Protease-activated receptor 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 is_associated_with::protein that in humans is encoded by the F2RL1 is_associated_with::gene. PAR2 modulates inflammatory responses and acts as a sensor for proteolytic enzymes generated during infection.

Gene
The F2RL1 gene contains two is_associated_with::exons and is widely expressed in human tissues. The predicted protein sequence is 83% identical to the mouse receptor sequence.

Mechanism of activation
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 is_associated_with::protease-activated receptor family. It is activated by is_associated_with::trypsin, but not by is_associated_with::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.

Agonists and antagonists
Potent and selective is_associated_with::small molecule is_associated_with::agonists and antagonists for PAR2 have been discovered.