The formylpeptide receptors (nomenclature agreed by the NC-IUPHAR Subcommittee on the formylpeptide receptor family [26]) respond to exogenous ligands such as the bacterial product fMet-Leu-Phe (fMLP) and endogenous ligands such as annexin I (ANXA1, P04083) , cathepsin G (CTSG, P08311), amyloid β42, serum amyloid A and spinorphin, derived from β-haemoglobin (HBB, P68871).

Note that the data for FPR2/ALX are also reproduced on the leukotriene receptor page.

* Key recommended reading is highlighted with an asterisk

Cattaneo F, Guerra G, Ammendola R. (2010) Expression and signaling of formyl-peptide receptors in the brain. Neurochem. Res., 35 (12): 2018-26. [PMID:21042851]

* Dorward DA, Lucas CD, Chapman GB, Haslett C, Dhaliwal K, Rossi AG. (2015) The Role of Formylated Peptides and Formyl Peptide Receptor 1 in Governing Neutrophil Function during Acute Inflammation. Am. J. Pathol., 185 (5): 1172-1184. [PMID:25791526]

* Dufton N, Perretti M. (2010) Therapeutic anti-inflammatory potential of formyl-peptide receptor agonists. Pharmacol. Ther., 127 (2): 175-88. [PMID:20546777]

Gavins FN. (2010) Are formyl peptide receptors novel targets for therapeutic intervention in ischaemia-reperfusion injury?. Trends Pharmacol. Sci., 31 (6): 266-76. [PMID:20483490]

Liberles SD, Horowitz LF, Kuang D, Contos JJ, Wilson KL, Siltberg-Liberles J, Liberles DA, Buck LB. (2009) Formyl peptide receptors are candidate chemosensory receptors in the vomeronasal organ. Proc. Natl. Acad. Sci. U.S.A., 106 (24): 9842-7. [PMID:19497865]

* Liu M, Zhao J, Chen K, Bian X, Wang C, Shi Y, Wang JM. (2012) G protein-coupled receptor FPR1 as a pharmacologic target in inflammation and human glioblastoma. Int. Immunopharmacol., 14 (3): 283-8. [PMID:22863814]

* Rabiet MJ, Macari L, Dahlgren C, Boulay F. (2011) N-formyl peptide receptor 3 (FPR3) departs from the homologous FPR2/ALX receptor with regard to the major processes governing chemoattractant receptor regulation, expression at the cell surface, and phosphorylation. J. Biol. Chem., 286 (30): 26718-31. [PMID:21543323]

* Yazid S, Norling LV, Flower RJ. (2012) Anti-inflammatory drugs, eicosanoids and the annexin A1/FPR2 anti-inflammatory system. Prostaglandins Other Lipid Mediat., 98 (3-4): 94-100. [PMID:22123264]

* Ye RD, Boulay F, Wang JM, Dahlgren C, Gerard C, Parmentier M, Serhan CN, Murphy PM. (2009) International Union of Basic and Clinical Pharmacology. LXXIII. Nomenclature for the formyl peptide receptor (FPR) family. Pharmacol. Rev., 61 (2): 119-61. [PMID:19498085]

1. Bae YS, Lee HY, Jo EJ, Kim JI, Kang HK, Ye RD, Kwak JY, Ryu SH. (2004) Identification of peptides that antagonize formyl peptide receptor-like 1-mediated signaling. J. Immunol., 173 (1): 607-14. [PMID:15210823]

2. Clish CB, O'Brien JA, Gronert K, Stahl GL, Petasis NA, Serhan CN. (1999) Local and systemic delivery of a stable aspirin-triggered lipoxin prevents neutrophil recruitment in vivo. Proc. Natl. Acad. Sci. U.S.A., 96 (14): 8247-52. [PMID:10393980]

3. Fiore S, Maddox JF, Perez HD, Serhan CN. (1994) Identification of a human cDNA encoding a functional high affinity lipoxin A4 receptor. J. Exp. Med., 180 (1): 253-60. [PMID:8006586]

4. Fiore S, Ryeom SW, Weller PF, Serhan CN. (1992) Lipoxin recognition sites. Specific binding of labeled lipoxin A4 with human neutrophils. J. Biol. Chem., 267 (23): 16168-76. [PMID:1322894]

5. Fiore S, Serhan CN. (1995) Lipoxin A4 receptor activation is distinct from that of the formyl peptide receptor in myeloid cells: inhibition of CD11/18 expression by lipoxin A4-lipoxin A4 receptor interaction. Biochemistry, 34 (51): 16678-86. [PMID:8527441]

6. Freer RJ, Day AR, Muthukumaraswamy N, Pinon D, Wu A, Showell HJ, Becker EL. (1982) Formyl peptide chemoattractants: a model of the receptor on rabbit neutrophils. Biochemistry, 21 (2): 257-63. [PMID:6280748]

