Protease activated receptor 2

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 • receptor activity • G-protein coupled receptor activity • receptor binding • thrombin receptor activity Cellular component • Golgi apparatus • plasma membrane • plasma membrane • integral to plasma membrane Biological process • positive regulation of leukocyte chemotaxis • G-protein coupled receptor protein signaling pathway • elevation of cytosolic calcium ion concentration • regulation of blood coagulation • positive regulation of positive chemotaxis Sources: Amigo / QuickGO
RNA expression pattern
More reference expression data
Orthologs
Species	Human	Mouse
Entrez	2150	14063
Ensembl	ENSG00000164251	ENSMUSG00000021678
UniProt	P55085	Q3TU81
RefSeq (mRNA)	NM_005242	NM_007974.4
RefSeq (protein)	NP_005233	NP_032000.3
Location (UCSC)	Chr 5: 76.11 – 76.13 Mb	Chr 13: 96.28 – 96.3 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

• Protease-activated receptor

References

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. http://www.jimmunol.org/cgi/content/abstract/167/2/1014. 
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". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=2150. 

External links

• "Protease-Activated Receptors: PAR2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=3020. 

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. PMC 2075212. PMID 17347265. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2075212. 
• 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. PMC 40942. PMID 7568091. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=40942. 
• 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. PMID 7937743. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=44781. 
• 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. PMID 8601636. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=507235. 
• 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. PMID 8615752. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1217107. 
• 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. PMC 2230143. PMID 8784787. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2230143. 
• 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. doi:10.1111/j.1600-0625.1999.tb00383.x. 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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