Heterologously expressed formyl peptide receptor 2 (FPR2/ALX) does not respond to lipoxin A₄

Biochem Pharmacol. 2013 Jun 15;85(12):1795-802. doi: 10.1016/j.bcp.2013.04.019. Epub 2013 May 1.

Abstract

Lipoxin A₄ (LXA₄) has been described as an anti-inflammatory mediator, which exerts its effects through the formyl peptide receptor FPR2, also known as ALX. However, there has been a controversy whether or not cells expressing FPR2/ALX, such as neutrophils, respond to LXA₄. We, therefore, systematically examined the ability of the human and murine forms of the receptor to respond to LXA₄. We show that both receptor orthologues responded to the FPR2/ALX peptide agonist WKYMVM when expressed heterologously. In contrast, LXA₄ from different sources neither increased [Ca²⁺](i) and extracellular-signal-regulated kinase (ERK) phosphorylation, nor did it induce a decrease in cAMP levels or a translocation of β-arrestin. Also, several LXA₄ analogs were found to be unable to signal through FPR2/ALX. We conclude that FPR2/ALX is not activated by LXA₄ and that the molecular mechanism by which LXA₄ functions still needs to be identified.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adaptor Proteins, Signal Transducing
  • Animals
  • CHO Cells
  • Cricetinae
  • Cricetulus
  • Cyclic AMP / antagonists & inhibitors
  • Cyclic AMP / metabolism
  • Gene Expression Regulation*
  • HEK293 Cells
  • Humans
  • Lipoxins / metabolism
  • Lipoxins / physiology*
  • Mice
  • Receptors, Formyl Peptide / administration & dosage*
  • Receptors, Formyl Peptide / biosynthesis
  • Receptors, Formyl Peptide / metabolism*
  • Receptors, Formyl Peptide / physiology
  • Receptors, Lipoxin / biosynthesis
  • Receptors, Lipoxin / metabolism*

Substances

  • Adaptor Proteins, Signal Transducing
  • FPR2 protein, human
  • Fpr1 protein, mouse
  • HSH2 protein, mouse
  • Lipoxins
  • Receptors, Formyl Peptide
  • Receptors, Lipoxin
  • lipoxin A4
  • Cyclic AMP