Property Summary

NCBI Gene PubMed Count 339
Grant Count 292
R01 Count 193
Funding $24,576,887
PubMed Score 534.62
PubTator Score 701.28

Knowledge Summary

Patent (77,288)

Expression

Synonym

Accession P25116 Q53XV0 Q96RF7 Q9BUN4 PAR-1
Symbols TR
HTR
CF2R
PAR1
PAR-1

Gene

F2R

PANTHER Protein Class (2)

PDB

1NRN   1NRO   1NRP   1NRQ   1NRR   3BEF   3HKI   3HKJ   3LU9   3VW7  

  TechDev Info (1)

 GWAS Trait (1)

MLP Assay (1)

AID Type Active / Inconclusive / Inactive Description
652255 confirmatory 1 / 0 / 1 Discovery of Novel Antagonists of Protease activated receptor 4: PAR 1 Selectivity CRC Assay

Gene RIF (297)

PMID Text
27023670 These results suggest that stabilization of microtubule-unbound tau by phosphorylation at Ser262/356 via the PAR-1/MARK may act in the initial steps of tau mismetabolism in AD pathogenesis
26875892 The serum levels of PAR1 might have a diagnostic value in lung cancer patients
26729042 Thrombin and the PAR-1 activating peptide, TFLLR, lead to the phosphorylation of eNOS-Ser-1177 in human coronary artery endothelial cells, which was blocked by SCH-79797 (SCH), a PAR-1 inhibitor.
26681756 PZ-128 is a promising antiplatelet agent that provides rapid, specific, dose dependent, and reversible inhibition of platelet protease-activated receptor-1 through a novel intracellular mechanism.
26635365 Rab11A and Rab11B differentially regulate intracellular trafficking of PAR1 through distinct endosomal sorting mechanisms
26600192 Binding of the PH domain of PAR-1 enables breast cancer growth and extravillous trophoblast invasion.
26475502 thrombin/PAR-1 interaction regulated MCP-1, TF, MCSF and IL-6 production.
26424552 conjugation of a peptide fragment derived from the third intracellular loop (i3) of the protease-activated receptor 1 (PAR1) to a peptide that can selectively target tumours
26283733 The data reveal a new proprotein convertases -PAR-1-interaction pathway, which offsets the effects of HIV-induced neuroinflammation, viral infection, and potentially the development of HIV-Associated Neurocognitive Disorder.
26283733 F2R (PAR1) DOES NOT block processing of Vpr by soluble PCSK6 (PACE4)
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AA Sequence

MGPRRLLLVAACFSLCGPLLSARTRARRPESKATNATLDPRSFLLRNPNDKYEPFWEDEEKNESGLTEYR      1 - 70
LVSINKSSPLQKQLPAFISEDASGYLTSSWLTLFVPSVYTGVFVVSLPLNIMAIVVFILKMKVKKPAVVY     71 - 140
MLHLATADVLFVSVLPFKISYYFSGSDWQFGSELCRFVTAAFYCNMYASILLMTVISIDRFLAVVYPMQS    141 - 210
LSWRTLGRASFTCLAIWALAIAGVVPLLLKEQTIQVPGLNITTCHDVLNETLLEGYYAYYFSAFSAVFFF    211 - 280
VPLIISTVCYVSIIRCLSSSAVANRSKKSRALFLSAAVFCIFIICFGPTNVLLIAHYSFLSHTSTTEAAY    281 - 350
FAYLLCVCVSSISCCIDPLIYYYASSECQRYVYSILCCKESSDPSSYNSSGQLMASKMDTCSSNLNNSIY    351 - 420
KKLLT                                                                     421 - 425
//

Text Mined References (341)

PMID Year Title
27023670 2016 Stabilization of Microtubule-Unbound Tau via Tau Phosphorylation at Ser262/356 by Par-1/MARK Contributes to Augmentation of AD-Related Phosphorylation and A?42-Induced Tau Toxicity.
26875892 2016 Clinical significance of serum protease activated receptor1 levels in patients with lung cancer.
26729042 2016 Featured Article: Differential regulation of endothelial nitric oxide synthase phosphorylation by protease-activated receptors in adult human endothelial cells.
26681756 2016 Cell-Penetrating Pepducin Therapy Targeting PAR1 in Subjects With Coronary Artery Disease.
26635365 2016 Recycling and Endosomal Sorting of Protease-activated Receptor-1 Is Distinctly Regulated by Rab11A and Rab11B Proteins.
26600192 2015 PH motifs in PAR1&2 endow breast cancer growth.
26475502 2016 Thrombin induced by the extrinsic pathway and PAR-1 regulated inflammation at the site of fracture repair.
26424552 2015 Down-regulation of PAR1 activity with a pHLIP-based allosteric antagonist induces cancer cell death.
26283733 2015 Neuroinflammation-Induced Interactions between Protease-Activated Receptor 1 and Proprotein Convertases in HIV-Associated Neurocognitive Disorder.
26278396 2015 Role of a functional polymorphism in the F2R gene promoter in sarcoidosis.
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