition has become a valuable technique in fluorescence imaging because of its ability to enhance imaging contrast. However, from a practical perspective, the accuracy of excimer formation at target sites warrants further exploration. Enzyme-triggered peptide self-assembly provides a promising solution to this limitation. As a proof-of-concept, in this study, we developed a furin-triggered peptide self-assembling fluorescent probe RF-Cou by coupling a coumarin dye 7-(diethylamino)-2-oxo-2H-chromene-3-carboxylic acid (Cou) with a furin-responsive peptide scaffold for precision live-cell imaging. Upon entering furin-overexpressing 4T1 tumor cells, RF-Cou underwent enzymatic cleavage, releasing an amphiphilic peptide motif and self-assembling into nanoparticles largely concentrated in the Golgi apparatus to confine the diffusion of Cou. During this process, the Cou excimers were formed and induced a red shift in the fluorescence emission, validating the feasibility of RF-Cou in efficient excimer imaging of furin-overexpressing tumor cells. We expect that our findings will highlight the potential of stimuli-responsive small molecular peptide probes to advance excimer-based imaging platforms, particularly for enzyme-specific cell imaging and therapeutic monitoring.
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institution Kabale University
issn 1420-3049
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publishDate 2025-06-01
publisher MDPI AG
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spelling doaj-art-d40d734de258459098455e040fe155f72025-08-20T03:46:38ZengMDPI AGMolecules1420-30492025-06-013011246510.3390/molecules30112465Furin-Triggered Peptide Self-Assembly Activates Coumarin Excimer Fluorescence for Precision Live-Cell ImagingPeiyao Chen0Liling Meng1Yuting Wang2Xiaoya Yan3Meiqin Li4Yun Deng5Yao Sun6Key Laboratory of Fermentation Engineering (Ministry of Education), National “111” Center for Cellular Regulation and Molecular Pharmaceutics, Hubei Key Laboratory of Industrial Microbiology, School of Life and Health Sciences, Hubei University of Technology, Wuhan 430068, ChinaKey Laboratory of Fermentation Engineering (Ministry of Education), National “111” Center for Cellular Regulation and Molecular Pharmaceutics, Hubei Key Laboratory of Industrial Microbiology, School of Life and Health Sciences, Hubei University of Technology, Wuhan 430068, ChinaKey Laboratory of Fermentation Engineering (Ministry of Education), National “111” Center for Cellular Regulation and Molecular Pharmaceutics, Hubei Key Laboratory of Industrial Microbiology, School of Life and Health Sciences, Hubei University of Technology, Wuhan 430068, ChinaKey Laboratory of Fermentation Engineering (Ministry of Education), National “111” Center for Cellular Regulation and Molecular Pharmaceutics, Hubei Key Laboratory of Industrial Microbiology, School of Life and Health Sciences, Hubei University of Technology, Wuhan 430068, ChinaState Key Laboratory of Green Pesticide, International Joint Research Center for Intelligent Biosensor Technology and Health, College of Chemistry, Central China Normal University, Wuhan 430079, ChinaKey Laboratory of Flexible Optoelectronic Materials and Technology, Ministry of Education, Jianghan University, Wuhan 430056, ChinaState Key Laboratory of Green Pesticide, International Joint Research Center for Intelligent Biosensor Technology and Health, College of Chemistry, Central China Normal University, Wuhan 430079, ChinaMonomer-to-excimer transition has become a valuable technique in fluorescence imaging because of its ability to enhance imaging contrast. However, from a practical perspective, the accuracy of excimer formation at target sites warrants further exploration. Enzyme-triggered peptide self-assembly provides a promising solution to this limitation. As a proof-of-concept, in this study, we developed a furin-triggered peptide self-assembling fluorescent probe RF-Cou by coupling a coumarin dye 7-(diethylamino)-2-oxo-2H-chromene-3-carboxylic acid (Cou) with a furin-responsive peptide scaffold for precision live-cell imaging. Upon entering furin-overexpressing 4T1 tumor cells, RF-Cou underwent enzymatic cleavage, releasing an amphiphilic peptide motif and self-assembling into nanoparticles largely concentrated in the Golgi apparatus to confine the diffusion of Cou. During this process, the Cou excimers were formed and induced a red shift in the fluorescence emission, validating the feasibility of RF-Cou in efficient excimer imaging of furin-overexpressing tumor cells. We expect that our findings will highlight the potential of stimuli-responsive small molecular peptide probes to advance excimer-based imaging platforms, particularly for enzyme-specific cell imaging and therapeutic monitoring.https://www.mdpi.com/1420-3049/30/11/2465peptide self-assemblyexcimerfurinfluorescence imaging
spellingShingle Peiyao Chen
Liling Meng
Yuting Wang
Xiaoya Yan
Meiqin Li
Yun Deng
Yao Sun
Furin-Triggered Peptide Self-Assembly Activates Coumarin Excimer Fluorescence for Precision Live-Cell Imaging
Molecules
peptide self-assembly
excimer
furin
fluorescence imaging
title Furin-Triggered Peptide Self-Assembly Activates Coumarin Excimer Fluorescence for Precision Live-Cell Imaging
title_full Furin-Triggered Peptide Self-Assembly Activates Coumarin Excimer Fluorescence for Precision Live-Cell Imaging
title_fullStr Furin-Triggered Peptide Self-Assembly Activates Coumarin Excimer Fluorescence for Precision Live-Cell Imaging
title_full_unstemmed Furin-Triggered Peptide Self-Assembly Activates Coumarin Excimer Fluorescence for Precision Live-Cell Imaging
title_short Furin-Triggered Peptide Self-Assembly Activates Coumarin Excimer Fluorescence for Precision Live-Cell Imaging
title_sort furin triggered peptide self assembly activates coumarin excimer fluorescence for precision live cell imaging
topic peptide self-assembly
excimer
furin
fluorescence imaging
url https://www.mdpi.com/1420-3049/30/11/2465
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AT lilingmeng furintriggeredpeptideselfassemblyactivatescoumarinexcimerfluorescenceforprecisionlivecellimaging
AT yutingwang furintriggeredpeptideselfassemblyactivatescoumarinexcimerfluorescenceforprecisionlivecellimaging
AT xiaoyayan furintriggeredpeptideselfassemblyactivatescoumarinexcimerfluorescenceforprecisionlivecellimaging
AT meiqinli furintriggeredpeptideselfassemblyactivatescoumarinexcimerfluorescenceforprecisionlivecellimaging
AT yundeng furintriggeredpeptideselfassemblyactivatescoumarinexcimerfluorescenceforprecisionlivecellimaging
AT yaosun furintriggeredpeptideselfassemblyactivatescoumarinexcimerfluorescenceforprecisionlivecellimaging