7. Freer RJ, Day AR, Radding JA, Schiffmann E, Aswanikumar S, Showell HJ, Becker EL. (1980) Further studies on the structural requirements for synthetic peptide chemoattractants. Biochemistry, 19 (11): 2404-10. [PMID:7387981]

8. Gronert K, Martinsson-Niskanen T, Ravasi S, Chiang N, Serhan CN. (2001) Selectivity of recombinant human leukotriene D(4), leukotriene B(4), and lipoxin A(4) receptors with aspirin-triggered 15-epi-LXA(4) and regulation of vascular and inflammatory responses. Am. J. Pathol., 158 (1): 3-9. [PMID:11141472]

9. Guilford WJ, Bauman JG, Skuballa W, Bauer S, Wei GP, Davey D, Schaefer C, Mallari C, Terkelsen J, Tseng JL et al.. (2004) Novel 3-oxa lipoxin A4 analogues with enhanced chemical and metabolic stability have anti-inflammatory activity in vivo. J. Med. Chem., 47 (8): 2157-65. [PMID:15056011]

10. He HQ, Liao D, Wang ZG, Wang ZL, Zhou HC, Wang MW, Ye RD. (2013) Functional characterization of three mouse formyl peptide receptors. Mol. Pharmacol., 83 (2): 389-98. [PMID:23160941]

11. Koo C, Lefkowitz RJ, Snyderman R. (1982) The oligopeptide chemotactic factor receptor on human polymorphonuclear leukocyte membranes exists in two affinity states. Biochem Biophys Res Commun., 106: 442-449. [PMID:6285921]

12. Krishnamoorthy S, Recchiuti A, Chiang N, Fredman G, Serhan CN. (2012) Resolvin D1 receptor stereoselectivity and regulation of inflammation and proresolving microRNAs. Am. J. Pathol., 180 (5): 2018-27. [PMID:22449948]

13. Krishnamoorthy S, Recchiuti A, Chiang N, Yacoubian S, Lee CH, Yang R, Petasis NA, Serhan CN. (2010) Resolvin D1 binds human phagocytes with evidence for proresolving receptors. Proc. Natl. Acad. Sci. U.S.A., 107 (4): 1660-5. [PMID:20080636]

14. Le Y, Murphy PM, Wang JM. (2002) Formyl-peptide receptors revisited. Trends Immunol., 23 (11): 541-8. [PMID:12401407]

15. Liang TS, Gao JL, Fatemi O, Lavigne M, Leto TL, Murphy PM. (2001) The endogenous opioid spinorphin blocks fMet-Leu-Phe-induced neutrophil chemotaxis by acting as a specific antagonist at the N-formylpeptide receptor subtype FPR. J. Immunol., 167 (11): 6609-14. [PMID:11714831]

16. Maddox JF, Hachicha M, Takano T, Petasis NA, Fokin VV, Serhan CN. (1997) Lipoxin A4 stable analogs are potent mimetics that stimulate human monocytes and THP-1 cells via a G-protein-linked lipoxin A4 receptor. J. Biol. Chem., 272 (11): 6972-8. [PMID:9054386]

17. Migeotte I, Riboldi E, Franssen JD, Grégoire F, Loison C, Wittamer V, Detheux M, Robberecht P, Costagliola S, Vassart G et al.. (2005) Identification and characterization of an endogenous chemotactic ligand specific for FPRL2. J. Exp. Med., 201 (1): 83-93. [PMID:15623572]

18. Murphy PM, Ozçelik T, Kenney RT, Tiffany HL, McDermott D, Francke U. (1992) A structural homologue of the N-formyl peptide receptor. Characterization and chromosome mapping of a peptide chemoattractant receptor family. J. Biol. Chem., 267 (11): 7637-43. [PMID:1373134]

19. Showell HJ, Freer RJ, Zigmond SH, Schiffmann E, Aswanikumar S, Corcoran B, Becker EL. (1976) The structure-activity relations of synthetic peptides as chemotactic factors and inducers of lysosomal secretion for neutrophils. J. Exp. Med., 143 (5): 1154-69. [PMID:1262785]

20. Stenfeldt AL, Karlsson J, Wennerås C, Bylund J, Fu H, Dahlgren C. (2007) Cyclosporin H, Boc-MLF and Boc-FLFLF are antagonists that preferentially inhibit activity triggered through the formyl peptide receptor. Inflammation, 30 (6): 224-9. [PMID:17687636]

