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F2RL1

Uredi veze

Izvor: Wikipedija

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Proteazom-aktivirani receptor 2

Identifikatori

Simboli

F2RL1; GPR11; PAR2

Vanjski ID

OMIM: 600933MGI: 101910HomoloGene: 21087IUPHAR:PAR2GeneCards:F2RL1 Gene

Ontologija gena
Molekularna funkcija	•rodopsinu-slična receptorska aktivnost•receptorska aktivnost•receptorsko vezivanje•aktivnost trombinskog receptora
Celularna komponenta	•Goldžijev aparat•membrana plazme•integralno sa membranom plazme
Biološki proces	•prenos signala•signalni put G-protein spregnutog receptora•povišenje koncentracije citosolnih jona•koagulacija krvi

Pregled RNK izražavanja

podaci

Ortolozi

Vrsta

Čovek

Miš

RefSeq (mRNA)

RefSeq (protein)

Lokacija (UCSC)

Chr 5:
76.15 - 76.17 Mb

Chr 13:
96.61 - 96.63 Mb

PubMed pretraga

[1]

[2]

Proteazom-aktivirani receptor 2 (PAR2) iliReceptoru koagulacionog faktora II (trombina) sličan 1, jeprotein kodiranF2RL1genom kod ljudi.

PAR2 je član velike familijeG-protein spregnutih receptora koji interaguju sa guanozin-nukleotid-vezujućim proteinima. PAR2 je takođe član familijeproteazom aktiviranih receptora. On je aktivirantripsinom, umestotrombina. Do aktivacije dolazi proteolitičkim odsecanjem njegovog ekstracelularnog amino terminusa. Novo-formiraniamino terminus dejstvuje kao vezani ligand i aktivira receptor. Ovi receptori isto tako mogu biti aktivirani egzogenim proteazama, kao što je protein Der P9 kućnogkrpelja.^[1] Ovi receptori mogu takođe biti aktiviran ne-proteolitički, egzogenim peptidima koji oponašaju finalnuaminokiselinsku sekvencu vezanog liganda.^[2] Nedavno su otkriveni potentni i selektivni mali-molekul agonisti ovih receptora.^[3]

F2RL1 gen se sastoji od dva eksona. On je široko je izražen u ljudskim tkivima. F2RL1 proteinska sekvenca je 83% identična sa sekvencom mišjeg receptora.^[4]

Povezano

[uredi |uredi kod]

Proteazom-aktivirani receptor

Literatura

[uredi |uredi kod]

↑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,et al. (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,et al. (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.
↑„Entrez Gene: F2RL1 coagulation factor II (thrombin) receptor-like 1”.

Dodatna literatura

[uredi |uredi kod]

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 ( Pt 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 ( Pt 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. 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. PMID 11907122.
„Protease-Activated Receptors: PAR2”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Arhivirano izoriginala na datum 2016-03-03.

Transmembranski receptor:G protein spregnuti receptori

Klasa A:Rodopsinu slični

Neurotransmiter

Adrenergički	α1 (A,B,D) • α2 (A,B,C) • β1 • β2 • β3
Purinski	Adenozinski (A1,A2A,A2B,A3) • P2Y (1,2,4,5,6,8,9,10,11,12,13,14)
Serotoninski	(svi osim 5-HT3)5-HT1 (A,B,D,E,F) • 5-HT2 (A,B,C) • 5-HT (4,5A,6,7)
Drugi	Acetilholin (M1,M2,M3,M4,M5) • Dopamin (D1,D2,D3,D4,D5) • Histamin (H1,H2,H3,H4) • Melatonin (1A,1B,1C) • TAAR (1,2,3,5,6,8,9)

Metaboliti i
signalni molekuli

Eikozanoidni	CysLT (1,2) • LTB4 (1,2) • FPRL1 • OXE • Prostaglandin (DP (1,2),EP (1,2,3,4),FP) • Prostaciklin • Tromboksan
Drugi	Žučna kiselina • Kanabinoidni (CB1,CB2,GPR (18,55,119)) • EBI2 • Estrogen • Slobodna masna kiselina (1,2,3,4) • Laktat • Lizofosfatidna kiselina (1,2,3,4,5,6) • Lizofosfolipid (1,2,3,4,5,6,7,8) • Niacin (1,2) • Oksoglutarat • PAF • Sfingozin-1-fosfat (1,2,3,4,5) • Sukcinat

