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F2R Membrane Protein Introduction

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
Gene Name F2R
Aliases TR, HTR, CF2R, PAR1, PAR-1
Organism Homo sapiens (Human)
UniProt ID P25116
Transmembrane Times 7
Length (aa) 442
Sequence MGPRRLLLVAACFSLCGPLLSARTRARRPESKATNATLDPRSFLLRNPNDKYEPFWEDEE
KNESGLTEYRLVSINKSSPLQKQLPAFISEDASGYLTSSWLTLFVPSVYTGVFVVSLPLN
IMAIVVFILKMKVKKPAVVYMLHLATADVLFVSVLPFKISYYFSGSDWQFGSELCRFVTA
AFYCNMYASILLMTVISIDRFLAVVYPMQSLSWRTLGRASFTCLAIWALAIAGVVPLLLK
EQTIQVPGLNITTCHDVLNETLLEGYYAYYFSAFSAVFFFVPLIISTVCYVSIIRCLSSS
AVANRSKKSRALFLSAAVFCIFIICFGPTNVLLIAHYSFLSHTSTTEAAYFAYLLCVCVS
SISCCIDPLIYYYASSECQRYVYSILCCKESSDPSSYNSSGQLMASKMDTCSSNLNNSIY
KKLLT

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.

Structure of F2R membrane protein. Fig.1 Structure of F2R membrane protein.

Application of F2R Membrane Protein in Literature

  1. Zhang C., et al. High-resolution crystal structure of human protease-activated receptor 1. Nature, 2012, 492: 387-392. PubMed ID: 23222541.

    This article reports that the 2.2 Å resolution crystal structure of human PAR1 bound to vorapaxar, a PAR1 antagonist.

  2. Schoergenhofer C., et al. Inhibition of Protease-Activated Receptor (PAR1) Reduces Activation of the Endothelium, Coagulation, Fibrinolysis and Inflammation during Human Endotoxemia. Thromb Haemost. 2018, 118(7): 1176-1184. PubMed ID: 29864779

    This article reveals that PAR-1 inhibition did not affect thrombomodulin, soluble P-selectin and platelet factor-4 concentrations.

  3. Takahashi K., et al. Thrombin-Induced Responses via Protease-Activated Receptor 1 Blocked by the Endothelium on Isolated Porcine Retinal Arterioles. Curr Eye Res. 2018, 43(11): 1374-1382. PubMed ID: 29966442

    This article reveals that a low level of thrombin results in vasoconstriction of smooth muscles via PAR-1, PKC, and ROCK.

  4. Hou H. H., et al. MMP-12 activates protease activated receptor (PAR)-1, upregulates placenta growth factor and leads to pulmonary emphysema. Am J Physiol Lung Cell Mol Physiol. 2018, 315(3): L432-L442. PubMed ID: 29722565

    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.

  5. Wang Q., et al. Knockdown of EPCR inhibits the proliferation and migration of human gastric cancer cells via the ERK1/2 pathway in a PAR-1-dependent manner. Oncol Rep. 2018, 39(4): 1843-1852. PubMed ID: 29484413

    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

To obtain the soluble and functional target protein, the versatile Magic™ membrane protein production platform in Creative Biolabs enables many flexible options, from which you can always find a better match for your particular project. Aided by our versatile Magic™ anti-membrane protein antibody discovery platform, we also provide customized anti-F2R antibody development services.


Based on world-leading technology platforms and professional scientific staff, Creative Biolabs has successfully generated a variety of functional membrane protein targets for our customers. We are pleased to tailor one-stop, custom-oriented service packages and provide lyophilization or freezing service for long-term storage of membrane proteins from weeks to months. Please feel free to contact us for more information.

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