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Aliases for F2R Gene

Aliases for F2R Gene

  • Coagulation Factor II Thrombin Receptor 2 3 5
  • PAR-1 3 4
  • CF2R 3 4
  • PAR1 3 4
  • TR 3 4
  • Coagulation Factor II (Thrombin) Receptor 2
  • Proteinase-Activated Receptor 1 3
  • Coagulation Factor II Receptor 4
  • Protease Activated Receptor 1 2
  • Protease-Activated Receptor 1 3
  • Thrombin Receptor 4
  • HTR 3

External Ids for F2R Gene

Previous GeneCards Identifiers for F2R Gene

  • GC05P074817
  • GC05P076246
  • GC05P076050
  • GC05P076095
  • GC05P076047
  • GC05P071219

Summaries for F2R Gene

Entrez Gene Summary for F2R Gene

  • Coagulation factor II receptor is a 7-transmembrane receptor involved in the regulation of thrombotic response. Proteolytic cleavage leads to the activation of the receptor. F2R is a G-protein coupled receptor family member. Alternative splicing results in multiple transcript variants. [provided by RefSeq, Aug 2015]

GeneCards Summary for F2R Gene

F2R (Coagulation Factor II Thrombin Receptor) is a Protein Coding gene. Diseases associated with F2R include Macrocytic Anemia, Refractory, Due To 5Q Deletion, Somatic and Orofacial Granulomatosis. Among its related pathways are Signaling by GPCR and Pathways in cancer. GO annotations related to this gene include G-protein coupled receptor activity and G-protein alpha-subunit binding. An important paralog of this gene is F2RL1.

UniProtKB/Swiss-Prot for F2R Gene

  • High affinity receptor for activated thrombin coupled to G proteins that stimulate phosphoinositide hydrolysis. May play a role in platelets activation and in vascular development.

Tocris Summary for F2R Gene

  • Protease-activated receptors (PARs, also known as thrombin receptors) are G-protein-coupled receptors, activated by cleavage of their N-terminal domains by serine proteases. Hydrolysis reveals a tethered peptide ligand, which affects transmembrane signaling.

Gene Wiki entry for F2R Gene

No data available for PharmGKB "VIP" Summary , fRNAdb sequence ontologies and piRNA Summary for F2R Gene

Genomics for F2R Gene

Regulatory Elements for F2R Gene

Enhancers for F2R Gene
GeneHancer Identifier Enhancer Score Enhancer Sources Gene-Enhancer Score TSS distance (kb) Number of Genes Away Size (kb) Transcription Factor Binding Sites within enhancer Gene Targets for Enhancer
GH05F076735 1.8 FANTOM5 Ensembl ENCODE 44.5 +22.2 22173 5.1 HDGF PKNOX1 ARNT ZFP64 ARID4B SIN3A FEZF1 ZNF2 ZNF548 FOS F2R RPL7P23 ENSG00000225407 IQGAP2 GC05P076755
GH05F076786 1.6 FANTOM5 Ensembl ENCODE 23 +73.7 73705 5.8 PKNOX1 ATF1 SIN3A FEZF1 ZNF2 GLIS2 FOS ZNF263 SP3 SP5 F2RL1 F2R ENSG00000225407 RPL7P23 CRHBP RAP1BL GC05P076755
GH05F076687 1.1 Ensembl ENCODE 18.6 -25.3 -25343 6.2 SOX13 ZNF146 JUN MAX BMI1 EBF1 ZNF366 SCRT2 EED FOS F2R ENSG00000225407 LOC101929109 IQGAP2 RNU6ATAC36P CRHBP F2RL1 ENSG00000277188 F2RL2
GH05F076818 1 ENCODE 20.3 +104.9 104909 5.6 ARID4B SIN3A GLI4 DMAP1 ZNF48 ZNF2 YY1 ZNF121 GLIS2 FOS F2RL1 F2R ENSG00000225407 RPL7P23 RAP1BL GC05P076819 GC05P076820 RN7SL208P
GH05F076720 1 Ensembl ENCODE 17.8 +5.1 5059 1.0 CTCF TBL1XR1 RAD21 ZBTB40 EED CREM MTA2 TRIM22 EP300 TBX21 F2R ENSG00000225407 GC05P076755
- Elite enhancer and/or Elite enhancer-gene association Download GeneHancer data dump

