Protease-activated receptor
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| Identifiers | |
| Symbol | F2R |
| Alt. Symbols | PAR1 |
| Entrez | 2149 |
| HUGO | 3537 |
| OMIM | 187930 |
| RefSeq | NM_001992 |
| UniProt | P25116 |
| Other data | |
| Locus | Chr. 5 q13 |
| Identifiers | |
| Symbol | F2RL1 |
| Alt. Symbols | PAR2, GPR11 |
| Entrez | 2150 |
| HUGO | 3538 |
| OMIM | 600933 |
| RefSeq | NM_005242 |
| UniProt | P55085 |
| Other data | |
| Locus | Chr. 5 q13 |
| Identifiers | |
| Symbol | F2RL2 |
| Alt. Symbols | PAR3 |
| Entrez | 2151 |
| HUGO | 3539 |
| OMIM | 601919 |
| RefSeq | NM_004101 |
| UniProt | O00254 |
| Other data | |
| Locus | Chr. 5 q13 |
| Identifiers | |
| Symbol | F2RL3 |
| Alt. Symbols | PAR4 |
| Entrez | 9002 |
| HUGO | 3540 |
| OMIM | 602779 |
| RefSeq | NM_003950 |
| UniProt | Q96RI0 |
| Other data | |
| Locus | Chr. 19 p12 |
Protease-activated receptors are a subfamily of related G protein-coupled receptors that are activated by cleavage of part of their extracellular domain. They are highly expressed in platelets, but also on endothelial cells, myocytes and neurons.[1]
Contents |
Classification
There are 4 known protease-activated receptors or PAR's, numbered from one to four. These receptors are members of the seven transmembrane G-protein-coupled receptor superfamily, and are expressed throughout the body.
Activation
PAR's are activated by the action of serine proteases such as thrombin (acts on PAR's 1, 3 and 4) and trypsin (PAR 2). These enzymes cleave the N-terminus of the receptor, which in turn acts as a tethered ligand. In the cleaved state, part of the receptor itself acts as the agonist, causing a physiological response.
Most of the PAR family act through the actions of G-proteins i (cAMP inhibitory), 12/13 (Raf/Ras activation) and q (calcium signalling) to cause cellular actions.
Function
Recent research has implicated these novel receptors in the inflammatory response (including arthritis), muscle growth, and bone cell differentiation and proliferation.
References
- ↑ Macfarlane SR, Seatter MJ, Kanke T, Hunter GD, Plevin R (2001). "Proteinase-activated receptors". Pharmacol Rev 53 (2): 245-82. PMID 11356985.
External links
Template:Membrane-protein-stub
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
