関: PAR、proteinase-activated receptor

WordNet

aerate (sewage) so as to favor the growth of organisms that decompose organic matter (同)aerate
make (substances) radioactive
make active or more active; "activate an old file"
make more adsorptive; "activate a metal"
rendered active; e.g. rendered radioactive or luminescent or photosensitive or conductive
(of e.g. a molecule) made reactive or more reactive (同)excited
(military) set up and placed on active assignment; "a newly activated unit"
(of sewage) treated with aeration and bacteria to aid decomposition
a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response
any enzyme that catalyzes the splitting of proteins into smaller peptide fractions and amino acids by a process known as proteolysis (同)peptidase, proteinase, proteolytic_enzyme
any tropical African shrub of the genus Protea having alternate rigid leaves and dense colorful flower heads resembling cones

PrepTutorEJDIC

…'を'活動的にする / …‘に'放射能を与える / 〈物質〉'を'活性化する
=sense organ / 受信装置

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/08/31 21:49:24」(JST)

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coagulation factor II (thrombin) receptor-like 3
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]

Classification

There are 4 known protease-activated receptors or PARs, 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

PARs are activated by the action of serine proteases such as thrombin (acts on PARs 1, 3 and 4) and trypsin (PAR 2).^[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 (Rho and Ras activation) and q (calcium signalling) to cause cellular actions.

Function

The cellular effects of thrombin are mediated by protease-activated receptors (PARs). Thrombin signalling in platelets contributes to hemostasis and thrombosis. Endothelial PARs participate in the regulation of vascular tone and permeability while in vascular smooth muscle they mediate contraction, proliferation, and hypertrophy. PARs contribute to the pro-inflammatory response observed in atherosclerosis and restenosis. Recent research has also implicated these novel receptors in muscle growth and bone cell differentiation and proliferation.^[3]

In T cells, activation of PAR1, PAR2 and PAR3 induce tyrosine phosphorylation of VAV1. Activation of PARs also led to an increase in tyrosine phosphorylation of ZAP-70 and SLP-76, two key proteins in T cell receptor (TCR) signalling.^[4]

References

^ Macfarlane SR, Seatter MJ, Kanke T, Hunter GD, Plevin R (2001). "Proteinase-activated receptors" (abstract). Pharmacol Rev 53 (2): 245–82. PMID 11356985.
^ Coughlin SR, Camerer E (January 2003). "PARticipation in inflammation". J. Clin. Invest. 111 (1): 25–7. doi:10.1172/JCI17564. PMC 151847. PMID 12511583.
^ Martorell L, Martínez-González J, Rodríguez C, Gentile M, Calvayrac O, Badimon L (February 2008). "Thrombin and protease-activated receptors (PARs) in atherothrombosis". Thromb. Haemost. 99 (2): 305–15. doi:10.1160/TH07-08-0481. PMID 18278179.
^ Bar-Shavit R, Maoz M, Yongjun Y, Groysman M, Dekel I, Katzav S (January 2002). "Signalling pathways induced by protease-activated receptors and integrins in T cells". Immunology 105 (1): 35–46. doi:10.1046/j.0019-2805.2001.01351.x. PMC 1782632. PMID 11849313.

External links

"Protease-Activated Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
Proteinase-Activated Receptors at the US National Library of Medicine Medical Subject Headings (MeSH)

This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it.

UpToDate Contents

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1. 非ST上昇型急性冠症候群における抗血小板薬 antiplatelet agents in acute non st elevation acute coronary syndromes
2. 止血の概要 overview of hemostasis
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4. 心血管疾患の二次予防 secondary prevention of cardiovascular disease
5. 血小板生物学 platelet biology

English Journal

Activation of PAR1 in the lateral hypothalamus of rats enhances food intake and REMS through CB1R.

Pérez-Morales M, Alvarado-Capuleño I, López-Colomé AM, Méndez-Díaz M, Ruiz-Contreras AE, Prospéro-García O.SourceaLaboratory of Cannabinoids, Department of Physiology, School of Medicine bNeuroscience Division, Institute of Cellular Physiology cLaboratory of Cognitive Neurogenomics, National Autonomus University of México (UNAM), DF, México.
Neuroreport.Neuroreport.2012 Oct 3;23(14):814-8.
The activation of protease-activated receptor 1 (PAR1) in cultured rat hippocampal neurons triggers synaptic retrograde signaling through the endocannabinoid 2-arachidonoylglycerol, thereby activating the cannabinoid receptor 1 (CB1R). CB1R is a metabotropic receptor activated by marihuana and endoc
PMID 22889888

Role of cockroach proteases in allergic disease.

Page K.SourceDivision of Critical Care Medicine, Cincinnati Children's Hospital Medical Center, 3333 Burnet Ave ML7006, Cincinnati, OH, USA, Kristen.page@cchmc.org.
Current allergy and asthma reports.Curr Allergy Asthma Rep.2012 Oct;12(5):448-55.
Allergic asthma is on the rise in developed countries, and cockroach exposure is a major risk factor for the development of asthma. In recent years, a number of studies have investigated the importance of allergen-associated proteases in modulating allergic airway inflammation. Many of the studies h
PMID 22644866

Japanese Journal

Protease-Activated ReceptorStimulated Interleukin-6 Expression in Endometriosis-Like Lesions in an Experimental Mouse Model of Endometriosis

Shinohara Akihiro,Kutsukake Masahiko,Takahashi Mirai [他]
Journal of pharmacological sciences 119(1), 40-51, 2012-05
NAID 40019255670

慢性腎臓病(CKD)における凝固系と凝固第Xa因子の役割 (慢性腎臓病(CKD)の概念 : 腎臓病の早期発見・早期治療を目指して)

小野孝彦
薬学雑誌 132(4), 449-453, 2012
NAID 40019258372

Related Pictures

★リンクテーブル★

リンク元	「PAR」「プロテアーゼ受容体」「proteinase-activated receptor」「プロテアーゼ活性化受容体」
拡張検索	「protease-activated receptor 2」「protease-activated receptor 1」
関連記事	「activated」「activate」

「PAR」

coagulation factor II (thrombin) receptor-like 2
Identifiers
Symbol	F2RL2
Alt. symbols	PAR3
Entrez	2151
HUGO	3539
OMIM	601919
RefSeq	NM_004101
UniProt	O00254
Other data
Locus	Chr. 5 q13

coagulation factor II (thrombin) receptor-like 1
Identifiers
Symbol	F2RL1
Alt. symbols	PAR2, GPR11
Entrez	2150
HUGO	3538
OMIM	600933
RefSeq	NM_005242
UniProt	P55085
Other data
Locus	Chr. 5 q13

coagulation factor II (thrombin) receptor
Identifiers
Symbol	F2R
Alt. symbols	PAR1
Entrez	2149
HUGO	3537
OMIM	187930
RefSeq	NM_001992
UniProt	P25116
Other data
Locus	Chr. 5 q13