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Coagulation factor II (thrombin) receptor-like 1
Symbols F2RL1; GPR11; PAR2
External IDs OMIM600933 MGI101910 HomoloGene21087 IUPHAR: PAR2 GeneCards: F2RL1 Gene
RNA expression pattern
PBB GE F2RL1 206429 at tn.png
PBB GE F2RL1 213506 at tn.png
More reference expression data
Species Human Mouse
Entrez 2150 14063
Ensembl ENSG00000164251 ENSMUSG00000021678
UniProt P55085 Q3TU81
RefSeq (mRNA) NM_005242 NM_007974
RefSeq (protein) NP_005233 NP_032000
Location (UCSC) Chr 5:
76.15 - 76.17 Mb
Chr 13:
96.61 - 96.63 Mb
PubMed search [1] [2]

Protease activated receptor 2 (PAR2) or Coagulation factor II (thrombin) receptor-like 1, is a protein encoded by the F2RL1 gene in humans.

PAR2 is a member of the large family of 7-transmembrane receptors that couple to guanosine-nucleotide-binding proteins. PAR2 is also a member of the protease-activated receptor family. It is activated by trypsin, but not by thrombin. It is activated by proteolytic cleavage of its extracellular amino terminus. The new amino terminus functions as a tethered ligand and activates the receptor. Additionally, these receptors can be activated by exogenous proteases, such as house dust mite protein Der P9.[1] These receptors can also be activated non-protealytically, by exogenous peptide sequences that mimic the final amino acids of the tethered ligand.[2] Recently, potent and selective small molecule agonists for these receptors have also been discovered but are not currently widely available.[3] The F2RL1 gene contains two exons and is widely expressed in human tissues. The predicted protein sequence is 83% identical to the mouse receptor sequence.[4]


See also


  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".  

External links

Further reading

  • 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. 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. 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. 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. 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. 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. 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. 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.  

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



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