Receptor koagulacionog faktora II‎‎

Identifikatori

F2R; CF2R; HTR; PAR1; TR

Vanjski ID

OMIM: 187930 MGI: 101802 HomoloGene: 1510 IUPHAR: PAR1 GeneCards: F2R 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	• regulacija progresa ćelijskog ciklusa • apoptoza • aktivacija kaspaze • ćelijska motilnost • prenos signala • signalni put G-protein spregnutog receptora • tirozinska fosforilacija STAT proteina • STAT proteinska jezgrena translokacija • razvoj multićelijskih organizama • koagulacija krvi • respons na ranjavanje • anatomska strukturna morfogeneza • pozitivna regulacija I-kapaB kinaze/NF-kapaB kaskade

Pregled RNK izražavanja

podaci

Ortolozi

Vrsta

Čovek

Miš

RefSeq (mRNA)

RefSeq (protein)

Lokacija (UCSC)

Chr 5:
76.05 - 76.07 Mb

Chr 13:
96.7 - 96.72 Mb

PubMed pretraga

[1]

[2]

Receptor koagulacionog faktora II, ili proteazom-aktivirani receptor‎‎ 1 (PAR1), je protein koji kod ljudi kodira F2R gen.^[1] PAR1 je G protein-spregnuti receptor koji učestvuje u regulaciji trombotskog responsa. Proteolitičko odsecanje dovodi do aktivacije receptora.^[2]

Ligandi

Nekoliko selektivnih antagonista PAR1 receptora je poznato. Oni se koriste kao antizgrušavajuća sredstva u lečenju bolesti srca.

SCH-530348

Vidi još

Proteazom-aktivirani receptor‎‎

Literatura

↑ Bahou WF, Nierman WC, Durkin AS, Potter CL, Demetrick DJ (September 1993). „Chromosomal assignment of the human thrombin receptor gene: localization to region q13 of chromosome 5”. Blood 82 (5): 1532–7. PMID 8395910.
↑ „Entrez Gene: F2R coagulation factor II (thrombin) receptor”.

Dodatna literatura

Coughlin SR, Vu TK, Hung DT, Wheaton VI (1992). „Characterization of a functional thrombin receptor. Issues and opportunities.”. J. Clin. Invest. 89 (2): 351–5. DOI:10.1172/JCI115592. PMC 442859. PMID 1310691.
Howell DC, Laurent GJ, Chambers RC (2002). „Role of thrombin and its major cellular receptor, protease-activated receptor-1, in pulmonary fibrosis.”. Biochem. Soc. Trans. 30 (2): 211–6. DOI:10.1042/BST0300211. PMID 12023853.
Tellez C, Bar-Eli M (2003). „Role and regulation of the thrombin receptor (PAR-1) in human melanoma.”. Oncogene 22 (20): 3130–7. DOI:10.1038/sj.onc.1206453. PMID 12789289.
Remillard CV, Yuan JX (2005). „PGE2 and PAR-1 in pulmonary fibrosis: a case of biting the hand that feeds you?”. Am. J. Physiol. Lung Cell Mol. Physiol. 288 (5): L789–92. DOI:10.1152/ajplung.00016.2005. PMID 15821019.
Leger AJ, Covic L, Kuliopulos A (2006). „Protease-activated receptors in cardiovascular diseases.”. Circulation 114 (10): 1070–7. DOI:10.1161/CIRCULATIONAHA.105.574830. PMID 16952995.
Traynelis SF, Trejo J (2007). „Protease-activated receptor signaling: new roles and regulatory mechanisms.”. Curr. Opin. Hematol. 14 (3): 230–5. DOI:10.1097/MOH.0b013e3280dce568. PMID 17414212.
Vu TK, Hung DT, Wheaton VI, Coughlin SR (1991). „Molecular cloning of a functional thrombin receptor reveals a novel proteolytic mechanism of receptor activation.”. Cell 64 (6): 1057–68. DOI:10.1016/0092-8674(91)90261-V. PMID 1672265.
Wojtukiewicz MZ, Tang DG, Ben-Josef E, et al. (1995). „Solid tumor cells express functional "tethered ligand" thrombin receptor.”. Cancer Res. 55 (3): 698–704. PMID 7834643.
Hein L, Ishii K, Coughlin SR, Kobilka BK (1994). „Intracellular targeting and trafficking of thrombin receptors. A novel mechanism for resensitization of a G protein-coupled receptor.”. J. Biol. Chem. 269 (44): 27719–26. PMID 7961693.
Mathews II, Padmanabhan KP, Ganesh V, et al. (1994). „Crystallographic structures of thrombin complexed with thrombin receptor peptides: existence of expected and novel binding modes.”. Biochemistry 33 (11): 3266–79. DOI:10.1021/bi00177a018. PMID 8136362.
Offermanns S, Laugwitz KL, Spicher K, Schultz G (1994). „G proteins of the G12 family are activated via thromboxane A2 and thrombin receptors in human platelets.”. Proc. Natl. Acad. Sci. U.S.A. 91 (2): 504–8. DOI:10.1073/pnas.91.2.504. PMC 42977. PMID 8290554.
Hoffman M, Church FC (1993). „Response of blood leukocytes to thrombin receptor peptides.”. J. Leukoc. Biol. 54 (2): 145–51. PMID 8395550.
Schmidt VA, Vitale E, Bahou WF (1996). „Genomic cloning and characterization of the human thrombin receptor gene. Structural similarity to the proteinase activated receptor-2 gene.”. J. Biol. Chem. 271 (16): 9307–12. DOI:10.1074/jbc.271.16.9809. PMID 8621593.
Li F, Baykal D, Horaist C, et al. (1996). „Cloning and identification of regulatory sequences of the human thrombin receptor gene.”. J. Biol. Chem. 271 (42): 26320–8. DOI:10.1074/jbc.271.42.26320. PMID 8824285.
Shapiro MJ, Trejo J, Zeng D, Coughlin SR (1997). „Role of the thrombin receptor's cytoplasmic tail in intracellular trafficking. Distinct determinants for agonist-triggered versus tonic internalization and intracellular localization.”. J. Biol. Chem. 271 (51): 32874–80. DOI:10.1074/jbc.271.51.32874. PMID 8955127.
Ogino Y, Tanaka K, Shimizu N (1997). „Direct evidence for two distinct G proteins coupling with thrombin receptors in human neuroblastoma SH-EP cells.”. Eur. J. Pharmacol. 316 (1): 105–9. DOI:10.1016/S0014-2999(96)00653-X. PMID 8982657.
Molino M, Bainton DF, Hoxie JA, et al. (1997). „Thrombin receptors on human platelets. Initial localization and subsequent redistribution during platelet activation.”. J. Biol. Chem. 272 (9): 6011–7. DOI:10.1074/jbc.272.9.6011. PMID 9038223.
Renesto P, Si-Tahar M, Moniatte M, et al. (1997). „Specific inhibition of thrombin-induced cell activation by the neutrophil proteinases elastase, cathepsin G, and proteinase 3: evidence for distinct cleavage sites within the aminoterminal domain of the thrombin receptor.”. Blood 89 (6): 1944–53. PMID 9058715.

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 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

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)

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