21. Sun R, Iribarren P, Zhang N, Zhou Y, Gong W, Cho EH, Lockett S, Chertov O, Bednar F, Rogers TJ, Oppenheim JJ, Wang JM. (2004) Identification of neutrophil granule protein cathepsin G as a novel chemotactic agonist for the G protein-coupled formyl peptide receptor. J. Immunology, 173: 428-436. [PMID:15210802]

22. Takano T, Fiore S, Maddox JF, Brady HR, Petasis NA, Serhan CN. (1997) Aspirin-triggered 15-epi-lipoxin A4 (LXA4) and LXA4 stable analogues are potent inhibitors of acute inflammation: evidence for anti-inflammatory receptors. J. Exp. Med., 185 (9): 1693-704. [PMID:9151906]

23. Walther A, Riehemann K, Gerke V. (2000) A novel ligand of the formyl peptide receptor: annexin I regulates neutrophil extravasation by interacting with the FPR. Mol. Cell, 5 (5): 831-40. [PMID:10882119]

24. Wenzel-Seifert K, Seifert R. (1993) Cyclosporin H is a potent and selective formyl peptide receptor antagonist. Comparison with N-t-butoxycarbonyl-L-phenylalanyl-L-leucyl-L-phenylalanyl-L- leucyl-L-phenylalanine and cyclosporins A, B, C, D, and E. J. Immunol., 150 (10): 4591-9. [PMID:8387097]

25. Yan P, Nanamori M, Sun M, Zhou C, Cheng N, Li N, Zheng W, Xiao L, Xie X, Ye RD et al.. (2006) The immunosuppressant cyclosporin A antagonizes human formyl peptide receptor through inhibition of cognate ligand binding. J. Immunol., 177 (10): 7050-8. [PMID:17082621]

26. Ye RD, Boulay F, Wang JM, Dahlgren C, Gerard C, Parmentier M, Serhan CN, Murphy PM. (2009) International Union of Basic and Clinical Pharmacology. LXXIII. Nomenclature for the formyl peptide receptor (FPR) family. Pharmacol. Rev., 61 (2): 119-61. [PMID:19498085]

Subcommittee members: Richard D. Ye (Chairperson) Department of Pharmacology College of Medicine University of Illinois Chicago Illinois U.S.A. François Boulay Commissariat à l’Energie Atomique Institut de Recherches en Technologies et Sciences pour le Vivant Laboratoire de Biochimie et de Biophysique des Systèmses Intégrés Grenoble France Claes Dahlgren Department of Rheumatology and Inflammation Research University of Göteborg Göteborg Sweden Craig Gerard Department of Pediatrics Harvard Medical School and Children's Hospital Boston Massachusetts U.S.A Philip M. Murphy Head, Molecular Signaling Section, Laboratory of Molecular Immunology, and Chief, Laboratory of Molecular Immunology National Institute of Allergy and Infectious Diseases National Institutes of Health 9000 Rockville Pike MSC-1888 Bldg. 10, Room 11N113 Bethesda MD 20892 USA Marc Parmentier Institut de Recherche Interdisciplinaire en Biologie Humaine et Moléculaire (IRIBHM) Université Libre de Bruxelles Brussels Belgium Mark Quinn Department of Microbiology and Immunology Montana State University Bozeman, MT 59717 U.S.A. Charles N. Serhan Center for Experimental Theraputics and Reperfusion Injury Brigham and Women's Hospital Hale Building for Transformative Medicine 60 Fenwood Road, Suite 3-016 Boston, MA 02115 USA Ji Ming Wang Laboratory of Molecular Immunoregulation Cancer and Inflammation Program Center for Cancer Research National Cancer Institute at Frederick Frederick Maryland USA

Other contributors: Magnus Bäck Translational Cardiology Karolinska Institutet, Department of Medicine Karolinska University Hospital M85 141 86 Stockholm Sweden Nan Chiang Center for Experimental Theraputics and Reperfusion Injury Brigham and Women's Hospital Hale Building for Transformative Medicine 60 Fenwood Road, Suite 3-016 Boston, MA 02115 USA Sven-Erik Dahlén Unit for Experimental Asthma and Allergy Research The National Institute of Environmental Medicine Karolinska Institutet Stockholm S-171 77 Sweden Jeffrey Drazen Respiratory Division Brigham and Woman's Hospital 75 Francis Street Boston MA 02115 USA Jilly F. Evans PharmAkea 12780 El Camino Real San Diego 92130 CA USA G. Enrico Rovati Laboratory of Molecular Pharmacology Department of Pharmaceutical Sciences University of Milan Via Balzaretti 9 Milan 201 33 Italy Takao Shimizu National Center for Global Health and Medicine Shinjyuku Tokyo 166-8655 Japan Takehiko Yokomizo Department of Biochemistry Juntendo University School of Medicine Hongo 2-1-1 Bunkyo-ku Tokyo 113-8421 Japan