- 関
- PAR-2 receptor、protease-activated receptor 2、proteinase-activated receptor 2
WordNet
- make a score (on a hole) equal to par
- (golf) the standard number of strokes set for each hole on a golf course, or for the entire course; "a par-5 hole"; "par for this course is 72"
- the 16th letter of the Roman alphabet (同)p
PrepTutorEJDIC
- 〈U〉同等,同価,同水準,同程度 / (また『par value』)〈U〉平価,額面価格 / 〈U〉(程度・質・状態・数量などの)平均,標準;(精神・健康などの)常態 / 〈C〉(ゴルフで)標準打数,パー / 《名詞の前にのみ用いて》平均の,標準の / 額面の
- (ゴルフで)〈1ホールまたは1コース〉‘を'基準打数でとる,パーで上がる
- personal assistant個人秘書 / public address [system]
- parking
- phosphorusの化学記号
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2014/09/29 01:48:32」(JST)
[Wiki en表示]
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
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Cellular component |
• Golgi apparatus
• plasma membrane
• integral component of plasma membrane
• pseudopodium
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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
• positive regulation of cytosolic calcium ion concentration
• blood coagulation
• negative regulation of tumor necrosis factor-mediated signaling pathway
• positive regulation of phosphatidylinositol 3-kinase signaling
• 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 signaling
• positive regulation of I-kappaB kinase/NF-kappaB signaling
• 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
• thrombin receptor signaling pathway
• 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
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Sources: Amigo / QuickGO |
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RNA expression pattern |
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More reference expression data |
Orthologs |
Species |
Human |
Mouse |
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Entrez |
2150 |
14063 |
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Ensembl |
ENSG00000164251 |
ENSMUSG00000021678 |
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UniProt |
P55085 |
P55086 |
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RefSeq (mRNA) |
NM_005242 |
NM_007974 |
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RefSeq (protein) |
NP_005233 |
NP_032000 |
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Location (UCSC) |
Chr 5:
76.11 – 76.13 Mb |
Chr 13:
95.51 – 95.53 Mb |
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PubMed search |
[1] |
[2] |
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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]
Contents
- 1 Gene
- 2 Mechanism of activation
- 3 Agonists and antagonists
- 4 See also
- 5 References
- 6 Further reading
- 7 External links
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]
See also
- Protease-activated receptor
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. doi:10.4049/jimmunol.167.2.1014. 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.
Further reading
- Kunzelmann K, Schreiber R, König J, Mall M (2003). "Ion transport induced by proteinase-activated receptors (PAR2) in colon and airways.". Cell Biochem. Biophys. 36 (2–3): 209–14. doi:10.1385/CBB:36:2-3:209. PMID 12139406.
- Kawabata A (2004). "PAR-2: structure, function and relevance to human diseases of the gastric mucosa". Expert Reviews in Molecular Medicine 4 (16): 1–17. doi:10.1017/S1462399402004799. PMID 14585156.
- Bushell T (2007). "The emergence of proteinase-activated receptor-2 as a novel target for the treatment of inflammation-related CNS disorders". J. Physiol. (Lond.) 581 (Pt 1): 7–16. doi:10.1113/jphysiol.2007.129577. PMC 2075212. PMID 17347265.
- Nystedt S, Emilsson K, Larsson AK, et al. (1995). "Molecular cloning and functional expression of the gene encoding the human proteinase-activated receptor 2". Eur. J. Biochem. 232 (1): 84–9. doi:10.1111/j.1432-1033.1995.tb20784.x. PMID 7556175.
- Santulli RJ, Derian CK, Darrow AL, et al. (1995). "Evidence for the presence of a protease-activated receptor distinct from the thrombin receptor in human keratinocytes". Proc. Natl. Acad. Sci. U.S.A. 92 (20): 9151–5. doi:10.1073/pnas.92.20.9151. PMC 40942. PMID 7568091.
- Nystedt S, Emilsson K, Wahlestedt C, Sundelin J (1994). "Molecular cloning of a potential proteinase activated receptor". Proc. Natl. Acad. Sci. U.S.A. 91 (20): 9208–12. doi:10.1073/pnas.91.20.9208. PMC 44781. PMID 7937743.
- Mirza H, Yatsula V, Bahou WF (1996). "The proteinase activated receptor-2 (PAR-2) mediates mitogenic responses in human vascular endothelial cells". J. Clin. Invest. 97 (7): 1705–14. doi:10.1172/JCI118597. PMC 507235. PMID 8601636.
- Bohm SK, Kong W, Bromme D, et al. (1996). "Molecular cloning, expression and potential functions of the human proteinase-activated receptor-2". Biochem. J. 314 (3): 1009–16. PMC 1217107. PMID 8615752.
- Böhm SK, Khitin LM, Grady EF, et al. (1996). "Mechanisms of desensitization and resensitization of proteinase-activated receptor-2". J. Biol. Chem. 271 (36): 22003–16. doi:10.1074/jbc.271.36.22003. PMID 8703006.
