Protease-activated receptor 2 signaling in inflammation

Semin Immunopathol. 2012 Jan;34(1):133-49. doi: 10.1007/s00281-011-0289-1. Epub 2011 Oct 6.

Abstract

Protease-activated receptors (PARs) are G protein-coupled receptors that are activated by proteolytical cleavage of the amino-terminus and thereby act as sensors for extracellular proteases. While coagulation proteases activate PARs to regulate hemostasis, thrombosis, and cardiovascular function, PAR2 is also activated in extravascular locations by a broad array of serine proteases, including trypsin, tissue kallikreins, coagulation factors VIIa and Xa, mast cell tryptase, and transmembrane serine proteases. Administration of PAR2-specific agonistic and antagonistic peptides, as well as studies in PAR2 knockout mice, identified critical functions of PAR2 in development, inflammation, immunity, and angiogenesis. Here, we review these roles of PAR2 with an emphasis on the role of coagulation and other extracellular protease pathways that cleave PAR2 in epithelial, immune, and neuronal cells to regulate physiological and pathophysiological processes.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Blood Coagulation / genetics
  • Blood Coagulation / immunology
  • Blood Proteins / genetics
  • Blood Proteins / immunology
  • Blood Proteins / metabolism
  • Humans
  • Inflammation / genetics
  • Inflammation / immunology*
  • Inflammation / pathology
  • Mice
  • Mice, Knockout
  • Neovascularization, Physiologic / genetics
  • Neovascularization, Physiologic / immunology
  • Receptor, PAR-2 / genetics
  • Receptor, PAR-2 / immunology*
  • Signal Transduction / genetics
  • Signal Transduction / immunology*
  • Thrombosis / blood
  • Thrombosis / genetics
  • Thrombosis / immunology
  • Thrombosis / pathology

Substances

  • Blood Proteins
  • Receptor, PAR-2