Enhancers around F2R on UCSC Golden Path with GeneCards custom track

Promoters for F2R Gene
Ensembl Regulatory Elements (ENSRs) TSS Distance (bp) Size (bp) Binding Sites for Transcription Factors within promoters
ENSR00001283316 757 3201 ZFP64 SIN3A ZNF48 GLIS2 GATA2 ZNF202 SP5 REST GLIS1 KDM1A

Genomic Location for F2R Gene

Chromosome:
5
Start:
76,716,043 bp from pter
End:
76,735,781 bp from pter
Size:
19,739 bases
Orientation:
Plus strand

Genomic View for F2R Gene

Genes around F2R on UCSC Golden Path with GeneCards custom track

Cytogenetic band:
F2R Gene in genomic location: bands according to Ensembl, locations according to GeneLoc (and/or Entrez Gene and/or Ensembl if different)
Genomic Location for F2R Gene
GeneLoc Logo Genomic Neighborhood Exon StructureGene Density

RefSeq DNA sequence for F2R Gene

Proteins for F2R Gene

  • Protein details for F2R Gene (UniProtKB/Swiss-Prot)

    Protein Symbol:
    P25116-PAR1_HUMAN
    Recommended name:
    Proteinase-activated receptor 1
    Protein Accession:
    P25116
    Secondary Accessions:
    • Q53XV0
    • Q96RF7
    • Q9BUN4

    Protein attributes for F2R Gene

    Size:
    425 amino acids
    Molecular mass:
    47441 Da
    Quaternary structure:
    No Data Available

    Three dimensional structures from OCA and Proteopedia for F2R Gene

neXtProt entry for F2R Gene

Post-translational modifications for F2R Gene

  • A proteolytic cleavage generates a new N-terminus that functions as a tethered ligand.
  • Phosphorylated in the C-terminal tail; probably mediating desensitization prior to the uncoupling and internalization of the receptor.
  • Glycosylation at Asn 35, Asn 62, Asn 75, Asn 250, and Asn 259
  • Modification sites at PhosphoSitePlus

Other Protein References for F2R Gene

ENSEMBL proteins:
REFSEQ proteins:

No data available for DME Specific Peptides for F2R Gene

Domains & Families for F2R Gene

Gene Families for F2R Gene

HGNC:
IUPHAR :

Suggested Antigen Peptide Sequences for F2R Gene

GenScript: Design optimal peptide antigens:

Graphical View of Domain Structure for InterPro Entry

P25116

UniProtKB/Swiss-Prot:

PAR1_HUMAN :
  • The cleaved signal peptide may not be degraded and may function as an intracellular angiogenesis inhibitor peptide known as parstatin.
  • Belongs to the G-protein coupled receptor 1 family.
Domain:
  • The cleaved signal peptide may not be degraded and may function as an intracellular angiogenesis inhibitor peptide known as parstatin.
Family:
  • Belongs to the G-protein coupled receptor 1 family.
genes like me logo Genes that share domains with F2R: view

Function for F2R Gene

Molecular function for F2R Gene

GENATLAS Biochemistry:
coagulation factor II (thrombin) receptor,proteinase activated receptor 1 (centromeric to the common proximal breakpoint and unlikely involved in 5q- syndrome), G protein coupled receptor superfamily
UniProtKB/Swiss-Prot Function:
High affinity receptor for activated thrombin coupled to G proteins that stimulate phosphoinositide hydrolysis. May play a role in platelets activation and in vascular development.

Gene Ontology (GO) - Molecular Function for F2R Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0001965 G-protein alpha-subunit binding IEA,ISS --
GO:0004871 signal transducer activity IEA --
GO:0004930 G-protein coupled receptor activity ISS,TAS 17848177
GO:0005102 receptor binding IPI 1672265
GO:0005515 protein binding IPI 17848177
genes like me logo Genes that share ontologies with F2R: view
genes like me logo Genes that share phenotypes with F2R: view

Animal Models for F2R Gene

MGI Knock Outs for F2R:

Animal Model Products

  • Taconic Biosciences Mouse Models for F2R

Inhibitory RNA Products

Clone Products

  • Addgene plasmids for F2R

Flow Cytometry Products

No data available for Enzyme Numbers (IUBMB) , Human Phenotype Ontology , Transcription Factor Targets and HOMER Transcription for F2R Gene

Localization for F2R Gene

Subcellular locations from UniProtKB/Swiss-Prot for F2R Gene

Cell membrane; Multi-pass membrane protein.

