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27 sources retrieved · Most recent: April 2026 · Index updated 14 days ago
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F2RL1
F2R like trypsin receptor 1
Chromosome 5 · 5q13.3
NCBI Gene: 2150Ensembl: ENSG00000164251.5HGNC: HGNC:3538UniProt: P55085
404PubMed Papers
20Diseases
0Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Receptor
RESEARCH IMPACT
Highly StudiedTrending
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
positive regulation of positive chemotaxisnegative regulation of toll-like receptor 3 signaling pathwaypositive regulation of toll-like receptor 3 signaling pathwaypositive regulation of toll-like receptor 4 signaling pathwayneurodegenerative diseasealcohol drinkingvenous thromboembolismhepatocellular carcinoma
✦AI Summary

F2RL1 (Protease-Activated Receptor 2, PAR2) is a G protein-coupled receptor that recognizes trypsin and serine proteases, serving as a critical sensor of proteolytic activity in multiple physiological contexts 1. The receptor activates diverse intracellular signaling pathways including phospholipase C, calcium mobilization, MAPK, NF-κB, and Rho, enabling broad cellular responses 1. F2RL1 plays dual roles in barrier function and inflammation. It maintains intestinal epithelial integrity and lysosomal autophagy through FOXA2-mediated ATP6V0E1 transcription, protecting against colitis-associated colorectal cancer 2. Conversely, F2RL1 activation promotes inflammatory responses by regulating leukocyte recruitment, dendritic cell maturation, and cytokine production 1. Bacterial proteases, including Bacteroides fragilis serine protease 1, exploit F2RL1 to disrupt intestinal barriers and trigger colonic inflammation 3. In disease contexts, elevated F2RL1 expression associates with poor prognosis in cervical cancer, correlating with reduced immune infiltration and immune evasion 4. PAR2 activation also induces cellular senescence in kidney disease, promoting renal fibrosis 5. Conversely, in auditory hair cell regeneration, proteolytic F2RL1 activation initiates a cascade through HBEGF-EGFR-ERK signaling essential for supporting cell proliferation 6. These findings establish F2RL1 as a context-dependent regulator of inflammation, barrier function, and tissue regeneration.

Sources cited
1
F2RL1 is a receptor for trypsin and trypsin-like enzymes that activates PLC, calcium, MAPK, NF-κB, and Rho signaling pathways
PMID: 28445455
2
F2RL1 deficiency in intestinal epithelial cells suppresses FOXA2 expression, leading to autophagy dysfunction and exacerbating colitis-associated colorectal cancer
PMID: 40205686
3
Bacteroides fragilis serine protease 1 cleaves and activates PAR2 (F2RL1), disrupting the intestinal barrier and triggering colonic inflammation
PMID: 41015045
4
F2RL1 expression is elevated in cervical cancer tissues compared to normal tissues, correlates with reduced overall survival, and shows inverse correlation with immune cell infiltration
PMID: 39939734
5
PAR2 activation induces cellular senescence in renal tubular epithelial cells with defective fatty acid oxidation, and PAR2-deficient kidneys are protected from renal fibrosis
PMID: 38687090
6
Proteolytic activation of F2RL1 initiates a signaling cascade through HBEGF shedding and EGFR-mediated ERK signaling essential for auditory hair cell regeneration in birds
PMID: 38128539
Disease Associationsⓘ20
neurodegenerative diseaseOpen Targets
0.46Moderate
alcohol drinkingOpen Targets
0.36Weak
venous thromboembolismOpen Targets
0.24Weak
hepatocellular carcinomaOpen Targets
0.12Weak
neoplasmOpen Targets
0.11Weak
colorectal carcinomaOpen Targets
0.11Weak
lung cancerOpen Targets
0.10Weak
lung adenocarcinomaOpen Targets
0.10Weak
colitisOpen Targets
0.10Suggestive
asthmaOpen Targets
0.09Suggestive
experimental autoimmune encephalomyelitisOpen Targets
0.09Suggestive
injuryOpen Targets
0.09Suggestive
ovarian cancerOpen Targets
0.09Suggestive
cancerOpen Targets
0.09Suggestive
obesityOpen Targets
0.09Suggestive
non-small cell lung carcinomaOpen Targets
0.08Suggestive
oral squamous cell carcinomaOpen Targets
0.08Suggestive
renal cell carcinomaOpen Targets
0.08Suggestive
gastroesophageal reflux diseaseOpen Targets
0.08Suggestive
posterior cortical atrophyOpen Targets
0.08Suggestive
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Related Genes
S1PR3Protein interaction97%GNAQProtein interaction97%TRPA1Protein interaction79%S1PR1Protein interaction79%PRSS3Protein interaction78%PRSS1Protein interaction76%
Tissue Expression6 tissues
Liver
100%
Bone Marrow
72%
Heart
57%
Lung
40%
Brain
9%
Ovary
5%
Gene Interaction Network
Click a node to explore
F2RL1S1PR3GNAQTRPA1S1PR1PRSS3PRSS1
PROTEIN STRUCTURE
Preparing viewer…
PDB5NDD · 2.80 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
0.99LoF Tolerant
pLIⓘ
0.00Tolerant
Observed/Expected LoF0.64 [0.43–0.99]
RankingsWhere F2RL1 stands among ~20K protein-coding genes
  • #717of 20,598
    Most Researched404 · top 5%
  • #9,481of 17,882
    Most Constrained (LOEUF)0.99
Genes detectedF2RL1
Sources retrieved27 papers
Response time—
📄 Sources
27▼
1
Dysfunction of autophagy in high-fat diet-induced non-alcoholic fatty liver disease.
PMID: 37700498
Autophagy · 2024
1.00
2
PAR2-mediated cellular senescence promotes inflammation and fibrosis in aging and chronic kidney disease.
PMID: 38687090
Aging Cell · 2024
0.90
3
Bioinformatics and experimental insights into F2RL1 as a key biomarker in cervical cancer diagnosis and prognosis.
PMID: 39939734
Sci Rep · 2025
0.80
4
Increased melanin induces aberrant keratinocyte - melanocyte - basal - fibroblast cell communication and fibrogenesis by inducing iron overload and ferroptosis resistance in keloids.
PMID: 40102920
Cell Commun Signal · 2025
0.72
5
Neutrophil-derived serine proteases induce FOXA2-mediated autophagy dysfunction and exacerbate colitis-associated carcinogenesis via protease activated receptor 2.
PMID: 40205686
Autophagy · 2025
0.70