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A General Strategy to Develop Highly Sensitive FAPα Fluorescent Probes for Invasive Cancer Detection.

Yurong Feng¹, Cheng Xie¹, Tian-Bing Ren¹

¹State Key Laboratory of Chemo/Biosensing, College of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, P.R. China.

Angewandte Chemie (International Ed. in English)

|August 18, 2025

Summary

This summary is machine-generated.

Researchers developed a novel fluorescent probe strategy to detect Fibroblast Activation Protein alpha (FAPα) in tumors. This new probe enhances sensitivity for precise tumor margin delineation and evaluation of tumor resection.

Keywords:

FAPα Fluorescent probe Imaging Invasive cancer

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Area of Science:

Biomedical Engineering
Chemical Biology
Oncology

Background:

Fibroblast Activation Protein alpha (FAPα) is implicated in carcinoma progression, including growth, invasion, and metastasis.
Current methods for detecting FAPα in tumors are limited by sensitivity, hindering accurate tumor margin delineation.

Purpose of the Study:

To develop a general design strategy for constructing highly sensitive FAPα-activated fluorescent probes.
To demonstrate the utility of a novel probe for sensitive FAPα detection and tumor imaging.

Main Methods:

A design strategy introducing positive charges into fluorophore skeletons was employed.
Molecular docking simulations and fluorescence spectroscopy were used to evaluate probe-FAPα interactions.
A specific probe, FQCy7, was synthesized and tested for its performance in vitro and in vivo.

Main Results:

The introduction of positive charges significantly improved probe affinity and sensitivity to FAPα.
FQCy7 demonstrated high sensitivity for FAPα, enabling studies on its role in carcinoma cell migration and invasion.
FQCy7 successfully distinguished invasive tumors from benign lesions and aided in evaluating tumor resection accuracy.

Conclusions:

A novel strategy for designing sensitive FAPα-activated fluorescent probes was established.
FQCy7 serves as a powerful tool for precise tumor detection, distinguishing malignant from benign tissues.
This work advances the capability for accurate tumor margin assessment and surgical guidance.