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Protease-activated receptor

Encyclopedia : P : PR : PRO : Protease-activated receptor


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|- | colspan="2" bgcolor="#dddddd" | Identifiers |- | bgcolor="#e7dcc3" | Symbol(s) | bgcolor="#eeeeee" | [F2R] |- | bgcolor="#e7dcc3" | Entrez | bgcolor="#eeeeee" | [2149] |- class="hiddenStructure" | bgcolor="#e7dcc3" | OMIM | bgcolor="#eeeeee" | [187930] |- | bgcolor="#e7dcc3" | RefSeq | bgcolor="#eeeeee" | [NM_001992] |- | bgcolor="#e7dcc3" | UniProt | bgcolor="#eeeeee" | [P25116] |- class="hiddenStructure" | bgcolor="#e7dcc3" | PDB | bgcolor="#eeeeee" | [] |- | colspan="2" bgcolor="#dddddd" | Other data |- class="hiddenStructure" | bgcolor="#e7dcc3" | EC number | bgcolor="#eeeeee" | [] |- | bgcolor="#e7dcc3" | Locus | bgcolor="#eeeeee" | Chr. 5[q13] |- |}
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|- | colspan="2" bgcolor="#dddddd" | Identifiers |- | bgcolor="#e7dcc3" | Symbol(s) | bgcolor="#eeeeee" | [F2RL1] GPR11 |- | bgcolor="#e7dcc3" | Entrez | bgcolor="#eeeeee" | [2150] |- class="hiddenStructure" | bgcolor="#e7dcc3" | OMIM | bgcolor="#eeeeee" | [600933] |- | bgcolor="#e7dcc3" | RefSeq | bgcolor="#eeeeee" | [NM_005242] |- | bgcolor="#e7dcc3" | UniProt | bgcolor="#eeeeee" | [P55085] |- class="hiddenStructure" | bgcolor="#e7dcc3" | PDB | bgcolor="#eeeeee" | [] |- | colspan="2" bgcolor="#dddddd" | Other data |- class="hiddenStructure" | bgcolor="#e7dcc3" | EC number | bgcolor="#eeeeee" | [] |- | bgcolor="#e7dcc3" | Locus | bgcolor="#eeeeee" | Chr. 5[q13] |- |}
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|- | colspan="2" bgcolor="#dddddd" | Identifiers |- | bgcolor="#e7dcc3" | Symbol(s) | bgcolor="#eeeeee" | [F2RL2] |- | bgcolor="#e7dcc3" | Entrez | bgcolor="#eeeeee" | [2151] |- class="hiddenStructure" | bgcolor="#e7dcc3" | OMIM | bgcolor="#eeeeee" | [601919] |- | bgcolor="#e7dcc3" | RefSeq | bgcolor="#eeeeee" | [NM_004101] |- | bgcolor="#e7dcc3" | UniProt | bgcolor="#eeeeee" | [O00254] |- class="hiddenStructure" | bgcolor="#e7dcc3" | PDB | bgcolor="#eeeeee" | [] |- | colspan="2" bgcolor="#dddddd" | Other data |- class="hiddenStructure" | bgcolor="#e7dcc3" | EC number | bgcolor="#eeeeee" | [] |- | bgcolor="#e7dcc3" | Locus | bgcolor="#eeeeee" | Chr. 5[q13] |- |}
|- | align="center" colspan="2" |
|- | colspan="2" bgcolor="#dddddd" | Identifiers |- | bgcolor="#e7dcc3" | Symbol(s) | bgcolor="#eeeeee" | [F2RL3] |- | bgcolor="#e7dcc3" | Entrez | bgcolor="#eeeeee" | [9002] |- class="hiddenStructure" | bgcolor="#e7dcc3" | OMIM | bgcolor="#eeeeee" | [602779] |- | bgcolor="#e7dcc3" | RefSeq | bgcolor="#eeeeee" | [NM_003950] |- | bgcolor="#e7dcc3" | UniProt | bgcolor="#eeeeee" | [Q96RI0] |- class="hiddenStructure" | bgcolor="#e7dcc3" | PDB | bgcolor="#eeeeee" | [] |- | colspan="2" bgcolor="#dddddd" | Other data |- class="hiddenStructure" | bgcolor="#e7dcc3" | EC number | bgcolor="#eeeeee" | [] |- | bgcolor="#e7dcc3" | Locus | bgcolor="#eeeeee" | Chr. 19[p12] |- |} A protease-activated receptor is a cell receptor that is activated by cleavage of part of its extracellular domain. It is located not only on platelets, but also on endothelial cells, myocytes and neurons.

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.

PAR's are activated by the action of serine based proteases such as thrombin (acts on PAR's 1, 3 and 4) and trypsin (PAR 2). These enzymes act upon the N-terminus of the receptor, and cause the formation of a tethered ligand. In this 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.

Recent research has implicated these novel receptors in the inflammatory response (including arthritis), muscle growth, and bone cell differentiation and proliferation.

 


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