title: Protease-activated receptors: potential therapeutic targets in irritable bowel syndrome?
abstract: Protease-activated receptors (PARs) are a family of four G-protein-coupled receptors (PAR-1 to PAR-4) activated by the proteolytic cleavage of their N-terminal extracellular domain. This activation first involves the recognition of the extracellular domain by proteases, such as thrombin, but also trypsin or tryptase which are particularly abundant in the gastrointestinal tract, both under physiological circumstances and in several digestive diseases. Activation of PARs, particularly of PAR-1 and -2, modulates intestinal functions, such as gastrointestinal motility, visceral nociception, mucosal inflammatory response, and epithelial functions (intestinal secretion and permeability). As these physiological properties have been shown to be altered in various extents and combinations in different clinical presentations of irritable bowel syndrome, PARs appear as putative targets for future therapeutic intervention in these patients.
authors.affiliation: Centre Hospitalier Universitaire de Caen, Service d'Hépato-Gastro-Entérologie et Nutrition, Avenue de la Côte de Nacre, 14033 Caen Cedex, France.
authors.forename: Romain
authors.initials: R
authors.lastname: Gloro
authors.forename: Philippe
authors.initials: P
authors.lastname: Ducrotte
authors.forename: Jean-Marie
authors.initials: JM
authors.lastname: Reimund
mesh_terms: D006801:Humans; D043183:Irritable Bowel Syndrome / Q000188:drug therapy* / Q000378:metabolism*; D044462:Receptors, Proteinase-Activated / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism
chemical_list: D044462:Receptors, Proteinase-Activated