Coagulation factor II receptor

Coagulation factor II receptor (also known as Protease-activated receptor 1 or PAR1) is a protein that in humans is encoded by the F2R gene. It is a member of the large family of G-protein coupled receptors (GPCRs).

Function

Coagulation factor II receptor is a cell surface receptor which is coupled to G protein and acts as a sensor for extracellular proteases. It is activated by thrombin, a serine protease in the coagulation cascade, which cleaves a part of the receptor's extracellular domain. This unmasking of the tethered ligand allows it to bind and activate the receptor, leading to platelet aggregation and other responses.

Clinical significance

Alterations in the coagulation factor II receptor have been implicated in a variety of diseases, including thrombosis, sepsis, and cancer. In particular, overexpression of PAR1 has been associated with breast cancer and melanoma.

Pharmacology

Several drugs that target the coagulation factor II receptor are currently in development. These include antagonists that block the receptor's activation by thrombin, as well as agonists that mimic the action of the tethered ligand.

See also

• Coagulation factor II
• Protease-activated receptor
• G protein-coupled receptor

References

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