F2RL1

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Proteazom-aktivirani receptor 2
Identifikatori
SimboliF2RL1; GPR11; PAR2
Vanjski IDOMIM: 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
VrstaČovekMiš
Entrez215014063
EnsemblENSG00000164251ENSMUSG00000021678
UniProtP55085Q3TU81
RefSeq (mRNA)NM_005242NM_007974
RefSeq (protein)NP_005233NP_032000
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) 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]

Vidi još

Literatura

  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. 
  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. 
  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”. 

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. 
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Klasa A: Rodopsinu slični
α1 (A, B, D) • α2 (A, B, C) • β1 • β2 • β3
Adenozinski (A1, A2A, A2B, A3) • P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(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
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
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 ne σ) • 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
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
GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157)
Drugi
Klasa C: Metabotropni
glutamat / feromon
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
Klasa F:
Frizzled / Zaglađeni
Uvojiti
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10)
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)