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GeneE
26 sources retrieved · Most recent: April 2026 · Index updated 14 days ago
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F2R
coagulation factor II thrombin receptor
Chromosome 5 · 5q13.3
NCBI Gene: 2149Ensembl: ENSG00000181104.7HGNC: HGNC:3537UniProt: P25116
414PubMed Papers
20Diseases
4Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Receptor
RESEARCH IMPACT
Highly StudiedTrending
CLINICAL
FDA Approved Target
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
connective tissue replacement involved in inflammatory response wound healingpositive regulation of apoptotic processpositive regulation of canonical NF-kappaB signal transductionpositive regulation of MAPK cascademyocardial infarctionneurodegenerative diseaseperipheral arterial diseasestroke
✦AI Summary

F2R (coagulation factor II thrombin receptor) is a G protein-coupled receptor that functions as a high-affinity thrombin receptor, mediating calcium signaling through phospholipase C activation and inositol 1,4,5-trisphosphate production 12. Beyond hemostasis, F2R regulates diverse physiological processes including platelet activation, vascular development 3, and inflammatory responses through upregulation of pro-inflammatory cytokines like IL-6 and MCP-1 45. F2R is increasingly recognized as oncogenic across multiple cancer types. In anaplastic thyroid cancer, POLR1F promotes F2R transcription via H3K4 methylation, activating p38 MAPK signaling to enhance proliferation and stemness 6. F2R expression is elevated in gastric adenocarcinoma and correlates with poor prognosis and advanced tumor stage 7. Similarly, high F2R expression in ovarian cancer associates with reduced progression-free survival, chemotherapy resistance, and increased metastatic potential; F2R suppression reduces cell motility and invasion 8. In gliomas, F2R missense variants (R214H, C378G) predict structural destabilization and altered cancer progression 9. Clinically, F2R IVSn-14 A/T polymorphisms influence clopidogrel response in stroke patients, with T-allele carriers showing reduced recurrent stroke risk 10. F2R also mediates fibroblast-endothelial interactions in tissue remodeling and contributes to psoriatic inflammation through the PRSS3-F2R pathway 1112.

Sources cited
1
Beyond hemostasis, F2R regulates diverse physiological processes including platelet activation, vascular development , and inflammatory responses through upregulation of pro-inflammatory cytokines like IL-6 and MCP-1 , .
PMID: 10079109
2
In anaplastic thyroid cancer, POLR1F promotes F2R transcription via H3K4 methylation, activating p38 MAPK signaling to enhance proliferation and stemness .
PMID: 40250711
3
F2R expression is elevated in gastric adenocarcinoma and correlates with poor prognosis and advanced tumor stage .
PMID: 38291086
4
Similarly, high F2R expression in ovarian cancer associates with reduced progression-free survival, chemotherapy resistance, and increased metastatic potential; F2R suppression reduces cell motility and invasion .
PMID: 40943451
5
In gliomas, F2R missense variants (R214H, C378G) predict structural destabilization and altered cancer progression .
PMID: 41550510
6
Clinically, F2R IVSn-14 A/T polymorphisms influence clopidogrel response in stroke patients, with T-allele carriers showing reduced recurrent stroke risk .
PMID: 33093222
Disease Associationsⓘ20
myocardial infarctionOpen Targets
0.53Moderate
neurodegenerative diseaseOpen Targets
0.49Moderate
peripheral arterial diseaseOpen Targets
0.46Moderate
strokeOpen Targets
0.37Weak
Recurrent thrombophlebitisOpen Targets
0.37Weak
preeclampsiaOpen Targets
0.29Weak
von Willebrand disease 1Open Targets
0.19Weak
dermatitisOpen Targets
0.14Weak
neoplasmOpen Targets
0.12Weak
acute coronary syndromeOpen Targets
0.11Weak
breast cancerOpen Targets
0.11Weak
coronary artery diseaseOpen Targets
0.10Weak
melanomaOpen Targets
0.10Suggestive
hepatocellular carcinomaOpen Targets
0.10Suggestive
esophageal squamous cell carcinomaOpen Targets
0.09Suggestive
injuryOpen Targets
0.09Suggestive
chronic obstructive pulmonary diseaseOpen Targets
0.09Suggestive
diabetic nephropathyOpen Targets
0.09Suggestive
non-small cell lung carcinomaOpen Targets
0.09Suggestive
glioblastoma multiformeOpen Targets
0.08Suggestive
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets4
ATOPAXARPhase II
Proteinase-activated receptor 1 antagonist
acute coronary syndrome
PZ-128Phase II
Proteinase-activated receptor 1 inhibitor
VORAPAXARApproved
Proteinase-activated receptor 1 antagonist
Recurrent thrombophlebitis
VORAPAXAR SULFATEApproved
Proteinase-activated receptor 1 antagonist
Related Genes
THBDProtein interaction100%PROCProtein interaction100%PROCRProtein interaction99%ARRB1Protein interaction99%LPAR6Protein interaction98%LPAR5Protein interaction98%
Tissue Expression6 tissues
Heart
100%
Lung
97%
Liver
26%
Ovary
10%
Brain
10%
Bone Marrow
10%
Gene Interaction Network
Click a node to explore
F2RTHBDPROCPROCRARRB1LPAR6LPAR5
PROTEIN STRUCTURE
Preparing viewer…
PDB3LU9 · 1.80 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
0.88LoF Tolerant
pLIⓘ
0.01Tolerant
Observed/Expected LoF0.55 [0.36–0.88]
RankingsWhere F2R stands among ~20K protein-coding genes
  • #691of 20,598
    Most Researched414 · top 5%
  • #516of 1,025
    FDA-Approved Drug Targets2
  • #7,817of 17,882
    Most Constrained (LOEUF)0.88
Genes detectedF2R
Sources retrieved26 papers
Response time—
📄 Sources
26▼
1
Fibroblast atlas: Shared and specific cell types across tissues.
PMID: 40173240
Sci Adv · 2025
1.00
2
Dysfunction of autophagy in high-fat diet-induced non-alcoholic fatty liver disease.
PMID: 37700498
Autophagy · 2024
0.90
3
POLR1F promotes proliferation and stemness of anaplastic thyroid cancer by activating F2R/p38 MAPK signaling.
PMID: 40250711
Biochim Biophys Acta Mol Cell Res · 2025
0.80
4
Identification of prognosis and therapy related intratumoral microbiome and immune signatures in gastric cancer.
PMID: 40677704
Front Immunol · 2025
0.76
5
Neutrophil-derived serine proteases induce FOXA2-mediated autophagy dysfunction and exacerbate colitis-associated carcinogenesis via protease activated receptor 2.
PMID: 40205686
Autophagy · 2025
0.72