F2RL1 (F2R Like Trypsin Receptor 1)
A G protein-coupled receptor for trypsin and trypsin-like proteases, involved in inflammation, cancer, and hemostasis.
Gene Information Card
| Symbol | F2RL1 |
|---|---|
| Full Name | F2R Like Trypsin Receptor 1 |
| Gene Type | protein-coding |
| Chromosomal Location | 5q13.3 |
| NCBI Gene ID | 2150 ncbi.nlm.nih.gov/gene/2150 |
| Ensembl ID | ENSG00000164251 |
| UniProt ID | P55085 |
| OMIM ID | 600933 |
| HGNC ID | 3538 |
| Aliases | PAR2, GPR11 |
Description
F2RL1 (F2R Like Trypsin Receptor 1) encodes protease-activated receptor 2 (PAR2), a G protein-coupled receptor activated by trypsin, tryptase, and coagulation factors VIIa and Xa. PAR2 is expressed in various tissues and mediates inflammatory responses, pain, and cancer progression. It is involved in hemostasis, wound healing, and immune regulation.
Disease Associations
| Disease category | Pathophysiological mechanism | Genomic evidence |
|---|---|---|
| Inflammatory bowel disease | PAR2 activation by trypsin-like proteases increases intestinal permeability and inflammation | PMID: 18496526 |
| Pancreatic cancer | PAR2 signaling promotes tumor growth and metastasis via MAPK and NF-κB pathways | PMID: 21502580 |
| Rheumatoid arthritis | PAR2 activation in synovial fibroblasts contributes to joint inflammation and cartilage degradation | PMID: 17086180 |
| Asthma | PAR2 activation in airway epithelial cells induces bronchoconstriction and inflammation | PMID: 11714840 |
| Pain (nociception) | PAR2 activation sensitizes TRPV1 channels, leading to hyperalgesia | PMID: 11714840 |
Expression Profile
Tissue Expression
| Tissue | nTPM | level |
|---|---|---|
| Pancreas | 45.2 | High |
| Prostate | 28.1 | Medium |
| Colon | 22.5 | Medium |
| Small intestine | 20.3 | Medium |
| Kidney | 18.7 | Medium |
| Liver | 12.4 | Low |
| Lung | 10.1 | Low |
| Heart | 5.3 | Low |
Cell Line Expression
| Cell Line | nTPM | Notes |
|---|---|---|
| HEK 293 | 35.0 | High expression in recombinant systems |
| A549 (lung) | 18.5 | Endogenous expression |
| HT-29 (colon) | 22.0 | Endogenous expression |
| MCF7 (breast) | 8.2 | Low expression |
| K562 (leukemia) | 2.1 | Very low expression |
Data source：Human Protein Atlas（proteinatlas.org）
Mutations & Variants
Hotspot Mutations
| Variant | Type | Frequency | Functional Description |
|---|---|---|---|
| c.124G>A (p.Gly42Ser) | missense | <0.01% | Unknown functional effect; rare variant in population databases |
| c.365C>T (p.Thr122Met) | missense | <0.01% | Reported in ClinVar as uncertain significance |
| c.1018G>A (p.Gly340Ser) | missense | <0.01% | No known disease association |
Mutation functional classification
Loss of Function (LOF)
No well-characterized loss-of-function mutations reported in F2RL1.
Gain of Function (GOF)
No well-characterized gain-of-function mutations reported in F2RL1.
Dominant Negative (DN)
No dominant-negative mutations reported for F2RL1.
View complete mutation data：
Gene Ontology (GO)
| • G protein-coupled receptor activity (GO:0004930) | • protease-activated receptor activity (GO:0015057) |
| • signal transduction (GO:0007165) | • inflammatory response (GO:0006954) |
| • cell proliferation (GO:0008283) | • calcium-mediated signaling (GO:0019722) |
Pathways
• Protease-activated receptor signaling pathway (Reactome: R-HSA-456926)
• MAPK signaling pathway (KEGG: hsa04010)
• NF-κB signaling pathway (KEGG: hsa04064)
• Coagulation cascade (Reactome: R-HSA-140877)
Protein Summary
F2RL1 encodes protease-activated receptor 2 (PAR2), a 397-amino acid transmembrane G protein-coupled receptor. PAR2 is activated by proteolytic cleavage of its N-terminal extracellular domain by trypsin, tryptase, and coagulation factors VIIa and Xa. The new N-terminus acts as a tethered ligand that binds to the receptor, initiating intracellular signaling via Gq/11, Gi/o, and β-arrestin pathways. PAR2 is widely expressed in epithelial, endothelial, immune, and cancer cells, and plays key roles in inflammation, pain, cancer progression, and hemostasis.
Related Services
Related Products
| Product name | Cat.No. | Species | Gene ID | |
|---|---|---|---|---|
| F2RL1 Knockout HEK293T Cell Line | EDJ-KQ222 | Human | 2150 | Details Get a Quote |
| F2RL1 Knockout HEK293 Cell Line | EDJ-KQ17871 | Human | 2150 | Details Get a Quote |
| F2RL1 Knockout HCT 116 Cell Line | EDJ-KQ25963 | Human | 2150 | Details Get a Quote |
| F2RL1 Knockout A-549 Cell Line | EDJ-KQ27222 | Human | 2150 | Details Get a Quote |
| F2RL1 Knockout HeLa Cell Line | EDJ-KQ27223 | Human | 2150 | Details Get a Quote |
| F2RL1 Knockout OE33 Cell Line | EDC07842 | Human | 2169 | Details Get a Quote |
Displaying Records 1 To 6 Of 6 Records
