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Protease-activated receptors: how proteases signal to cells.
- Source :
-
Current opinion in pharmacology [Curr Opin Pharmacol] 2001 Dec; Vol. 1 (6), pp. 575-82. - Publication Year :
- 2001
-
Abstract
- Certain proteases from the circulation, mast cells and elsewhere signal directly to cells by cleaving protease-activated receptors (PARs), members of a new subfamily of G-protein-coupled receptor. Cleavage exposes a tethered ligand domain that binds to and activates the cleaved receptors. Advances in the past year have improved our understanding of the molecular mechanisms of this signaling and how it is switched off. It is now recognized that PARs play important roles in 'emergency situations' - such as trauma, when there is generation or release of proteases - and are involved in coagulation, inflammation, pain, healing and protection. Selective antagonists or agonists of these receptors may be useful therapeutic agents for the treatment of human diseases.
- Subjects :
- Animals
Digestive System enzymology
Endopeptidases metabolism
Humans
Intestinal Diseases enzymology
Mice
Polymorphism, Genetic
Protein Binding
Receptor, PAR-1
Receptor, PAR-2
Receptors, Thrombin genetics
Receptors, Thrombin metabolism
Endopeptidases physiology
Receptors, Thrombin physiology
Signal Transduction physiology
Subjects
Details
- Language :
- English
- ISSN :
- 1471-4892
- Volume :
- 1
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Current opinion in pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 11757812
- Full Text :
- https://doi.org/10.1016/s1471-4892(01)00099-6