Protease activated receptor 2

Protease activated receptor 2
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_007974.4
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


  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

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