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F2R Gene Record

  • Summary
  • Interactions
  • Claims
  • F2R 2149 Druggable Genome

    Alternate Names:

    2149
    COAGULATION FACTOR II THROMBIN RECEPTOR
    F2R
    CF2R
    HTR
    PAR-1
    PAR1
    TR
    187930
    3537
    ENSG00000181104
    OTTHUMG00000131299
    THROMBIN RECEPTOR
    PROTEINASE ACTIVATED RECEPTOR 1
    COAGULATION FACTOR II RECEPTOR
    P25116
    PAR1_HUMAN
    PROTEINASE ACTIVATED RECEPTOR 1 PRECURSOR (PAR-1) (THROMBIN RECEPTOR) (COAGULATION FACTOR II RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P25116]
    Proteinase-activated receptor 1
    T36483

    Gene Info:

    Human Readable Name G PROTEIN COUPLED RECEPTOR
    Human Readable Name DRUGGABLE GENOME
    Interpro Type Family
    Uniprot Evidence 1: Evidence at protein level
    Interpro Acc IPR000276
    Interpro Short Name 7TM_GPCR_Rhodpsn
    Uniprot Status Swiss-Prot
    Interpro Name GPCR, rhodopsin-like, 7TM
    Target Class Receptors
    Target Subclass GPCR
    Target Subclass Rhodopsin
    Gene Biotype PROTEIN_CODING
    (6 More Sources)

    Gene Categories: Category Details

    CELL SURFACE
    G PROTEIN COUPLED RECEPTOR
    DRUGGABLE GENOME

    Publications:

    Bonaca et al., 2009, SCH 530348: a novel oral thrombin receptor antagonist., Future Cardiol
    Robinson et al., 2002, Widespread but regionally specific effects of experimenter- versus self-administered morphine on dendritic spines in the nucleus accumbens, hippocampus, and neocortex of adult rats., Synapse
    Kasuda et al., 2006, Inhibition of PAR4 signaling mediates ethanol-induced attenuation of platelet function in vitro., Alcohol. Clin. Exp. Res.
    Hartwig et al., 1996, D3 phosphoinositides and outside-in integrin signaling by glycoprotein IIb-IIIa mediate platelet actin assembly and filopodial extension induced by phorbol 12-myristate 13-acetate., J. Biol. Chem.
    Zhang et al., 1995, Phosphatidylinositol (3,4,5)-trisphosphate stimulates phosphorylation of pleckstrin in human platelets., J. Biol. Chem.
    Pigazzi et al., 1999, Nitric oxide inhibits thrombin receptor-activating peptide-induced phosphoinositide 3-kinase activity in human platelets., J. Biol. Chem.
    Mirabet et al., 2005, Thrombin increases cardiomyocyte acute cell death after ischemia and reperfusion., J. Mol. Cell. Cardiol.
    Heider et al., 2004, PAR1-type thrombin receptor stimulates migration and matrix adhesion of human colon carcinoma cells by a PKCepsilon-dependent mechanism., Oncol. Res.
    Turcotte et al., 2004, von Hippel-Lindau tumor suppressor protein stimulation by thrombin involves RhoA activation., Int. J. Cancer
    Darmoul et al., 2004, Activation of proteinase-activated receptor 1 promotes human colon cancer cell proliferation through epidermal growth factor receptor transactivation., Mol. Cancer Res.
    Shi et al., 2004, Protease-activated receptors (PAR1 and PAR2) contribute to tumor cell motility and metastasis., Mol. Cancer Res.
    Chen et al., 2004, Termination of protease-activated receptor-1 signaling by beta-arrestins is independent of receptor phosphorylation., J. Biol. Chem.
    Darmoul et al., 2003, Aberrant expression and activation of the thrombin receptor protease-activated receptor-1 induces cell proliferation and motility in human colon cancer cells., Am. J. Pathol.
    Suo et al., 2002, Participation of protease-activated receptor-1 in thrombin-induced microglial activation., J. Neurochem.
    Rudroff et al., 2001, Thrombin enhances adhesion in pancreatic cancer in vitro through the activation of the thrombin receptor PAR 1., Eur J Surg Oncol
    Henrikson et al., 1999, Role of thrombin receptor in breast cancer invasiveness., Br. J. Cancer
    Leger AJ et al., 2006, Blocking the protease-activated receptor 1-4 heterodimer in platelet-mediated thrombosis., Circulation
    Kaushal et al., 2004, Thalidomide protects endothelial cells from doxorubicin-induced apoptosis but alters cell morphology., J. Thromb. Haemost.
    Howell et al., 2005, Absence of proteinase-activated receptor-1 signaling affords protection from bleomycin-induced lung inflammation and fibrosis., Am. J. Pathol.
    Serebruany et al., 2004, Magnitude and time course of platelet inhibition with Aggrenox and Aspirin in patients after ischemic stroke: the AGgrenox versus Aspirin Therapy Evaluation (AGATE) trial., Eur. J. Pharmacol.
    Nylander et al., 2003, Thrombin-induced platelet activation and its inhibition by anticoagulants with different modes of action., Blood Coagul. Fibrinolysis
    Buresi et al., 2005, Activation of proteinase-activated receptor-1 inhibits neurally evoked chloride secretion in the mouse colon in vitro., Am. J. Physiol. Gastrointest. Liver Physiol.
    Kato et al., 1999, In vitro antiplatelet profile of FR171113, a novel non-peptide thrombin receptor antagonist., Eur. J. Pharmacol.
  • ATOPAXAR   F2R