- Kahn M, Ishii K, Kuo WL, et al. (1996). "Conserved structure and adjacent location of the thrombin receptor and protease-activated receptor 2 genes define a protease-activated receptor gene cluster". Mol. Med. 2 (3): 349–57. PMC 2230143. PMID 8784787.
- Molino M, Barnathan ES, Numerof R, et al. (1997). "Interactions of mast cell tryptase with thrombin receptors and PAR-2". J. Biol. Chem. 272 (7): 4043–9. doi:10.1074/jbc.272.7.4043. PMID 9020112.
- Howells GL, Macey MG, Chinni C, et al. (1997). "Proteinase-activated receptor-2: expression by human neutrophils". J. Cell. Sci. 110 (7): 881–7. PMID 9133675.
- D'Andrea MR, Derian CK, Leturcq D, et al. (1998). "Characterization of protease-activated receptor-2 immunoreactivity in normal human tissues". J. Histochem. Cytochem. 46 (2): 157–64. PMID 9446822.
- Guyonnet Dupérat V, Jacquelin B, Boisseau P, et al. (1998). "Protease-activated receptor genes are clustered on 5q13". Blood 92 (1): 25–31. PMID 9639495.
- Steinhoff M, Corvera CU, Thoma MS, et al. (1999). "Proteinase-activated receptor-2 in human skin: tissue distribution and activation of keratinocytes by mast cell tryptase". Exp. Dermatol. 8 (4): 282–94. doi:10.1111/j.1600-0625.1999.tb00383.x. PMID 10439226.
- Takeuchi T, Harris JL, Huang W, et al. (2000). "Cellular localization of membrane-type serine protease 1 and identification of protease-activated receptor-2 and single-chain urokinase-type plasminogen activator as substrates". J. Biol. Chem. 275 (34): 26333–42. doi:10.1074/jbc.M002941200. PMID 10831593.
- Loew D, Perrault C, Morales M, et al. (2000). "Proteolysis of the exodomain of recombinant protease-activated receptors: prediction of receptor activation or inactivation by MALDI mass spectrometry". Biochemistry 39 (35): 10812–22. doi:10.1021/bi0003341. PMID 10978167.
- Knight DA, Lim S, Scaffidi AK, et al. (2001). "Protease-activated receptors in human airways: upregulation of PAR-2 in respiratory epithelium from patients with asthma". J. Allergy Clin. Immunol. 108 (5): 797–803. doi:10.1067/mai.2001.119025. PMID 11692107.
- Miike S, McWilliam AS, Kita H (2002). "Trypsin induces activation and inflammatory mediator release from human eosinophils through protease-activated receptor-2". J. Immunol. 167 (11): 6615–22. doi:10.4049/jimmunol.167.11.6615. PMID 11714832.
- Asokananthan N, Graham PT, Fink J, et al. (2002). "Activation of protease-activated receptor (PAR)-1, PAR-2, and PAR-4 stimulates IL-6, IL-8, and prostaglandin E2 release from human respiratory epithelial cells". J. Immunol. 168 (7): 3577–85. doi:10.4049/jimmunol.168.7.3577. PMID 11907122.
- Wong, D. M.; Tam, V.; Lam, R. et al. (2010). "Protease-activated receptor 2 has pivotal roles in cellular mechanisms involved in experimental periodontitis.". Infect. Immun. 78 (7): 629–38. doi:10.1128/IAI.01019-09. PMC 2812191. PMID 19933835.
External links
- "Protease-Activated Receptors: PAR2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
Cell surface receptor: G protein-coupled receptors
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Class B: Secretin like
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Orphan |
- GPR (56
- 64
- 97
- 98
- 110
- 111
- 112
- 113
- 114
- 115
- 116
- 123
- 124
- 125
- 126
- 128
- 133
- 143
- 144
- 155
- 157)
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Other |
- Brain-specific angiogenesis inhibitor (1
- 2
- 3)
- Cadherin (1
- 2
- 3)
- Calcitonin
- CALCRL
- CD97
- Corticotropin-releasing hormone (1
- 2)
- EMR (1
- 2
- 3)
- Glucagon (GR
- GIPR
- GLP1R
- GLP2R)
- Growth hormone releasing hormone
- PACAPR1
- GPR
- Latrophilin (1
- 2
- 3
- ELTD1)
- Methuselah-like proteins
- Parathyroid hormone (1
- 2)
- Secretin
- Vasoactive intestinal peptide (1
- 2)
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Class C: Metabotropic glutamate / pheromone
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Taste |
- TAS1R (1
- 2
- 3)
- TAS2R (1
- 3
- 4
- 5
- 7
- 8
- 9
- 10
- 13
- 14
- 16
- 19
- 20
- 30
- 31
- 38
- 39
- 40
- 41
- 42
- 43
- 45
- 46
- 50
- 60)
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Other |
- Calcium-sensing receptor
- GABA B (1
- 2)
- Glutamate receptor (Metabotropic glutamate (1
- 2
- 3
- 4
- 5
- 6
- 7
- 8))
- GPRC6A
- GPR (156
- 158
- 179)
- RAIG (1
- 2
- 3
- 4)
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Class F: Frizzled / Smoothened
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Frizzled |
- Frizzled (1
- 2
- 3
- 4
- 5
- 6
- 7
- 8
- 9
- 10)
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Smoothened |
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B trdu: iter (nrpl/grfl/cytl/horl), csrc (lgic, enzr, gprc, igsr, intg, nrpr/grfr/cytr), itra (adap, gbpr, mapk), calc, lipd; path (hedp, wntp, tgfp+mapp, notp, jakp, fsap, hipp, tlrp)
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This article incorporates text from the United States National Library of Medicine, which is in the public domain.
