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Proteazom-aktivirani receptor 2
Identifikatori
Simboli	F2RL1; GPR11; PAR2
Vanjski ID	OMIM: 600933 MGI: 101910 HomoloGene: 21087 IUPHAR: PAR2 GeneCards: 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

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Proteazom-aktivirani receptor 2 (PAR2) ili Receptoru koagulacionog faktora II (trombina) sličan 1, je protein kodiran F2RL1 genom kod ljudi.

PAR2 je član velike familije G-protein spregnutih receptora koji interaguju sa guanozin-nukleotid-vezujućim proteinima. PAR2 je takođe član familije proteazom aktiviranih receptora. On je aktiviran tripsinom, umesto trombina. Do aktivacije dolazi proteolitičkim odsecanjem njegovog ekstracelularnog amino terminusa. Novo-formirani amino terminus dejstvuje kao vezani ligand i aktivira receptor. Ovi receptori isto tako mogu biti aktivirani egzogenim proteazama, kao što je protein Der P9 kućnog krpelja.^[1] Ovi receptori mogu takođe biti aktiviran ne-proteolitički, egzogenim peptidima koji oponašaju finalnu aminokiselinsku 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

Proteazom-aktivirani receptor

Literatura

↑ 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

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 iz originala na datum 2016-03-03.

[pmid11441110-1] 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.

[pmid14976227-2] 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.

[pmid18768780-3] 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.

[4] „Entrez Gene: F2RL1 coagulation factor II (thrombin) receptor-like 1”.

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