[Physiological functions of protease-activated receptor-2].
Protease-activated receptors (PARs) are a family of G-protein-coupled-seven-trans-membrane-domain-receptors activated by specific proteases, consisting of four family members. PAR-2, a receptor activated by trypsin, tryptase or coagulation factors VIIa and Xa, is unevenly distributed throughout the mammalian body, modulating multiple physiological functions. In the gastrointestinal tract, PAR-2 is involved in gastric mucosal cytoprotection, smooth muscle motility modulation, salivary and pancreatic exocrine secretion, intestinal ionic transport, etc. In the circulatory system, endothelial PAR-2, upon activation, induces vascular relaxation by mechanisms dependent on nitric oxide or endothelium-derived hyperpolarizing factor (EDHF), resulting in hypotension in vivo. In the respiratory system, PAR-2 appears to play a dual role, being pro- and anti-inflammatory. In the nervous system, PAR-2 present in capsaicin-sensitive sensory neurons participates in processing of pain information. PAR-2 is thus involved in a variety of physiological and pathophysiological functions. PAR-2 is now considered one of the most important molecules as a target for drug development.
Kawabata
Atsufumi
A
Department of Physiology and Pathophysiology, School of Pharmaceutical Sciences, Kinki University, Higashi-Osaka, Japan. kawabata@phar.kindai.ac.jp
D000818:Animals; D002320:Cardiovascular Physiological Phenomena; D004068:Digestive System Physiological Phenomena; D015195:Drug Design; D006801:Humans; D009424:Nervous System Physiological Phenomena; D044464:Receptor, PAR-2; D018179:Receptors, Thrombin / Q000819:agonists / Q000037:antagonists & inhibitors / Q000502:physiology*; D012143:Respiratory Physiological Phenomena; D012697:Serine Endopeptidases / Q000502:physiology; D015398:Signal Transduction; D014357:Trypsin / Q000502:physiology; D053802:Tryptases
D044464:Receptor, PAR-2; D018179:Receptors, Thrombin; D012697:Serine Endopeptidases; D014357:Trypsin; D053802:Tryptases