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This gene encodes a member of the G-protein coupled receptor 1 family of proteins. The encoded cell surface receptor is activated through proteolytic cleavage of its extracellular amino terminus, resulting in a new amino terminus that acts as a tethered ligand that binds to an extracellular loop domain. Activation of the receptor has been shown to stimulate vascular smooth muscle relaxation, dilate blood vessels, increase blood flow, and lower blood pressure. This protein is also important in the inflammatory response, as well as innate and adaptive immunity. [provided by RefSeq, Jun 2016]
F2RL1 (F2R Like Trypsin Receptor 1) is a Protein Coding gene. Diseases associated with F2RL1 include Pulmonary Vein Stenosis and Granulomatous Orchitis. Among its related pathways are RET signaling and Signaling by GPCR. Gene Ontology (GO) annotations related to this gene include G protein-coupled receptor activity. An important paralog of this gene is F2R.
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.
GO ID | Qualified GO term | Evidence | PubMed IDs |
---|---|---|---|
GO:0001965 | G-protein alpha-subunit binding | IEA,ISS | -- |
GO:0004930 | G protein-coupled receptor activity | TAS,ISS | -- |
GO:0005102 | signaling receptor binding | TAS | 8615752 |
GO:0005515 | protein binding | IPI | 10725339 |
GO:0015057 | thrombin-activated receptor activity | IEA | -- |
GO ID | Qualified GO term | Evidence | PubMed IDs |
---|---|---|---|
GO:0005623 | cell | IEA | -- |
GO:0005769 | early endosome | IDA | 22547407 |
GO:0005794 | Golgi apparatus | TAS | 8615752 |
GO:0005886 | plasma membrane | TAS | -- |
GO:0005887 | integral component of plasma membrane | IDA | 17848177 |
SuperPathway | Contained pathways | ||
---|---|---|---|
1 | Peptide ligand-binding receptors | ||
2 | Signaling by GPCR | ||
3 | RET signaling | ||
4 | Angiogenesis (CST) | ||
5 | Cytoskeletal Signaling |
GO ID | Qualified GO term | Evidence | PubMed IDs |
---|---|---|---|
GO:0002286 | T cell activation involved in immune response | IEA,ISS | -- |
GO:0002376 | immune system process | IEA | -- |
GO:0002690 | positive regulation of leukocyte chemotaxis | IDA | 17991872 |
GO:0002720 | positive regulation of cytokine production involved in immune response | IDA | 11441110 |
GO:0002741 | positive regulation of cytokine secretion involved in immune response | IDA | -- |
Name | Status | Disease Links | Group | Role | Mechanism of Action | Clinical Trials |
---|---|---|---|---|---|---|
2-furoyl-LIGRLO-amide | Pharma | Agonist, Full agonist | 0 | |||
SLIGKV-NH2 | Pharma | PAR2 agonist, PAR2 receptor agonist | 0 | |||
SLIGRL-NH2 | Pharma | PAR2 activator, PAR2-activating peptide | 0 | |||
Thrombin Receptor Agonist Peptide | Pharma | Causes platelet aggregation and secretion | 0 | |||
2-furoyl-LIGRL[N-(Alexa Fluor 594)-O]-NH<sub>2 </sub> | Pharma | 0 |
Name | Synonyms | Role | CAS Number | PubChem IDs | PubMed IDs |
---|
Compound | Action | Cas Number |
---|---|---|
AY-NH2 | Selective PAR4 agonist | 352017-71-1 |
SLIGKV-NH2 | PAR2 receptor agonist | 190383-13-2 |
SLIGRL-NH2 | PAR2-activating peptide | 171436-38-7 |
TFLLR-NH2 | PAR1-activating peptide | 197794-83-5 |
Thrombin Receptor Agonist Peptide | Causes platelet aggregation and secretion | 137339-65-2 |
Compound | Action | Cas Number |
---|---|---|
2-Furoyl-LIGRLO-amide | 729589-58-6 | |
AC 264613 | PAR2 agonist,potent and selective | 1051487-82-1 |
AC 55541 | PAR2 agonist,potent and selective | 916170-19-9 |
LRGILS-NH2 | 245329-01-5 | |
SLIGKV-NH2 | PAR2 agonist | 190383-13-2 |
SLIGRL-NH2 | PAR2 activator | 171436-38-7 |
Thrombin Receptor Activator for Peptide 5 (TRAP-5) | 141685-53-2 | |
Thrombin Receptor Agonist Peptide | 137339-65-2 |
This gene was present in the common ancestor of chordates.
Organism | Taxonomy | Gene | Similarity | Type | Details |
---|---|---|---|---|---|
Chimpanzee (Pan troglodytes) |
Mammalia | F2RL1 30 31 |
|
OneToOne | |
Cow (Bos Taurus) |
Mammalia | F2RL1 30 31 |
|
OneToOne | |
Dog (Canis familiaris) |
Mammalia | F2RL1 30 31 |
|
OneToOne | |
Mouse (Mus musculus) |
Mammalia | F2rl1 30 17 31 |
|
OneToOne | |
Rat (Rattus norvegicus) |
Mammalia | F2rl1 30 |
|
||
Oppossum (Monodelphis domestica) |
Mammalia | F2RL1 31 |
|
OneToOne | |
Platypus (Ornithorhynchus anatinus) |
Mammalia | F2RL1 31 |
|
OneToOne | |
Chicken (Gallus gallus) |
Aves | F2RL1 30 31 |
|
OneToOne | |
Lizard (Anolis carolinensis) |
Reptilia | -- 31 |
|
ManyToMany | |
Tropical Clawed Frog (Silurana tropicalis) |
Amphibia | f2rl1 30 |
|
||
African clawed frog (Xenopus laevis) |
Amphibia | Xl.5507 30 |
|
||
Zebrafish (Danio rerio) |
Actinopterygii | f2rl1.2 30 31 |
|
OneToMany | |
f2rl1.1 31 |
|
OneToMany | |||
Rainbow Trout (Oncorhynchus mykiss) |
Actinopterygii | Omy.9406 30 |
|
Variant ID | Type | Subtype | PubMed ID |
---|---|---|---|
dgv5703n100 | CNV | gain | 25217958 |
dgv9885n54 | CNV | gain | 21841781 |
esv2763908 | CNV | gain | 21179565 |
esv3575858 | CNV | gain | 25503493 |
esv3605474 | CNV | gain | 21293372 |
esv994503 | CNV | deletion | 20482838 |
Disorder | Aliases | PubMed IDs |
---|---|---|
pulmonary vein stenosis |
|
|
granulomatous orchitis |
|
|
rhinitis |
|
|
orofacial granulomatosis |
|
|
gastroesophageal reflux |
|
|