Protease-activated receptor


Protease-activated receptor

protein
Name = coagulation factor II (thrombin) receptor
caption =


width =
HGNCid = 3537
Symbol = F2R
AltSymbols = PAR1
EntrezGene = 2149
OMIM = 187930
RefSeq = NM_001992
UniProt = P25116
PDB =
ECnumber =
Chromosome = 5
Arm = q
Band = 13
LocusSupplementaryData =
protein
Name = coagulation factor II (thrombin) receptor-like 1
caption =


width =
HGNCid = 3538
Symbol = F2RL1
AltSymbols = PAR2, GPR11
EntrezGene = 2150
OMIM = 600933
RefSeq = NM_005242
UniProt = P55085
PDB =
ECnumber =
Chromosome = 5
Arm = q
Band = 13
LocusSupplementaryData =
protein
Name = coagulation factor II (thrombin) receptor-like 2
caption =


width =
HGNCid = 3539
Symbol = F2RL2
AltSymbols = PAR3
EntrezGene = 2151
OMIM = 601919
RefSeq = NM_004101
UniProt = O00254
PDB =
ECnumber =
Chromosome = 5
Arm = q
Band = 13
LocusSupplementaryData =
protein
Name = coagulation factor II (thrombin) receptor-like 3
caption =


width =
HGNCid = 3540
Symbol = F2RL3
AltSymbols = PAR4
EntrezGene = 9002
OMIM = 602779
RefSeq = NM_003950
UniProt = Q96RI0
PDB =
ECnumber =
Chromosome = 19
Arm = p
Band = 12
LocusSupplementaryData =

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.cite journal |author=Macfarlane SR, Seatter MJ, Kanke T, Hunter GD, Plevin R |title=Proteinase-activated receptors |journal= Pharmacol Rev |volume= 53 |issue= 2 |pages= 245–82 |year= 2001| doi = |pmid= 11356985 | url = http://pharmrev.aspetjournals.org/cgi/content/abstract/53/2/245 |format=abstract]

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

External links

* [http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1351 IUPHAR GPCR Database - Protease-activated receptors]
*


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