Subcellular locations from

COMPARTMENTS
Extracellular space Cytosol Plasma membrane Cytoskeleton Lysosome Endosome Peroxisome ER Golgi Apparatus Nucleus Mitochondrion 0 1 2 3 4 5 Confidence
COMPARTMENTS Subcellular localization image for F2R gene
Compartment Confidence
plasma membrane 5
extracellular 5
endosome 5
golgi apparatus 4
cytoskeleton 2
cytosol 2
nucleus 1

Gene Ontology (GO) - Cellular Components for F2R Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0005576 extracellular region TAS --
GO:0005623 cell IEA --
GO:0005769 early endosome IDA 22547407
GO:0005770 late endosome IDA 24732013
GO:0005794 Golgi apparatus TAS 7961693
genes like me logo Genes that share ontologies with F2R: view

Pathways & Interactions for F2R Gene

genes like me logo Genes that share pathways with F2R: view

SIGNOR curated interactions for F2R Gene

Activates:
Inactivates:
Is activated by:

Gene Ontology (GO) - Biological Process for F2R Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0000186 activation of MAPKK activity ISS --
GO:0002248 connective tissue replacement involved in inflammatory response wound healing IDA 9639571
GO:0003105 negative regulation of glomerular filtration ISS --
GO:0006919 activation of cysteine-type endopeptidase activity involved in apoptotic process IDA 10692450
GO:0006954 inflammatory response IEA,ISS --
genes like me logo Genes that share ontologies with F2R: view

Drugs & Compounds for F2R Gene

(91) Drugs for F2R Gene - From: DrugBank, ApexBio, DGIdb, Tocris, and Novoseek

Name Status Disease Links Group Role Mechanism of Action Clinical Trials
Vorapaxar Approved Pharma Target, antagonist PAR-1 antagonist,potent and orally active 15
Streptokinase Approved Pharma Target, cleavage 14
Argatroban Approved, Investigational Pharma Thrombin mediated fibrinogen cleavage inhibitor 19
SCH-530348 Investigational Pharma Target 0
SR-123781A Investigational Pharma Target 0

(58) Additional Compounds for F2R Gene - From: Novoseek and IUPHAR

Name Synonyms Role CAS Number PubChem IDs PubMed IDs
[<sup>3</sup>H]haTRAP
Agonist
atopaxar
Antagonist
RWJ-56110
Antagonist
SCH530348
Antagonist
TFLLR-NH<sub>2</sub>
Full agonist, Agonist

(5) Tocris Compounds for F2R Gene

Compound Action Cas Number
RWJ 56110 Selective PAR1 antagonist 252889-88-6
SCH 79797 dihydrochloride Potent, selective non-peptide PAR1 antagonist 1216720-69-2
SLIGKV-NH2 PAR2 receptor agonist 190383-13-2
SLIGRL-NH2 PAR2-activating peptide 171436-38-7
TRAP-6 PAR1 peptide fragment (residues 42-47); acts as a PAR1 agonist 141136-83-6

(20) ApexBio Compounds for F2R Gene

Compound Action Cas Number
APC 366 Selective tryptase inhibitor 158921-85-8
Argatroban Thrombin mediated fibrinogen cleavage inhibitor 74863-84-6
Axitinib (AG 013736) VEGFR1/ c-Kit inhibitor 319460-85-0
BIBR 953 (Dabigatran, Pradaxa) Thrombin inhibitor,potent,reversible and direct 211914-51-1
BIBR-1048 Thrombin inhibitor 211915-06-9
FR 171113 173904-50-2
FSLLRY-NH2 245329-02-6
ML161 PAR1 inhibitor 423735-93-7
Parstatin (human) 1065755-99-8
Q94 hydrochloride 1052076-77-3
RLLFT-NH2 447408-68-6
RWJ 56110 252889-88-6
SCH 79797 dihydrochloride 1216720-69-2
tcY-NH2 327177-34-4
TFLLR-NH2 PAR1 selective agonist 197794-83-5
Thrombin Receptor Activator for Peptide 5 (TRAP-5) 141685-53-2
Thrombin Receptor Agonist Peptide 137339-65-2
TRAP-6 PAR1 agonist 141136-83-6
VKGILS-NH2 control peptide for SLIGKV-NH2, PAR1 agonist 942413-05-0
Vorapaxar PAR-1 antagonist,potent and orally active 618385-01-6
genes like me logo Genes that share compounds with F2R: view

Transcripts for F2R Gene

mRNA/cDNA for F2R Gene

Unigene Clusters for F2R Gene

Coagulation factor II (thrombin) receptor:
Representative Sequences:

Inhibitory RNA Products

Clone Products

  • Addgene plasmids for F2R

Flow Cytometry Products

Alternative Splicing Database (ASD) splice patterns (SP) for F2R Gene

ExUns: 1 ^ 2 ^ 3a · 3b
SP1:
SP2: -

Relevant External Links for F2R Gene

GeneLoc Exon Structure for
F2R
ECgene alternative splicing isoforms for
F2R

Expression for F2R Gene

mRNA expression in normal human tissues from GTEx, Illumina, BioGPS, and SAGE for F2R Gene

mRNA expression in embryonic tissues and stem cells from LifeMap Discovery

mRNA differential expression in normal tissues according to GTEx for F2R Gene

This gene is overexpressed in Minor Salivary Gland (x4.6) and Artery - Aorta (x4.4).

