Protease-activated receptor 2

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Coagulation factor II (thrombin) receptor-like 1
Identifiers
Symbols F2RL1 ; GPR11; PAR2
External IDs OMIM600933 MGI101910 HomoloGene21087 IUPHAR: PAR2 ChEMBL: 5963 GeneCards: F2RL1 Gene
RNA expression pattern
PBB GE F2RL1 206429 at tn.png
PBB GE F2RL1 213506 at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez 2150 14063
Ensembl ENSG00000164251 ENSMUSG00000021678
UniProt P55085 P55086
RefSeq (mRNA) NM_005242 NM_007974
RefSeq (protein) NP_005233 NP_032000
Location (UCSC) Chr 5:
76.11 – 76.13 Mb
Chr 13:
95.51 – 95.53 Mb
PubMed search [1] [2]

Protease activated receptor 2 (PAR2) also known as coagulation factor II (thrombin) receptor-like 1 (F2RL1) or G-protein coupled receptor 11 (GPR11) is a protein that in humans is encoded by the F2RL1 gene. PAR2 modulates inflammatory responses and acts as a sensor for proteolytic enzymes generated during infection.[1]

Gene[edit]

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.[2]

Mechanism of activation[edit]

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.[3] These receptors can also be activated non-protealytically, by exogenous peptide sequences that mimic the final amino acids of the tethered ligand.[4]

Agonists and antagonists[edit]

Potent and selective small molecule agonists and antagonists for PAR2 have been discovered.[5][6]

See also[edit]

References[edit]

  1. ^ Lee SE, Jeong SK, Lee SH (November 2010). "Protease and protease-activated receptor-2 signaling in the pathogenesis of atopic dermatitis". Yonsei Med. J. 51 (6): 808–22. doi:10.3349/ymj.2010.51.6.808. PMC 2995962. PMID 20879045. 
  2. ^ "Entrez Gene: F2RL1 coagulation factor II (thrombin) receptor-like 1". 
  3. ^ 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. doi:10.4049/jimmunol.167.2.1014. PMID 11441110. 
  4. ^ Kawabata A, Kanke T, Yonezawa D, Ishiki T, Saka M, Kabeya M, Sekiguchi F, Kubo S, Kuroda R, Iwaki M, Katsura K, Plevin R (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. 
  5. ^ Gardell LR, Ma JN, Seitzberg JG, Knapp AE, Schiffer HH, Tabatabaei A, Davis CN, Owens M, Clemons B, Wong KK, Lund B, Nash NR, Gao Y, Lameh J, Schmelzer K, Olsson R, Burstein ES (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. 
  6. ^ Barry GD, Suen JY, Le GT, Cotterell A, Reid RC, Fairlie DP (October 2010). "Novel agonists and antagonists for human protease activated receptor 2". J. Med. Chem. 53 (20): 7428–40. doi:10.1021/jm100984y. PMID 20873792. 


Further reading[edit]

External links[edit]

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