プロテアーゼ活性化受容体2、プロテアーゼ活性化レセプター2

関: PAR-2、PAR-2 receptor、proteinase-activated receptor 2、trypsin 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

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/04/19 21:12:33」(JST)

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[Wiki en表示]

Protease activated receptor 2 (PAR2) also known as coagulation factor II (thrombin) receptor-like 1 (F2RL1) or G-protein coupled receptor 11 (GPR11) is a protein that in humans is encoded by the F2RL1 gene. PAR2 modulates inflammatory responses and acts as a sensor for proteolytic enzymes generated during infection.^[1]

Gene

The F2RL1 gene contains two exons and is widely expressed in human tissues. The predicted protein sequence is 83% identical to the mouse receptor sequence.^[2]

Mechanism of activation

PAR2 is a member of the large family of 7-transmembrane receptors that couple to guanosine-nucleotide-binding proteins. PAR2 is also a member of the protease-activated receptor family. It is activated by trypsin, but not by thrombin. It is activated by proteolytic cleavage of its extracellular amino terminus. The new amino terminus functions as a tethered ligand and activates the receptor. Additionally, these receptors can be activated by exogenous proteases, such as house dust mite protein Der P9.^[3] These receptors can also be activated non-protealytically, by exogenous peptide sequences that mimic the final amino acids of the tethered ligand.^[4]

Agonists and antagonists

Potent and selective small molecule agonists and antagonists for PAR2 have been discovered.^[5]^[6]

References

^ Lee SE, Jeong SK, Lee SH (November 2010). "Protease and protease-activated receptor-2 signaling in the pathogenesis of atopic dermatitis". Yonsei Med. J. 51 (6): 808–22. doi:10.3349/ymj.2010.51.6.808. PMC 2995962. PMID 20879045.
^ "Entrez Gene: F2RL1 coagulation factor II (thrombin) receptor-like 1".
^ Sun G, Stacey MA, Schmidt M, Mori L, Mattoli S (July 2001). "Interaction of mite allergens Der p3 and Der p9 with protease-activated receptor-2 expressed by lung epithelial cells". J. Immunol. 167 (2): 1014–21. PMID 11441110.
^ Kawabata A, Kanke T, Yonezawa D, Ishiki T, Saka M, Kabeya M, Sekiguchi F, Kubo S, Kuroda R, Iwaki M, Katsura K, Plevin R (June 2004). "Potent and metabolically stable agonists for protease-activated receptor-2: evaluation of activity in multiple assay systems in vitro and in vivo". J. Pharmacol. Exp. Ther. 309 (3): 1098–107. doi:10.1124/jpet.103.061010. PMID 14976227.
^ Gardell LR, Ma JN, Seitzberg JG, Knapp AE, Schiffer HH, Tabatabaei A, Davis CN, Owens M, Clemons B, Wong KK, Lund B, Nash NR, Gao Y, Lameh J, Schmelzer K, Olsson R, Burstein ES (December 2008). "Identification and characterization of novel small-molecule protease-activated receptor 2 agonists". J. Pharmacol. Exp. Ther. 327 (3): 799–808. doi:10.1124/jpet.108.142570. PMID 18768780.
^ Barry GD, Suen JY, Le GT, Cotterell A, Reid RC, Fairlie DP (October 2010). "Novel agonists and antagonists for human protease activated receptor 2". J. Med. Chem. 53 (20): 7428–40. doi:10.1021/jm100984y. PMID 20873792.

External links

"Protease-Activated Receptors: PAR2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

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

UpToDate Contents

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1. 心不全の疫学および原因 epidemiology and causes of heart failure
2. 血小板生物学 platelet biology
3. 血栓溶解異常による血栓性および出血性疾患 thrombotic and hemorrhagic disorders due to abnormal fibrinolysis
4. 成人における緊急気道管理困難に使用するデバイス devices for difficult emergency airway management in adults
5. 非メンデル遺伝のパターン non mendelian inheritance patterns

English Journal

Wnt signaling pathway in rheumatoid arthritis, with special emphasis on the different roles in synovial inflammation and bone remodeling.

Miao CG, Yang YY, He X, Li XF, Huang C, Huang Y, Zhang L, Lv XW, Jin Y, Li J.SourceSchool of Pharmacy, Institute for Liver Diseases of Anhui Medical University, Anhui Key Laboratory of Bioactivity of Natural Products, Anhui Medical University, Hefei 230032, China.
Cellular signalling.Cell Signal.2013 Oct;25(10):2069-78. doi: 10.1016/j.cellsig.2013.04.002. Epub 2013 Apr 17.
Rheumatoid arthritis (RA) is a chronic symmetrical autoimmune disease of unknown etiology that affects primarily the diarthrodial joints. Characteristic features of RA pathogenesis are synovial inflammation and proliferation accompanied by cartilage erosion and bone loss. Fibroblast-like synoviocyte
PMID 23602936

Hemophagocytosis-mediated keratinization in oral carcinoma in situ and squamous cell carcinoma: a possible histopathogenesis of keratin pearls.

