Coagulation factor II receptor

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Coagulation factor II (thrombin) receptor
Identifiers
SymbolsF2R; CF2R; HTR; PAR1; TR
External IDsOMIM: 187930 MGI: 101802 HomoloGene: 1510 IUPHAR: PAR1 GeneCards: F2R Gene
RNA expression pattern
250px
More reference expression data
Orthologs
SpeciesHumanMouse
Entrez214914062
EnsemblENSG00000181104ENSMUSG00000048376
UniProtP25116Q3UK34
RefSeq (mRNA)NM_001992NM_010169
RefSeq (protein)NP_001983NP_034299
Location (UCSC)Chr 5:
76.05 - 76.07 Mb		Chr 13:
96.7 - 96.72 Mb
PubMed search[1][2]

Proteinase-activated receptor 1 (PAR1) also known as the coagulation factor II (thrombin) receptor is a protein that in humans is encoded by the F2R gene.[1] PAR1 is a G protein-coupled receptor involved in the regulation of thrombotic response. Proteolytic cleavage leads to the activation of the receptor.[2]

Ligands

Several selective antagonists for the PAR1 receptor have been developed, for use as anti-clotting agents for the treatment of heart disease.

See also

References

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Further reading

  • 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 Freely accessible. 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 Freely accessible. 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. 

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

40x30px This transmembrane receptor-related article is a stub. You can help ssf by expanding it.
Class A: Rhodopsin like
α1 (A, B, D) · α2 (A, B, C) · β1 · β2 · β3
Adenosine (A1, A2A, A2B, A3) · P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(all but 5-HT3) 5-HT1 (A, B, D, E, F) · 5-HT2 (A, B, C) · 5-HT (4, 5A, 6, 7)
Other
Acetylcholine (M1, M2, M3, M4, M5) · Dopamine (D1, D2, D3, D4, D5) · Histamine (H1, H2, H3, H4) · Melatonin (1A, 1B, 1C) · TAAR (1, 2, 3, 5, 6, 8, 9)
Metabolites and
signaling molecules
CysLT (1, 2) · LTB4 (1, 2) · FPRL1 · OXE · Prostaglandin (DP (1, 2), EP (1, 2, 3, 4), FP) · Prostacyclin · Thromboxane
Other
Bile acid · Cannabinoid (CB1, CB2, GPR (18, 55, 119)) · EBI2 · Estrogen · Free fatty acid (1, 2, 3, 4) · Lactate  · Lysophosphatidic acid (1, 2, 3, 4, 5, 6)  · Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) · Niacin (1, 2) · Oxoglutarate · PAF · Sphingosine-1-phosphate (1, 2, 3, 4, 5) · Succinate
Peptide
B/W (1, 2) · FF (1, 2) · S · Y (1, 2, 4, 5) · Neuromedin (B, U (1, 2)) · Neurotensin (1, 2)
Other
Miscellaneous
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)
Other
Class B: Secretin like
GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157)
Other
Class C: Metabotropic
glutamate / pheromone
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)
Other
Class F:
Frizzled / Smoothened
Frizzled
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10)
Smoothened
  1. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  2. ↑ "Entrez Gene: F2R coagulation factor II (thrombin) receptor". 
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