    Interaction Score: 7.73

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Proteinase-activated receptor 1 antagonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions TTD

  • ARGATROBAN   F2R

    Interaction Score: 3.86

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10611442


    Sources:
    NCI

  • DALTEPARIN   F2R

    Interaction Score: 3.86

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12632026


    Sources:
    NCI

  • VORAPAXAR SULFATE   F2R

    Interaction Score: 3.86

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Proteinase-activated receptor 1 antagonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • VORAPAXAR   F2R

    Interaction Score: 3.86

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Novel Target
    Trial Name vorapaxar , SCH-530348

    PMIDs:
    19715408


    Sources:
    TdgClinicalTrial TTD

  • RIGOSERTIB SODIUM   F2R

    Interaction Score: 3.86

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Proteinase-activated receptor 1 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LEPIRUDIN   F2R

    Interaction Score: 2.58

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16038707


    Sources:
    NCI

  • THROMBIN   F2R

    Interaction Score: 1.77

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15559761 15386385 15383630 15280447 14699102 12707033 11841573 11504518 10027305 16505172


    Sources:
    NCI

  • RUSALATIDE   F2R

    Interaction Score: 1.29

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name TP-508,Chrysalin
    Novel drug target Novel Target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • ATROPINE   F2R

    Interaction Score: 0.7

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15345469


    Sources:
    NCI

  • WORTMANNIN   F2R

    Interaction Score: 0.55

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8955143 7559410 10318860


    Sources:
    NCI

  • BLEOMYCIN   F2R

    Interaction Score: 0.41

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15855637


    Sources:
    NCI

  • MORPHINE   F2R

    Interaction Score: 0.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12373743


    Sources:
    NCI

  • THALIDOMIDE   F2R

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    14995997


    Sources:
    NCI

  • ASPIRIN   F2R

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15381054


    Sources:
    NCI

  • ALCOHOL   F2R

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16930224


    Sources:
    NCI

  • Ensembl: ENSG00000181104

    • Version: 101_38

    Alternate Names:
    F2R Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • TdgClinicalTrial: P25116

    • Version: January-2014

    Alternate Names:
    F2R Gene Symbol

    Gene Info:
    Target Class Receptors
    Target Subclass GPCR
    Target Subclass Rhodopsin

    Publications:

  • RussLampel: ENSG00000181104

    • Version: 26-July-2011

    Alternate Names:
    PROTEINASE ACTIVATED RECEPTOR 1 PRECURSOR (PAR-1) (THROMBIN RECEPTOR) (COAGULATION FACTOR II RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P25116] Description
    ENSG00000181104 Ensembl Gene Id
    F2R Display Id

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • HopkinsGroom: P25116

    • Version: 11-September-2012

    Alternate Names:
    PROTEINASE-ACTIVATED RECEPTOR 1 Uniprot Protein Name
    ENSG00000181104 Ensembl Gene Id
    P25116 Uniprot Accession

    Gene Info:
    Interpro Type Family
    Uniprot Evidence 1: Evidence at protein level
    Interpro Acc IPR000276

    Gene Categories:
    G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

    Publications:

  • NCI: F2R

    • Version: 14-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Pigazzi et al., 1999, Nitric oxide inhibits thrombin receptor-activating peptide-induced phosphoinositide 3-kinase activity in human platelets., J. Biol. Chem.
    Zhang et al., 1995, Phosphatidylinositol (3,4,5)-trisphosphate stimulates phosphorylation of pleckstrin in human platelets., J. Biol. Chem.
    Hartwig et al., 1996, D3 phosphoinositides and outside-in integrin signaling by glycoprotein IIb-IIIa mediate platelet actin assembly and filopodial extension induced by phorbol 12-myristate 13-acetate., J. Biol. Chem.

  • HingoraniCasas: ENSG00000181104

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000181104 Gene Symbol
    F2R Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • ChemblInteractions: CF2R

    • Version: chembl_23

    Alternate Names:
    PAR1 GENE_SYMBOL
    TR GENE_SYMBOL
    F2R GENE_SYMBOL

    Gene Info:

    Publications:

  • GO: F2R

    • Version: 01-February-2022

    Alternate Names:
    CF2R GO Gene Synonym
    PAR1 GO Gene Synonym
    TR GO Gene Synonym

    Gene Info:

    Gene Categories:
    CELL SURFACE, G PROTEIN COUPLED RECEPTOR

    Publications:

  • dGene: F2R

    • Version: 27-Jun-2013

    Alternate Names:
    2149 Gene ID
    CF2R dGene Synonym
    HTR dGene Synonym

    Gene Info:

    Gene Categories:
    G PROTEIN COUPLED RECEPTOR

    Publications:

  • TTD: Proteinase activated receptor 1

    • Version: 2020.06.01

    Alternate Names:
    F2R TTD Gene Abbreviation
    T36483 TTD Target ID

    Gene Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21