Protein differential expression in normal tissues from HIPED for F2R Gene

This gene is overexpressed in Testis (31.6), Breast (23.2), and Platelet (14.2).

Integrated Proteomics: protein expression in normal tissues and cell lines from ProteomicsDB, PaxDb, MaxQB, and MOPED for F2R Gene



Protein tissue co-expression partners for F2R Gene

- Elite partner

NURSA nuclear receptor signaling pathways regulating expression of F2R Gene:

F2R

SOURCE GeneReport for Unigene cluster for F2R Gene:

Hs.482562

mRNA Expression by UniProt/SwissProt for F2R Gene:

P25116-PAR1_HUMAN
Tissue specificity: Platelets and vascular endothelial cells.
genes like me logo Genes that share expression patterns with F2R: view

Orthologs for F2R Gene

This gene was present in the common ancestor of chordates.

Orthologs for F2R Gene

Organism Taxonomy Gene Similarity Type Details
chimpanzee
(Pan troglodytes)
Mammalia F2R 34 35
  • 99.53 (n)
dog
(Canis familiaris)
Mammalia F2R 34 35
  • 86.41 (n)
cow
(Bos Taurus)
Mammalia F2R 34 35
  • 80.55 (n)
mouse
(Mus musculus)
Mammalia F2r 34 16 35
  • 79.87 (n)
rat
(Rattus norvegicus)
Mammalia F2r 34
  • 79.01 (n)
oppossum
(Monodelphis domestica)
Mammalia F2R 35
  • 70 (a)
OneToOne
chicken
(Gallus gallus)
Aves F2R 34 35
  • 63.18 (n)
lizard
(Anolis carolinensis)
Reptilia F2R 35
  • 62 (a)
OneToOne
tropical clawed frog
(Silurana tropicalis)
Amphibia f2r 34
  • 59.49 (n)
African clawed frog
(Xenopus laevis)
Amphibia f2r-A-prov 34
zebrafish
(Danio rerio)
Actinopterygii f2r 34 35
  • 56.88 (n)
Species where no ortholog for F2R was found in the sources mined by GeneCards:
  • A. gosspyii yeast (Ashbya gossypii)
  • Actinobacteria (Mycobacterium tuberculosis)
  • African malaria mosquito (Anopheles gambiae)
  • Alicante grape (Vitis vinifera)
  • alpha proteobacteria (Wolbachia pipientis)
  • amoeba (Dictyostelium discoideum)
  • Archea (Pyrococcus horikoshii)
  • baker's yeast (Saccharomyces cerevisiae)
  • barley (Hordeum vulgare)
  • beta proteobacteria (Neisseria meningitidis)
  • bread mold (Neurospora crassa)
  • Chromalveolata (Phytophthora infestans)
  • common water flea (Daphnia pulex)
  • corn (Zea mays)
  • E. coli (Escherichia coli)
  • filamentous fungi (Aspergillus nidulans)
  • Firmicute bacteria (Streptococcus pneumoniae)
  • fission yeast (Schizosaccharomyces pombe)
  • fruit fly (Drosophila melanogaster)
  • green algae (Chlamydomonas reinhardtii)
  • honey bee (Apis mellifera)
  • K. lactis yeast (Kluyveromyces lactis)
  • loblloly pine (Pinus taeda)
  • malaria parasite (Plasmodium falciparum)
  • medicago trunc (Medicago Truncatula)
  • moss (Physcomitrella patens)
  • orangutan (Pongo pygmaeus)
  • pig (Sus scrofa)
  • platypus (Ornithorhynchus anatinus)
  • rainbow trout (Oncorhynchus mykiss)
  • rice (Oryza sativa)
  • rice blast fungus (Magnaporthe grisea)
  • schistosome parasite (Schistosoma mansoni)
  • sea anemone (Nematostella vectensis)
  • sea squirt (Ciona intestinalis)
  • sea squirt (Ciona savignyi)
  • sea urchin (Strongylocentrotus purpuratus)
  • sorghum (Sorghum bicolor)
  • soybean (Glycine max)
  • stem rust fungus (Puccinia graminis)
  • sugarcane (Saccharum officinarum)
  • thale cress (Arabidopsis thaliana)
  • tomato (Lycopersicon esculentum)
  • toxoplasmosis (Toxoplasma gondii)
  • Trichoplax (Trichoplax adhaerens)
  • wheat (Triticum aestivum)
  • worm (Caenorhabditis elegans)

