DGIdb - F2R Gene Record

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
347
NP_001983
NM_001992
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:

GuideToPharmacology Gene Category Name	Proteinase-activated receptors
GuideToPharmacology Gene Category ID	59
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

(7 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: 11.96

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Proteinase-activated receptor 1 antagonist

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology TTD
VORAPAXAR F2R

Interaction Score: 5.32

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Novel Target

Trial Name vorapaxar , SCH-530348

Specific Action of the Ligand Antagonist

PMIDs:
19715408

Sources:
TdgClinicalTrial GuideToPharmacology TTD
ARGATROBAN F2R

Interaction Score: 3.99

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10611442

Sources:
NCI
VORAPAXAR SULFATE F2R

Interaction Score: 3.99

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Proteinase-activated receptor 1 antagonist

PMIDs:
None found

Sources:
ChemblInteractions
RIGOSERTIB SODIUM F2R

Interaction Score: 3.99

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Proteinase-activated receptor 1 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DALTEPARIN F2R

Interaction Score: 2.66

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12632026

Sources:
NCI
LEPIRUDIN F2R

Interaction Score: 2.66

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16038707

Sources:
NCI
THROMBIN F2R

Interaction Score: 1.83

Interaction Types & Directionality:

n/a

Interaction Info:

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

Sources:
NCI
RUSALATIDE F2R

Interaction Score: 1.33

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: 0.66

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15345469

Sources:
NCI
WORTMANNIN F2R

Interaction Score: 0.44

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8955143 7559410 10318860

Sources:
NCI
BLEOMYCIN F2R

Interaction Score: 0.42

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15855637

Sources:
NCI
MORPHINE F2R

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12373743

Sources:
NCI
THALIDOMIDE F2R

Interaction Score: 0.23

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:
GuideToPharmacology: 2149
- Version: 29-September-2020
Alternate Names:

3537 HUGO Gene ID

3537 HUGO Gene Symbol

coagulation factor II thrombin receptor HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Proteinase-activated receptors

GuideToPharmacology Gene Category ID 59

Gene Categories:

G PROTEIN COUPLED RECEPTOR

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:
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:
GO: F2R
- Version: 01-May-2021
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:

Direct Interaction	yes
Mechanism of Interaction	Proteinase-activated receptor 1 antagonist
Specific Action of the Ligand	Antagonist

Novel drug target	Novel Target
Trial Name	vorapaxar , SCH-530348
Specific Action of the Ligand	Antagonist

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

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

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

3537	HUGO Gene ID
3537	HUGO Gene Symbol
coagulation factor II thrombin receptor	HUGO Gene Name

F2R Gene Record

F2R 2149 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Proteinase-activated receptor 1 antagonist Specific Action of the Ligand Antagonist

PMIDs: None found

Sources: ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Novel Target Trial Name vorapaxar , SCH-530348 Specific Action of the Ligand Antagonist

PMIDs: 19715408

Sources: TdgClinicalTrial GuideToPharmacology TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10611442

Sources: NCI

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12632026

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16038707

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

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

Sources: NCI

Interaction Types & Directionality: n/a

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

PMIDs: None found

Sources: TdgClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15345469

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 8955143 7559410 10318860

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15855637

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12373743

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 14995997

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15381054

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16930224

Sources: NCI

Ensembl: ENSG00000181104

Alternate Names: F2R Ensembl Gene Name

Gene Info: Gene Biotype PROTEIN_CODING

Publications:

TdgClinicalTrial: P25116

Alternate Names: F2R Gene Symbol

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

Publications:

RussLampel: ENSG00000181104

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

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Proteinase-activated receptor 1 antagonist

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Novel Target

Trial Name vorapaxar , SCH-530348

Specific Action of the Ligand Antagonist

PMIDs:
19715408

Sources:
TdgClinicalTrial GuideToPharmacology TTD

Interaction Types & Directionality:

n/a

PMIDs:
10611442

Sources:
NCI

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Proteinase-activated receptor 1 antagonist

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Proteinase-activated receptor 1 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
12632026

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
16038707

Sources:
NCI

Interaction Types & Directionality:

n/a

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

Sources:
NCI

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name TP-508,Chrysalin

Novel drug target Novel Target

PMIDs:
None found

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
15345469

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
8955143 7559410 10318860

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
15855637

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
12373743

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
14995997

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
15381054

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
16930224

Sources:
NCI

Alternate Names:

F2R Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Alternate Names:

F2R Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

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

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

Alternate Names:

3537 HUGO Gene ID

3537 HUGO Gene Symbol

coagulation factor II thrombin receptor HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Proteinase-activated receptors

GuideToPharmacology Gene Category ID 59

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Alternate Names:

ENSG00000181104 Gene Symbol

F2R Ensembl Id

Gene Categories:

DRUGGABLE GENOME

Alternate Names:

PAR1 GENE_SYMBOL

TR GENE_SYMBOL

F2R GENE_SYMBOL

Alternate Names:

2149 Gene ID

CF2R dGene Synonym

HTR dGene Synonym

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Alternate Names:

F2R TTD Gene Abbreviation

T36483 TTD Target ID

Alternate Names:

CF2R GO Gene Synonym

PAR1 GO Gene Synonym

TR GO Gene Synonym

Gene Categories:

CELL SURFACE, G PROTEIN COUPLED RECEPTOR