F2R

The protein encoded by F2R is Protease-Activated Receptor 1 (PAR1), also known as thrombin receptor or CD141. As a G protein-coupled receptor (GPCR), it is activated by thrombin cleavage of its N-terminal domain, exposing a tethered ligand that binds to the receptor’s extracellular loop, triggering downstream signaling via Gq, Gi, and G12/13 pathways to mediate platelet aggregation, vascular smooth muscle contraction, and inflammation.
PAR1 participates in PI3K/Akt and MAPK signaling pathways. Dysregulation is linked to thrombotic disorders (myocardial infarction, stroke), inflammatory diseases, and cancer metastasis. Vorapaxar, a PAR1 antagonist, is approved for reducing cardiovascular events. Ongoing research explores novel small-molecule inhibitors targeting PAR1 for thrombosis and cancer therapy.