Evolution for F2R Gene

ENSEMBL:
Gene Tree for F2R (if available)
TreeFam:
Gene Tree for F2R (if available)

Paralogs for F2R Gene

(7) SIMAP similar genes for F2R Gene using alignment to 2 proteins:

genes like me logo Genes that share paralogs with F2R: view

Variants for F2R Gene

Sequence variations from dbSNP and Humsavar for F2R Gene

SNP ID Clin Chr 05 pos Sequence Context AA Info Type
rs10035419 -- 76,730,570(+) aacca(A/G)ttctc intron-variant
rs1055103 -- 76,733,027(+) ACTAT(C/G)CCTAC reference, missense
rs1055222 -- 76,735,584(+) CTAGC(A/C)CTGGT utr-variant-3-prime
rs1055227 -- 76,735,707(+) ATGTC(A/C)CTGTT utr-variant-3-prime
rs111343436 -- 76,721,420(+) ACCTT(C/G)TCGTG intron-variant

Structural Variations from Database of Genomic Variants (DGV) for F2R Gene

Variant ID Type Subtype PubMed ID
nsv1035135 CNV gain 25217958
esv2730324 CNV deletion 23290073
esv2730323 CNV deletion 23290073

Variation tolerance for F2R Gene

Residual Variation Intolerance Score: 28.9% of all genes are more intolerant (likely to be disease-causing)
Gene Damage Index Score: 0.83; 17.44% of all genes are more intolerant (likely to be disease-causing)

Relevant External Links for F2R Gene

Human Gene Mutation Database (HGMD)
F2R
SNPedia medical, phenotypic, and genealogical associations of SNPs for
F2R

No data available for Polymorphic Variants from UniProtKB/Swiss-Prot for F2R Gene

Disorders for F2R Gene

MalaCards: The human disease database

(10) MalaCards diseases for F2R Gene - From: DISEASES, Novoseek, and GeneCards

Disorder Aliases PubMed IDs
macrocytic anemia, refractory, due to 5q deletion, somatic
  • chromosome 5q deletion syndrome
orofacial granulomatosis
  • granulomatosis, orofacial
melanoma metastasis
ariboflavinosis
  • riboflavin deficiency
bernard-soulier syndrome, type c
  • bernard-soulier syndrome, type a1
- elite association - COSMIC cancer census association via MalaCards
Search F2R in MalaCards View complete list of genes associated with diseases

Relevant External Links for F2R

Genetic Association Database (GAD)
F2R
Human Genome Epidemiology (HuGE) Navigator
F2R
Atlas of Genetics and Cytogenetics in Oncology and Haematology:
F2R
genes like me logo Genes that share disorders with F2R: view

No data available for UniProtKB/Swiss-Prot and Genatlas for F2R Gene

Publications for F2R Gene

  1. Protease-activated receptors 1 and 4 mediate activation of human platelets by thrombin. (PMID: 10079109) Kahn M.L. … Coughlin S.R. (J. Clin. Invest. 1999) 3 4 22 64
  2. The protease-activated receptor 1 possesses a functional and cleavable signal peptide which is necessary for receptor expression. (PMID: 22659187) Zampatis D.E. … Schulein R. (FEBS Lett. 2012) 3 4 64
  3. New gene functions in megakaryopoiesis and platelet formation. (PMID: 22139419) Gieger C. … Soranzo N. (Nature 2011) 3 46 64
  4. Kallikrein-related peptidase 4: a new activator of the aberrantly expressed protease-activated receptor 1 in colon cancer cells. (PMID: 20056842) Gratio V. … Darmoul D. (Am. J. Pathol. 2010) 3 22 64
  5. Variation at the NFATC2 locus increases the risk of thiazolidinedione-induced edema in the Diabetes REduction Assessment with ramipril and rosiglitazone Medication (DREAM) study. (PMID: 20628086) Bailey S.D. … Anand S. (Diabetes Care 2010) 3 46 64

Products for F2R Gene

Sources for F2R Gene

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