N-formylpeptide GPCR Family Subtypes and Products

What Are N-formylpeptide Receptors?

N-formylpeptide receptors (FPRs) are a family of G protein-coupled receptors (GPCRs) comprised of three receptor subtypes: FPR1, FPR2, and FPR3. FPRs are involved in a variety of cellular functions, such as chemotaxis and the production of superoxides. More specifically, FPR1 has been found to play a role in the host defense against infection, while FPR2 plays a role in inflammation, tumorigenesis, and epithelial cell homeostasis within the colon. FPR3 is still being heavily researched, as not much is known about its pharmacological properties. Further research also needs to be done on N-formylpeptide receptor agonist and antagonist activity.

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N-formylpeptide Receptor Information

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FPR1

FPR2

FPR3

The gene FPR1 encodes the formylpeptide receptor (FPR), which is a G-protein-coupled receptor that mediates chemotaxis of phagocytic leukocytes induced by bacterial peptide N-formyl-methionyl-leucyl-phenylalanine (fMLP). Agonist binding to FPR in phagocytic leukocytes leads to the activation of phosphatidylinositol 3-kinase (PI3K), mitogen-activated protein kinases (MAPKs), and the transcription factor nuclear factor (NF)-kB via heterotrimeric Gαi proteins. FPR is involved in host defense against bacterial infection and in the clearance of damaged cells. Recently a large number of non-formylated peptide ligands for FPR have now been identified. Some of the new ligands (e.g. Ac1–26 from annexin) are endogenous in origin, and some come from pathogens that are associated with human diseases such as HIV, which have suggested novel roles for this receptor in the regulation of acute and chronic inflammation as well as host responses during HIV-1 infection.

The lipoxin A4 receptor ALX is also known as formyl peptide receptor- like 1 (FPRL1) or formyl peptide receptor 2 (FPR2). It shares 69% amino acid identity with FPR but displays low affinity for bacterial peptide N-formyl-methionyl- leucyl-phenylalanine (fMLF). ALX is highly expressed on neutrophils and monocytes and mediates cell chemotaxis. By interacting with a variety of exogenous and host- derived agonists, ALX may have important implications in the pathogenesis of human diseases such as HIV, Alzheimer’s disease (AD), amyloidosis and prion diseases.

FPR is involved in host defense against bacterial infection and in the clearance of damaged cells. Recently a large number of non-formylated peptide ligands for FPR have now been identified. Some of the new ligands (e.g. Ac1–26 from annexin) are endogenous in origin, and some come from pathogens that are associated with human diseases such as HIV, which have suggested novel roles for this receptor in the regulation of acute and chronic inflammation as well as host responses during HIV-1 infection.

N-formylpeptide Cell Lines

Receptor FamilyReceptorSpeciesParentalStable Cell Lines Division-Arrested Cells Membranes
N-formylpeptideFPR1humanHEK293TC1243DC1243MC1243
FPR1humanHEK293TC1243aDC1243aMC1243a
FPR1humanHEK293T Gαqi5CG1243DCG1243MCG1243
FPR2humanHEK293TC1244DC1244MC1244
FPR2humanHEK293TC1244aDC1244aMC1244a
FPR3humanHEK293TC1245DC1245MC1245

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