G-protein-coupled receptor expression, function, and signaling in macrophages

J Leukoc Biol. 2007 Jul;82(1):16-32. doi: 10.1189/jlb.0107051. Epub 2007 Apr 24.


G-protein-coupled receptors (GPCRs) are widely targeted in drug discovery. As macrophages are key cellular mediators of acute and chronic inflammation, we review here the role of GPCRs in regulating macrophage function, with a focus on contribution to disease pathology and potential therapeutic applications. Within this analysis, we highlight novel GPCRs with a macrophage-restricted expression profile, which provide avenues for further exploration. We also review an emerging literature, which documents novel roles for GPCR signaling components in GPCR-independent signaling in macrophages. In particular, we examine the crosstalk between GPCR and TLR signaling pathways and highlight GPCR signaling molecules which are likely to have uncharacterized functions in this cell lineage.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Humans
  • Macrophages / chemistry
  • Macrophages / physiology
  • Receptor Cross-Talk
  • Receptors, G-Protein-Coupled / genetics
  • Receptors, G-Protein-Coupled / metabolism
  • Receptors, G-Protein-Coupled / physiology*
  • Signal Transduction*
  • Toll-Like Receptors / metabolism
  • Toll-Like Receptors / physiology


  • Receptors, G-Protein-Coupled
  • Toll-Like Receptors