Al-Eryani K, Cheng J, Abé T, Yamazaki M, Maruyama S, Tsuneki M, Essa A, Babkair H, Saku T.SourceDivision of Oral Pathology, Department of Tissue Regeneration and Reconstruction, Niigata University Graduate School of Medical and Dental Sciences, Chuo-Ku, Niigata, Japan.
Journal of cellular physiology.J Cell Physiol.2013 Oct;228(10):1977-88. doi: 10.1002/jcp.24364.
Although the histopathogenetic process of keratin pearls is still poorly understood, acceleration of keratinization in squamous cell carcinoma (SCC) cells may represent one possible therapeutic avenue. Based on our histopathological observations, we have hypothesized that SCC cells are keratinized b
PMID 23526486

Diallylsulfide attenuates excessive collagen production and apoptosis in a rat model of bleomycin induced pulmonary fibrosis through the involvement of protease activated receptor-2.

Kalayarasan S, Sriram N, Soumyakrishnan S, Sudhandiran G.SourceUniversity of Madras, Department of Biochemistry, Cell Biology Laboratory, Guindy Campus, Chennai 600 025, Tamil Nadu, India. Electronic address: kalaivasanbio@gmail.com.
Toxicology and applied pharmacology.Toxicol Appl Pharmacol.2013 Sep 1;271(2):184-95. doi: 10.1016/j.taap.2013.04.021. Epub 2013 May 5.
Pulmonary fibrosis (PF) can be a devastating lung disease. It is primarily caused by inflammation leading to severe damage of the alveolar epithelial cells. The pathophysiology of PF is not yet been clearly defined, but studying lung parenchymal injury by involving reactive oxygen species (ROS) thro
PMID 23656969

Japanese Journal

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

Shinohara Akihiro,Kutsukake Masahiko,Takahashi Mirai [他],KYO Satoru,TACHIKAWA Eiichi,TAMURA Kazuhiro
Journal of pharmacological sciences 119(1), 40-51, 2012-05-20
… The present study was undertaken to investigate the function of protease-activated receptor (PAR) in endometriotic lesions using a mouse model of endometriosis. … IL-6 expression induced by PAR activation was blocked by the treatment of cells with serine protease inhibitors. …
NAID 10030760253

慢性腎臓病（CKD）における凝固系と凝固第Xa因子の役割

小野孝彦
薬学雑誌 132(4), 449-453, 2012
… Factor Xa activates various cell types through protease-activated receptor 2 (PAR2). …
NAID 130001872047

JKCF2-5 A synonymous variation in Protease-Activated Receptor-2 is associated with atopy in Korean children(Atopic eczema and related diseases,Free Paper Session 2,Japan-Korea-China Joint Symposium)

Lee Ji Hyun,Kim Kyung Won,Gee Heon Yung,Lee Jaechun,Lee Keun-Hwa,Park Hae-Sim,Kim Seung-Hyun,Kim So Won,Kim Kyu-Earn,Lee Min Goo,Sohn Myung Hyun
アレルギー 60(9・10), 1317, 2011-10-10
NAID 110008912146

「プロテアーゼ活性化受容体2」

Coagulation factor II (thrombin) receptor-like 1
Identifiers
Symbols	F2RL1 ; GPR11; PAR2
External IDs	OMIM: 600933 MGI: 101910 HomoloGene: 21087 IUPHAR: PAR2 ChEMBL: 5963 GeneCards: F2RL1 Gene
Gene ontology
Molecular function	• G-protein alpha-subunit binding; • receptor activity; • G-protein coupled receptor activity; • receptor binding; • protein binding; • thrombin receptor activity; • G-protein beta-subunit binding;
Cellular component	• Golgi apparatus; • plasma membrane; • integral to plasma membrane; • pseudopodium;
Biological process	• T cell activation involved in immune response; • positive regulation of leukocyte chemotaxis; • positive regulation of cytokine secretion involved in immune response; • positive regulation of glomerular filtration; • inflammatory response; • G-protein coupled receptor signaling pathway; • elevation of cytosolic calcium ion concentration; • blood coagulation; • negative regulation of tumor necrosis factor-mediated signaling pathway; • positive regulation of phosphatidylinositol 3-kinase cascade; • regulation of blood coagulation; • positive regulation of cell migration; • positive regulation of actin filament depolymerization; • positive regulation of pseudopodium assembly; • positive regulation of superoxide anion generation; • positive regulation of toll-like receptor 2 signaling pathway; • negative regulation of toll-like receptor 3 signaling pathway; • positive regulation of toll-like receptor 3 signaling pathway; • positive regulation of toll-like receptor 4 signaling pathway; • positive regulation of Rho protein signal transduction; • chemokine (C-C motif) ligand 2 secretion; • neutrophil activation; • regulation of I-kappaB kinase/NF-kappaB cascade; • positive regulation of I-kappaB kinase/NF-kappaB cascade; • positive regulation of eosinophil degranulation; • innate immune response; • positive regulation of vasodilation; • positive regulation of transcription from RNA polymerase II promoter; • regulation of JNK cascade; • negative regulation of JNK cascade; • positive regulation of JNK cascade; • interleukin-1 beta secretion; • leukocyte migration; • positive regulation of chemotaxis; • positive regulation of positive chemotaxis; • defense response to virus; • positive regulation of phagocytosis, engulfment; • establishment of endothelial barrier; • positive regulation of ERK1 and ERK2 cascade; • leukocyte proliferation; • positive regulation of neutrophil mediated killing of gram-negative bacterium; • interleukin-10 secretion; • interferon-gamma secretion; • chemokine secretion; • negative regulation of chemokine secretion; • mature dendritic cell differentiation; • positive regulation of renin secretion into blood stream; • positive regulation of interleukin-8 secretion; • positive regulation of interleukin-6 secretion;
	Sources: Amigo / QuickGO
RNA expression pattern
	More reference expression data
Orthologs
	This box: view; talk; edit;

