Coagulation factor II receptor

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Coagulation factor II (thrombin) receptor
PDB 1nrn EBI.jpg
Rendering of F2R from PDB 1NRN
Available structures
PDB Ortholog search: PDBe, RCSB
Symbols F2R ; CF2R; HTR; PAR-1; PAR1; TR
External IDs OMIM187930 MGI101802 HomoloGene1510 IUPHAR: 347 ChEMBL: 3974 GeneCards: F2R Gene
RNA expression pattern
PBB GE F2R 203989 x at tn.png
More reference expression data
Species Human Mouse
Entrez 2149 14062
Ensembl ENSG00000181104 ENSMUSG00000048376
UniProt P25116 P30558
RefSeq (mRNA) NM_001311313 NM_010169
RefSeq (protein) NP_001298242 NP_034299
Location (UCSC) Chr 5:
76.72 – 76.74 Mb
Chr 13:
95.6 – 95.62 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] PAR-1 has multifaceted effects and plays a key role in mediating the interplay between coagulation and inflammation, which is important in the pathogenesis of inflammatory and fibrotic lung diseases.[3]


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

SCH530348 has been recently shown to attenuate the neutrophilic inflammatory response to S. pneumoniae by reducing levels of pro-inflamamtory cytokines sucha s IL-1β and chemokines CXCL1, CCL2 and CCL7.[4]

See also[edit]


  1. ^ Bahou WF, Nierman WC, Durkin AS, Potter CL, Demetrick DJ (Sep 1993). "Chromosomal assignment of the human thrombin receptor gene: localization to region q13 of chromosome 5". Blood 82 (5): 1532–7. PMID 8395910. 
  2. ^ "Entrez Gene: F2R coagulation factor II (thrombin) receptor". 
  3. ^ "José RJ, Williams AE, Chambers RC (Feb 2014). "Proteinase-activated receptors in fibroproliferative lung disease". Thorax 69 (2): 190–2. doi:10.1136/thoraxjnl-2013-204367. PMID 24186921. 
  4. ^ José RJ, Williams AE, Mercer PF, Sulikowski MG, Brown JS, Chambers RC (Jun 2015). "Regulation of neutrophilic inflammation by proteinase-activated receptor 1 during bacterial pulmonary infection". Journal of Immunology 194 (12): 6024–34. doi:10.4049/jimmunol.1500124. PMID 25948816. 

Further reading[edit]

  • Coughlin SR, Vu TK, Hung DT, Wheaton VI (Feb 1992). "Characterization of a functional thrombin receptor. Issues and opportunities". The Journal of Clinical Investigation 89 (2): 351–5. doi:10.1172/JCI115592. PMC 442859. PMID 1310691. 
  • Wu H, Zhang Z, Li Y, Zhao R, Li H, Song Y, Qi J, Wang J (Oct 2010). "Time course of upregulation of inflammatory mediators in the hemorrhagic brain in rats: correlation with brain edema". Neurochemistry International 57 (3): 248–53. doi:10.1016/j.neuint.2010.06.002. PMID 20541575. 
  • Howell DC, Laurent GJ, Chambers RC (Apr 2002). "Role of thrombin and its major cellular receptor, protease-activated receptor-1, in pulmonary fibrosis". Biochemical Society Transactions 30 (2): 211–6. doi:10.1042/BST0300211. PMID 12023853. 
  • Tellez C, Bar-Eli M (May 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 (May 2005). "PGE2 and PAR-1 in pulmonary fibrosis: a case of biting the hand that feeds you?". American Journal of Physiology. Lung Cellular and Molecular Physiology 288 (5): L789–92. doi:10.1152/ajplung.00016.2005. PMID 15821019. 
  • Leger AJ, Covic L, Kuliopulos A (Sep 2006). "Protease-activated receptors in cardiovascular diseases". Circulation 114 (10): 1070–7. doi:10.1161/CIRCULATIONAHA.105.574830. PMID 16952995. 
  • Traynelis SF, Trejo J (May 2007). "Protease-activated receptor signaling: new roles and regulatory mechanisms". Current Opinion in Hematology 14 (3): 230–5. doi:10.1097/MOH.0b013e3280dce568. PMID 17414212. 
  • Vu TK, Hung DT, Wheaton VI, Coughlin SR (Mar 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, Renaud C, Walz DA, Honn KV (Feb 1995). "Solid tumor cells express functional "tethered ligand" thrombin receptor". Cancer Research 55 (3): 698–704. PMID 7834643. 
  • Hein L, Ishii K, Coughlin SR, Kobilka BK (Nov 1994). "Intracellular targeting and trafficking of thrombin receptors. A novel mechanism for resensitization of a G protein-coupled receptor". The Journal of Biological Chemistry 269 (44): 27719–26. PMID 7961693. 
  • Mathews II, Padmanabhan KP, Ganesh V, Tulinsky A, Ishii M, Chen J, Turck CW, Coughlin SR, Fenton JW (Mar 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 (Jan 1994). "G proteins of the G12 family are activated via thromboxane A2 and thrombin receptors in human platelets". Proceedings of the National Academy of Sciences of the United States of America 91 (2): 504–8. doi:10.1073/pnas.91.2.504. PMC 42977. PMID 8290554. 
  • Hoffman M, Church FC (Aug 1993). "Response of blood leukocytes to thrombin receptor peptides". Journal of Leukocyte Biology 54 (2): 145–51. PMID 8395550. 
  • Schmidt VA, Vitale E, Bahou WF (Apr 1996). "Genomic cloning and characterization of the human thrombin receptor gene. Structural similarity to the proteinase activated receptor-2 gene". The Journal of Biological Chemistry 271 (16): 9307–12. doi:10.1074/jbc.271.16.9809. PMID 8621593. 
  • Li F, Baykal D, Horaist C, Yan CN, Carr BN, Rao GN, Runge MS (Oct 1996). "Cloning and identification of regulatory sequences of the human thrombin receptor gene". The Journal of Biological Chemistry 271 (42): 26320–8. doi:10.1074/jbc.271.42.26320. PMID 8824285. 
  • Shapiro MJ, Trejo J, Zeng D, Coughlin SR (Dec 1996). "Role of the thrombin receptor's cytoplasmic tail in intracellular trafficking. Distinct determinants for agonist-triggered versus tonic internalization and intracellular localization". The Journal of Biological Chemistry 271 (51): 32874–80. doi:10.1074/jbc.271.51.32874. PMID 8955127. 
  • Ogino Y, Tanaka K, Shimizu N (Nov 1996). "Direct evidence for two distinct G proteins coupling with thrombin receptors in human neuroblastoma SH-EP cells". European Journal of Pharmacology 316 (1): 105–9. doi:10.1016/S0014-2999(96)00653-X. PMID 8982657. 
  • Molino M, Bainton DF, Hoxie JA, Coughlin SR, Brass LF (Feb 1997). "Thrombin receptors on human platelets. Initial localization and subsequent redistribution during platelet activation". The Journal of Biological Chemistry 272 (9): 6011–7. doi:10.1074/jbc.272.9.6011. PMID 9038223. 
  • Renesto P, Si-Tahar M, Moniatte M, Balloy V, Van Dorsselaer A, Pidard D, Chignard M (Mar 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.