Protease-activated receptors: Protease signaling in the gastrointestinal tract

Silvia Amadesi, Nigel Bunnett

Research output: Contribution to journalReview articlepeer-review

Abstract

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 (US)
Pages (from-to)551-556
Number of pages6
JournalCurrent Opinion in Pharmacology
Volume4
Issue number6
DOIs
StatePublished - Dec 2004

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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