F2RL1

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Coagulation factor II (thrombin) receptor-like 1
Identifiers
Symbols	F2RL1; GPR11; PAR2
External IDs	OMIM: 600933 MGI: 101910 HomoloGene: 21087 IUPHAR: PAR2 GeneCards: F2RL1 Gene
Gene Ontology Molecular function • rhodopsin-like receptor activity • receptor activity • receptor binding • thrombin receptor activity Cellular component • Golgi apparatus • plasma membrane • integral to plasma membrane Biological process • signal transduction • G-protein coupled receptor protein signaling pathway • elevation of cytosolic calcium ion concentration • blood coagulation Sources: Amigo / EGO
RNA expression pattern
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More reference expression data
Orthologs
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. These receptors can also be activated non-protealytically, by exogenous peptide sequences that mimic the final amino acids of the tethered ligand. Recently, potent and selective small molecule agonists for these receptors have also been discovered but are not currently widely available. 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.

See also

• Protease-activated receptor

External links

• "Protease-Activated Receptors: PAR2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. 

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. CS1 maint: Multiple names: authors list (link)
• 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 Freely accessible. 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. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• 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 Freely accessible. PMID 7568091. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• 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 Freely accessible. PMID 7937743. CS1 maint: Multiple names: authors list (link)
• 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 Freely accessible. PMID 8601636. CS1 maint: Multiple names: authors list (link)
• 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 Freely accessible. PMID 8615752. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• 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. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• 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 Freely accessible. PMID 8784787. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• 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. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• 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. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• 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. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• 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. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• 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. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• 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. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• 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. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• 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. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• 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. CS1 maint: Multiple names: authors list (link)
• 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. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)

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