Human FPR1

Figure. Concentration-dependent activation of FPR1 by fMLP

Reporter cells were transfected with either the expression plasmid for human formyl peptide receptor 1 (FPR1) or the mock plasmid and treated with various concentrations of fMLP. Data points shown are the mean ± SEM of an experiment (n = 3), and the curve is a fit to Hill equation with an EC50 of 3.5 nM.

formyl peptide receptor 1
Available assay modes
Agonist, Inverse agonist, Antagonist, PAM, NAM
à la carte, Human non-orphan GPCRs

Formylpeptide receptors

The formylpeptide receptors respond to exogenous ligands such as the bacterial product fMet-Leu-Phe (fMLP) and endogenous ligands such as lipoxin A4 (LXA4), 15-epi-lipoxin A4, annexin I, cathepsin G, amyloid β42, serum amyloid A and spinorphin, derived from β-haemoglobin. FPR1 also serves as a plague receptor for selective destruction of human immune cells by Y. pestis [1]. The FPR1/2 agonists 'compound 17b' and 'compound 43' have shown cardiac protective functions [2,3].


  1. Osei-Owusu P, Charlton TM, Kim HK, et al. FPR1 is the plague receptor on host immune cells. Nature 2019;574:57-62.
  2. Qin CX, May LT, Li R, et al. Small-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in mice. Nat Commun 2017;8:14232.
  3. García RA, Ito BR, Lupisella JA, et al. Preservation of Post-Infarction Cardiac Structure and Function via Long-Term Oral Formyl Peptide Receptor Agonist Treatment. JACC Basic Transl Sci 2019;4:905-920.
Excerpt from IUPHAR/BPS Guide to Pharmacology

Related Receptors

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