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Bioluminescent Probe for Monitoring Endogenous Fibroblast Activation Protein-Alpha
Yuxing Lin1,2, Zhao Ma1, Zhenzhen Li1
1Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy , Shandong University , Jinan , Shandong 250012 , China.
Analytical Chemistry
|November 1, 2019
Summary
Researchers developed a novel bioluminogenic probe to detect Fibroblast Activation Protein-α (FAP), crucial in tumors and fibrosis. This probe accurately measures FAP levels in vitro and in vivo, aiding in evaluating FAP inhibitors and disease progression.
Area of Science:
- Biochemistry
- Molecular Biology
- Medical Imaging
Background:
- Fibroblast Activation Protein-α (FAP) is a cell surface glycoprotein highly expressed in reactive fibroblasts associated with tumors and fibrotic diseases.
- FAP is a significant target for drug design and a key component in prodrug strategies for anticancer agents, aiming to broaden the therapeutic window.
- Accurate detection and quantification of FAP are essential for understanding its role in disease and for developing targeted therapies.
Purpose of the Study:
- To develop the first bioluminogenic probe for the detection and quantification of Fibroblast Activation Protein-α (FAP).
- To validate the probe's efficacy in evaluating FAP inhibitors in vitro.
- To assess the probe's capability to reflect endogenous FAP levels in vivo using animal models.
Main Methods:
- Development of a novel bioluminogenic probe (probe 1) for FAP detection.
- In vitro assays to determine the limit of detection and evaluate FAP inhibitor efficacy.
- In vivo studies using transgenic mice and tumor-bearing nude mice to assess endogenous FAP levels.
- Application of the probe in bleomycin-induced idiopathic pulmonary fibrosis mouse models to detect FAP upregulation.
Main Results:
- The developed bioluminogenic probe achieved a limit-of-detection of 0.254 ng/mL.
- The probe successfully quantified FAP levels in vitro, enabling the evaluation of FAP inhibitors.
- In vivo experiments confirmed that probe 1 accurately reflects endogenous FAP levels in transgenic and tumor-bearing mice.
- The probe demonstrated successful detection of FAP upregulation in lung homogenates from mice with induced idiopathic pulmonary fibrosis.
Conclusions:
- A novel bioluminogenic probe for FAP has been successfully developed, offering a sensitive detection method.
- The probe is validated for in vitro assessment of FAP inhibitors and in vivo monitoring of FAP expression.
- This tool provides a valuable method for studying FAP's role in cancer and fibrotic diseases, including idiopathic pulmonary fibrosis.
