Formyl Peptide GPCR Assays
Background of Formyl Peptide Receptors
The formyl peptide receptors (FPRs) are a group of G protein-coupled receptors that are involved in antibacterial host defense and inflammation. The formyl peptide receptors play important roles in neutrophil transcriptional regulation and cytokine production and induce neutrophil apoptosis in a ROS-dependent manner. Studies have shown that formyl peptide receptors are associated with various diseases, such as Alzheimer's disease, prion diseases, and HIV.
Fig.1 Structure of the FPR1 receptor and key polymorphisms within the protein. (Dorward, 2015)
Distribution and Functions of Formyl Peptide Receptors
The formyl peptide receptors are expressed mainly by mammalian phagocytic leukocytes. Among them, the expression of FPR1 and FPR2 can be found in both monocytes and neutrophils, while FPR3 is expressed in monocytes but not neutrophils. In general, FPR2 presents an even wider distribution pattern than FPR1. Activation of formyl peptide receptors mediates induction of neutrophil chemotaxis and stimulation of neutrophil degranulation.
Subtypes and Mechanisms of Formyl Peptide Receptors
In humans, there are three formyl peptide receptor isoforms, including formyl peptide receptor 1 (FPR1), formyl peptide receptor 2 (FPR2), and formyl peptide receptor 3 (FPR3).
| Receptor | Gene | Mechanism | Agonists | Antagonists |
| Formyl peptide receptor 1 | FPR1 |
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| Formyl peptide receptor 2 | FPR2 |
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| Formyl peptide receptor 3 | FPR3 |
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Assay List of N-formylpeptide Receptors
Creative Biolabs can provide a range of assays of N-formylpeptide receptors. You can choose the assay in the list or contact us for more information:
| Assay No. | Assay Name | Host Cell | Assay Type | Datasheet |
|---|---|---|---|---|
| Calcium Flux Assay | ||||
| S01YF-1122-KX421 | Magic™ Human FPR1 In Vitro Calcium Flux Assay | CHO-K1-Gα16 | Calcium Flux Assay | |
| Assay No. | Assay Name | Host Cell | Assay Type | Datasheet |
|---|---|---|---|---|
| Calcium Flux Assay | ||||
| S01YF-1122-KX429 | Magic™ Human FPR3 In Vitro Calcium Flux Assay | CHO-K1-Gα16 | Calcium Flux Assay | |
Published Data
| Paper Title |
Formyl-Peptide Receptors in Infection, Inflammation, and Cancer |
| Journal |
Trends in immunology |
| Published | 2018 |
| Abstract |
FPRs are expressed on various host cell types, especially neutrophils and macrophages. Since the first discovery of FPRs on leukocytes, researchers hypothesized that these receptors primarily control pro-inflammatory responses and ultimately lead to degranulation, chemotaxis, and oxidative bursts during infection. The FPR recognizes bacterial and mitochondrial formylated peptides as well as endogenous non-formylated peptides and even lipids. In addition, the activation of FPRs can promote the resolution of inflammation. In the present literature, a relationship between FPR function and inflammation has been demonstrated, including inflammatory diseases, cancer, and infection. |
| Result |
Formylated bacterial peptides or host-derived mitochondrial peptides activate FPR to locally control infection and promote wound healing. However, the release of formylated peptides into the blood may lead to various harmful effects. Therefore, preventing FPR activation has been considered to be a new candidate for the treatment of sepsis or systemic inflammatory response syndrome (SIRS). The expression of FPR1 is critical for the activation of human leukocytes and targeting FPR can also be used to treat certain cancers. Specifically, increased FPR expression on tumor cells can also promote proliferation and metastasis.
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Fig.2 Signal Transduction Pathways of FPRs. (Weiß & Kretschmer, 2018)
References
- Dorward, D.; et al. The role of formylated peptides and formyl peptide receptor 1 in governing neutrophil function during acute inflammation. The American journal of pathology. 2015, 185(5): 1172-1184.
- Weiß, E.; Kretschmer, D. Formyl-peptide receptors in infection, inflammation, and cancer. Trends in immunology. 2018, 39(10): 815-829.
