Introduction of F2R
F2R also referred as proteinase-activated receptor 1 (PAR1), which is encoded by the F2R gene, is a 7-transmembrane receptor in human belonging to the G-protein coupled receptor families involved in the regulation of thrombotic response. F2R is ubiquitously expressed covering from spleen, gallbladder to the 21 other tissues. Proteolytic cleavage makes a contribution to the activation of the receptor. With multifaceted effects, F2R is associated with the pathogenesis of inflammatory and fibrotic lung diseases and is crucial in mediating the interplay between coagulation and inflammation.
|Basic Information of F2R|
|Protein Name||Proteinase-activated receptor 1|
|Aliases||TR, HTR, CF2R, PAR1, PAR-1|
|Organism||Homo sapiens (Human)|
Function of F2R Membrane Protein
PAR1 belongs to a family of G-protein-coupled receptors that mediate cellular responses to thrombin and related proteases. Through cleaving the amino-terminal exodomain of the receptor, thrombin irreversibly activates PAR1 and exposes a tethered peptide ligand that binds the heptahelical bundle of the receptor to affect G-protein activation. Protease-activated receptors are important targets for drug development. The structure reported here will aid the development of improved PAR1 antagonists and the discovery of antagonists to other members of this receptor family. High-affinity receptor for activated thrombin coupled to G proteins that stimulate phosphoinositide hydrolysis. F2R may play a role in platelets activation and in vascular development.
Fig.1 Structure of F2R membrane protein.
Application of F2R Membrane Protein in Literature
This article reports that the 2.2 Å resolution crystal structure of human PAR1 bound to vorapaxar, a PAR1 antagonist.
This article reveals that PAR-1 inhibition did not affect thrombomodulin, soluble P-selectin and platelet factor-4 concentrations.
This article reveals that a low level of thrombin results in vasoconstriction of smooth muscles via PAR-1, PKC, and ROCK.
This article demonstrates that only MMP-12 can increase the expression of PGF by increasing early growth response protein 1 (Egr-1) level through the activation of PAR-1.
This article shows that the activation of PAR-1 was significantly reduced on the cell surface of SGC7901 and AGS cells after the knockdown of EPCR.
F2R Preparation Options
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