UpToDate Contents
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English Journal
- Glycyrrhetinic acid prevents cutaneous scratching behavior in mice elicited by substance P or PAR-2 agonist.
- Akasaka Y, Yoshida T, Tsukahara M, Hatta A, Inoue H.AbstractAlthough glycyrrhetinic acid (GA) has been used for the prevention of itch in chronic dermatitis, the mechanism underlying the antipruritic effects of GA is still unclear. Recently, several mediators other than histamine, such as substance P and tryptase, were found to participate in chronic itch. Here, we investigated the effect of GA on pruritus induced by various pruritic agents including histamine in mice. We also determined the level of leukotriene (LT)B(4) in mouse skin injected with substance P in an effort to uncover part of the antipruritic mechanism of GA. Scratching events were counted for 10min after intradermal injection of histamine, substance P (100nmol per site each), protease-activated receptor-2 (PAR-2) agonistic peptide (50nmol per site), or LTB(4) (0.03nmol per site) with or without GA (4nmol per site) into male ICR mice. Levels of LTB(4) in the skin after injection of substance P were determined by ELISA. GA did not suppress scratching behavior induced by histamine and LTB(4), but markedly and dose-dependently suppressed that induced by substance P and PAR-2 agonistic peptide. LTB(4) levels in skin elevated by substance P were lowered by GA. These data support the efficacy of GA in counteracting itch in chronic dermatitis because GA reduced scratching behavior induced by substance P and PAR-2 agonistic peptide. GA may exert antipruritic effects via inhibition of LTB(4) production in skin.
- European journal of pharmacology.Eur J Pharmacol.2011 Nov 16;670(1):175-9. Epub 2011 Sep 10.
- Although glycyrrhetinic acid (GA) has been used for the prevention of itch in chronic dermatitis, the mechanism underlying the antipruritic effects of GA is still unclear. Recently, several mediators other than histamine, such as substance P and tryptase, were found to participate in chronic itch. H
- PMID 21925497
- Redox regulation of human protease-activated receptor-2 by activated factor X.
- Jobi K, Rauch BH, Dangwal S, Freidel K, Doller A, Eberhardt W, Fischer JW, Schror K, Rosenkranz AC.SourceInstitut fur Pharmakologie und Klinische Pharmakologie, Heinrich-Heine-Universitat Dusseldorf, 40225 Dusseldorf, Germany.
- Free radical biology & medicine.Free Radic Biol Med.2011 Nov 1;51(9):1758-64. Epub 2011 Aug 12.
- Activated factor X (FXa) exerts coagulation-independent actions such as proliferation of vascular smooth muscle cells (SMCs) through the protease-activated receptors PAR-1 and PAR-2. Both receptors are upregulated upon vascular injury but the underlying mechanisms have not been defined. We examined
- PMID 21871560
Japanese Journal
- P2-10-20 子宮頸癌のリンパ節転移におけるprotease activated receptor (PAR)-2の発現の臨床的意義(Group85 子宮頸部腫瘍・基礎,一般演題,第63回日本産科婦人科学会学術講演会)
- 日本人幼児における日常の身体活動量と生活環境の関係
- 田中 千晶,田中 茂穂,安藤 貴史
- 発育発達研究 2011(51), 51_37-51_45, 2011
- … Presence of hills was significantly associated with less time in PAR (physical activity ratio)≥4. … On the other hand, relationships between the amount of time in 2>=PAR<3 and fatigue and between the amount of time in PAR<2 or 2>=PAR<3 and motion sickness were significant. …
- NAID 130000954020
Related Pictures
★リンクテーブル★
[★]
- 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
[★]
- 関
- PAR-2、PAR-2 receptor、proteinase-activated receptor 2、trypsin receptor
[★]
- 関
- PAR-2、PAR-2 receptor、protease-activated receptor 2
[★]
- 関
- PAR-2、protease-activated receptor 2、proteinase-activated receptor 2、trypsin receptor
[★]
- 英
- PAR-2 receptor
- 関
- プロテアーゼ活性化受容体2、PAR-2レセプター
[★]
- 英
- PAR-2 receptor
- 関
- プロテアーゼ活性化受容体2、PAR-2受容体
[★]
- 微生物学:粒子凝集法(particle agglutination test)
- 薬理学:
[★]
[★]
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- →para