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Visualizing the Conformational Dynamics of Membrane Receptors Using Single-Molecule FRET
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Monoclonal Antibody 5F1 Modulates Formyl Peptide Receptor 1 Conformation for Transmembrane Signaling
Yue Wang1, Yezhou Liu1, Yixin Chang1
1Kobilka Institute of Innovative Drug Discovery, School of Medicine The Chinese University of Hong Kong Shenzhen Guangdong China.
FASEB Bioadvances
|September 10, 2025
Summary
The monoclonal antibody 5F1 targets formyl peptide receptor 1 (FPR1), altering its conformation and signaling. This antibody shows selectivity for human FPR1 and may have therapeutic potential beyond detection.
Area of Science:
- Immunology
- Cell Biology
- Pharmacology
Background:
- Formyl peptide receptor 1 (FPR1) is a G protein-coupled receptor (GPCR) crucial for phagocyte functions like chemotaxis and bacterial killing.
- The monoclonal antibody 5F1 is commonly used to detect FPR1 expression.
Purpose of the Study:
- To comprehensively characterize the functional properties of the monoclonal antibody 5F1 against FPR1.
- To investigate the binding epitope and downstream signaling effects of 5F1 on FPR1.
Main Methods:
- Epitope mapping using synthetic peptides.
- NanoLuc Bioluminescence Resonance Energy Transfer (BRET) for conformational change analysis.
- Assays for receptor internalization, G protein dissociation, and β-arrestin translocation.
Main Results:
- 5F1 demonstrated high selectivity for human FPR1 over FPR2.
- Extracellular loop 2 (ECL2) was identified as a major epitope for 5F1 binding.
- 5F1 binding induced significant FPR1 conformational changes, internalization, Gi protein dissociation, and β-arrestin recruitment.
- Mutations at F110 and R205 reduced 5F1 binding, indicating sensitivity to conformational alterations.
Conclusions:
- Monoclonal antibody 5F1 can modulate FPR1 conformation and transmembrane signaling pathways.
- These functional properties suggest potential applications for 5F1 beyond simple FPR1 detection.
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