Protease-activated receptors: protease signaling in the gastrointestinal tract

Silvia Amadesi, Nigel Bunnett

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42 Citations (Scopus)


Serine proteases from the circulation, inflammatory cells, digestive glands and microorganisms can signal to cells by cleaving protease-activated receptors (PARs), a family of four G-protein-coupled receptors. Proteases cleave PARs at specific sites to expose tethered ligand domains that bind to and activate the cleaved receptors. Despite this irreversible mechanism of activation, PAR signaling is tightly regulated to prevent the uncontrolled stimulation of cells. Although PARs are found in all organ systems, protease signaling is of particular interest in the gastrointestinal tract, where proteases regulate neurotransmission, secretion, motility, epithelial permeability and intestinal inflammation, and can thus contribute to disease.
Original languageEnglish
Pages (from-to)551 - 556
Number of pages6
JournalCurrent Opinion in Pharmacology
Issue number6
Publication statusPublished - 2004

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