Antiflammin-2 activates the human formyl-peptide receptor like 1

ScientificWorldJournal. 2006 Oct 25;6:1375-84. doi: 10.1100/tsw.2006.247.


The anti-inflammatory actions of the nonapeptide antiflammin-2, identified by homology with uteroglobin and annexin-A1 sequences, have been described in some detail, yet its mechanisms of action remain elusive. Since recent data indicate an involvement of the formyl peptide receptor (FPR)-like 1 (or FPRL-1) in the effects of annexin-A1, we have tested here the effect of antiflammin-2 with respect to this receptor family. Using HEK-293 cells expressing either human FPR and FPRL-1, and an annexin-A1 peptide as tracer ([125I-Tyr]-Ac2-26), we found that antiflammin-2 competed for binding only at FPRL-1, and not FPR, with an approximate EC50 of 1 mM. In line with data produced for the full-length protein, genuine receptor activation by antiflammin-2 was confirmed by rapid phosphorylation of extracellular-regulated kinase 1 and 2. Finally, study of the neutrophil interaction with activated endothelium under flow demonstrated an inhibitory effect of antiflammin-2, thus providing functional support to a role for the antiflammin-2/FPRL-1 anti-inflammatory axis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Binding, Competitive
  • Cells, Cultured
  • Humans
  • Kidney / cytology
  • Kidney / embryology
  • Mitogen-Activated Protein Kinase 1 / metabolism
  • Mitogen-Activated Protein Kinase 3 / metabolism
  • Oligopeptides / pharmacology*
  • Peptide Fragments / pharmacology*
  • Phosphorylation
  • Receptors, Formyl Peptide / drug effects*
  • Receptors, Formyl Peptide / physiology
  • Receptors, Lipoxin / drug effects*
  • Receptors, Lipoxin / physiology


  • Anti-Inflammatory Agents, Non-Steroidal
  • FPR2 protein, human
  • Oligopeptides
  • Peptide Fragments
  • Receptors, Formyl Peptide
  • Receptors, Lipoxin
  • antiflammin P2
  • Mitogen-Activated Protein Kinase 1
  • Mitogen-Activated Protein Kinase 3