Peptid

Neuropeptidni

B/W (1,2) • FF (1,2) • S • Y (1,2,4,5) • Neuromedin (B,U (1,2)) • Neurotenzin (1,2)

Drugi

Anafilatoksin (C3a,C5a) • Angiotenzin (1,2) • Apelin • Bombezin (BRS3,GRPR,NMBR) • Bradikinin (B1,B2) • Hemokin • Holecistokinin (A,B) • Endotelin (A,B) • Formil peptid (1,2,3) • FSH • Galanin (1,2,3) • GHB receptor • Gonadotropin-oslobađajući hormon (1,2) • Grelin • Kispeptin • Luteinizirajući hormon/horiogonadotropin • MAS (1,1L,D,E,F,G,X1,X2,X3,X4) • Melanokortin (1,2,3,4,5) • MCHR (1,2) • Motilin • Opioidni (δ,κ,μ,Nociceptin &ζ, ali neσ) • Oreksin (1,2) • Oksitocin • Prokineticin (1,2) • Prolaktin-oslobađajući peptid • Relaksin (1,2,3,4) • Somatostatin (1,2,3,4,5) • Tahikinin (1,2,3) • Tirotropin • Tirotropin-oslobađajući hormon • Urotenzin-II • Vazopresin (1A,1B,2)

Razno

Orfan	GPR (1,3,4,6,12,15,17,18,19,20,21,22,23,25,26,27,31,32,33,34,35,37,39,42,44,45,50,52,55,61,62,63,65,68,75,77,78,81,82,83,84,85,87,88,92,101,103,109A,109B,119,120,132,135,137B,139,141,142,146,148,149,150,151,152,153,160,161,162,171,173,174,176,177,182,183)
Drugi	Adrenomedulin • Mirisni • Opsin (3,4,5,1LW,1MW,1SW,RGR,RRH) • Proteazom-aktivirani (1,2,3,4) • SREB (1,2,3)

Klasa B:Sekretinu slični

Orfan

GPR (56,64,97,98,110,111,112,113,114,115,116,123,124,125,126,128,133,143,144,155,157)

Drugi

Moždano specifični angiogenezni inhibitor (1,2,3) • Cadherin (1,2,3) • Kalcitonin • CALCRL • CD97 • Kortikotropin-oslobađajući hormon (1,2) • EMR (1,2,3) • Glukagon (GR,GIPR,GLP1R,GLP2R) • Hormon rasta oslobađajući hormon • PACAPR1 • GPR • Latrofilin (1,2,3,ELTD1) • Metuselah-slični proteini • Paratiroidni hormon (1,2) • Sekretin • Vazoaktivni intestinalni peptid (1,2)

Klasa C:Metabotropni
glutamat /feromon

Ukus	TAS1R (1,2,3) • TAS2R (1,3,4,5,8,9,10,12,13,14,16,19,20,30,31,38,39,40,41,42,43,45,46,50)
Drugi	Kalcijum-detektujući receptor • GABA B (1,2) • Glutamatni receptor (Metabotropni glutamat (1,2,3,4,5,6,7,8)) • GPRC6A • GPR (156,158,179) • RAIG (1,2,3,4)

Klasa F:
Frizzled /Zaglađeni

Uvojiti	Frizzled (1,2,3,4,5,6,7,8,9,10)
Zaglađeni	Zaglađeni

B trdu:peptidi (nrpl/grfl/cytl/horl),receptori (lgic,enzr,gprc,igsr,intg,nrpr/grfr/cytr),itra (adap,gbpr,mapk),calc,lipd, signalni putevi (hedp,wntp,tgfp+mapp,notp,jakp,fsap,hipp,tlrp)

Izvor:https://sh.wikipedia.org/w/index.php?title=F2RL1&oldid=42508294

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