　　[★]

英: protease-activated receptor 2、proteinase-activated receptor 2、PAR-2 receptor、PAR-2
関: PAR-2受容体、PAR-2レセプター、プロテアーゼ活性化レセプター2、トリプシン受容体

「PAR-2 receptor」

　　[★]

プロテアーゼ活性化受容体2、PAR-2受容体、PAR-2レセプター

関: PAR-2、protease-activated receptor 2、proteinase-activated receptor 2、trypsin receptor

「PAR-2」

　　[★]

プロテアーゼ活性化受容体2

関: PAR-2 receptor、protease-activated receptor 2、proteinase-activated receptor 2

「trypsin receptor」

　　[★]

トリプシン受容体、トリプシンレセプター

関: PAR-2 receptor、protease-activated receptor 2

「proteinase-activated receptor 2」

　　[★]

プロテアーゼ活性化受容体2

関: PAR-2、PAR-2 receptor、protease-activated receptor 2

「activated」

　　[★]

adj.

活性化の、活性化型の、賦活化の

関: activate、activated form、activation、turn on

「activate」

　　[★]

v.

活性化する、賦活化する、賦活する

関: activated、activation、turn on

[pmid20879045-1] Lee SE, Jeong SK, Lee SH (November 2010). "Protease and protease-activated receptor-2 signaling in the pathogenesis of atopic dermatitis". Yonsei Med. J. 51 (6): 808–22. doi:10.3349/ymj.2010.51.6.808. PMC 2995962. PMID 20879045.

[2] "Entrez Gene: F2RL1 coagulation factor II (thrombin) receptor-like 1".

[pmid11441110-3] Sun G, Stacey MA, Schmidt M, Mori L, Mattoli S (July 2001). "Interaction of mite allergens Der p3 and Der p9 with protease-activated receptor-2 expressed by lung epithelial cells". J. Immunol. 167 (2): 1014–21. PMID 11441110.

[pmid14976227-4] Kawabata A, Kanke T, Yonezawa D, Ishiki T, Saka M, Kabeya M, Sekiguchi F, Kubo S, Kuroda R, Iwaki M, Katsura K, Plevin R (June 2004). "Potent and metabolically stable agonists for protease-activated receptor-2: evaluation of activity in multiple assay systems in vitro and in vivo". J. Pharmacol. Exp. Ther. 309 (3): 1098–107. doi:10.1124/jpet.103.061010. PMID 14976227.

[pmid18768780-5] Gardell LR, Ma JN, Seitzberg JG, Knapp AE, Schiffer HH, Tabatabaei A, Davis CN, Owens M, Clemons B, Wong KK, Lund B, Nash NR, Gao Y, Lameh J, Schmelzer K, Olsson R, Burstein ES (December 2008). "Identification and characterization of novel small-molecule protease-activated receptor 2 agonists". J. Pharmacol. Exp. Ther. 327 (3): 799–808. doi:10.1124/jpet.108.142570. PMID 18768780.

[pmid20873792-6] Barry GD, Suen JY, Le GT, Cotterell A, Reid RC, Fairlie DP (October 2010). "Novel agonists and antagonists for human protease activated receptor 2". J. Med. Chem. 53 (20): 7428–40. doi:10.1021/jm100984y. PMID 20873792.

リンク元	「プロテアーゼ活性化受容体2」「PAR-2 receptor」「PAR-2」「trypsin receptor」「proteinase-activated receptor 2」
関連記事	「activated」「activate」

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案内

protease-activated receptor 2