An activatable fluorescent probe for fibroblast activation protein α and its bioimaging applications.
5 affiliations
- 1Second Affiliated Hospital, Dalian Medical University Dalian 116023 China [email protected].
- 2Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical University Xuzhou 221004 China.
- 3School of Life Science and Technology, Northwestern Polytechnical University Xi'an 710072 China.
- 4College of Pharmacy, Dalian Medical University Dalian 116044 China [email protected].
- 5Department of Neurosurgery, General Hospital of Northern Theater Command Shenyang China [email protected].
Abstract
Fibroblast activation protein α (FAP) is a member of the plasma membrane-bound serine protease family, which exhibits exopeptidase and endopeptidase activity in organisms. Recently, considerable studies have focused on the key role of FAP in various pathological processes, indicating that it may be a therapeutic target for treating human disorders and diseases. In the present study, a fluorescent probe for FAP was constructed by the introduction of a substrate recognition dipeptide that was rationally modified by tert-butoxycarbonyl group to the fluorophore DDAN. The probe DDAF, synthesized from DDAN, exhibited high selectivity and sensitivity for FAP, with a detection limit of 0.71 ng mL⁻¹. DDAF was successfully applied for the rapid screening of potent inhibitors of FAP, and a quinoline derivative was identified that exhibited a strong inhibitory effect on FAP. Subsequently, the in vitro visualization and monitoring of FAP in living cancer cells and tissues were performed using DDAF, indicating the widespread expression of FAP in a variety of tumors. These findings provide a promising tool for discovering potent therapeutic agents targeting FAP and for the real-time visualization and monitoring of FAP in tumors.
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BibTeX
@article{feng2026activatable,
title = {{An activatable fluorescent probe for fibroblast activation protein α and its bioimaging applications.}},
author = {Lei Feng and Hengjing Chen and Zhenhao Tian and Wenpeng Li and Yifei Dang and Guobiao Liang and Chengjuan Xing and Xiaohong Shu and Jing Ning and Fangyu Yang and Xiaochi Ma},
journal = {RSC advances},
year = {2026},
month = oct,
doi = {10.1039/d6ra05595h},
url = {https://europepmc.org/article/MED/42910326},
note = {CC BY-NC},
}
RIS
TY - JOUR
TI - An activatable fluorescent probe for fibroblast activation protein α and its bioimaging applications.
AU - Lei Feng
AU - Hengjing Chen
AU - Zhenhao Tian
AU - Wenpeng Li
AU - Yifei Dang
AU - Guobiao Liang
AU - Chengjuan Xing
AU - Xiaohong Shu
AU - Jing Ning
AU - Fangyu Yang
AU - Xiaochi Ma
PY - 2026
DA - 2026/10/21
JO - RSC advances
DO - 10.1039/d6ra05595h
UR - https://europepmc.org/article/MED/42910326
AB - Fibroblast activation protein α (FAP) is a member of the plasma membrane-bound serine protease family, which exhibits exopeptidase and endopeptidase activity in organisms. Recently, considerable studies have focused on the key role of FAP in various pathological processes, indicating that it may be a therapeutic target for treating human disorders and diseases. In the present study, a fluorescent probe for FAP was constructed by the introduction of a substrate recognition dipeptide that was rationally modified by tert-butoxycarbonyl group to the fluorophore DDAN. The probe DDAF, synthesized from DDAN, exhibited high selectivity and sensitivity for FAP, with a detection limit of 0.71 ng mL⁻¹. DDAF was successfully applied for the rapid screening of potent inhibitors of FAP, and a quinoline derivative was identified that exhibited a strong inhibitory effect on FAP. Subsequently, the in vitro visualization and monitoring of FAP in living cancer cells and tissues were performed using DDAF, indicating the widespread expression of FAP in a variety of tumors. These findings provide a promising tool for discovering potent therapeutic agents targeting FAP and for the real-time visualization and monitoring of FAP in tumors.
SN - 2046-2069
ER -