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This gene encodes a member of the G protein-coupled receptor (GPCR) superfamily. This enzyme functions as a cell surface receptor for bile acids. Treatment of cells expressing this GPCR with bile acids induces the production of intracellular cAMP, activation of a MAP kinase signaling pathway, and internalization of the receptor. The receptor is implicated in the suppression of macrophage functions and regulation of energy homeostasis by bile acids. Alternative splicing results in multiple transcript variants encoding the same protein. [provided by RefSeq, Jul 2008]
GPBAR1 (G Protein-Coupled Bile Acid Receptor 1) is a Protein Coding gene. Diseases associated with GPBAR1 include Sclerosing Cholangitis and Intrahepatic Cholestasis Of Pregnancy. Among its related pathways are Signaling by GPCR and Peptide ligand-binding receptors. Gene Ontology (GO) annotations related to this gene include G protein-coupled receptor activity and G protein-coupled bile acid receptor activity.
GPBA receptors (TGR5, GPBAR1, M-BAR) are G protein-coupled receptors (GPCRs) that are activated by bile acids. They are highly expressed in the gallbladder, ileum and colon, and are important in the regulation of glucose and lipid metabolism, and energy utilization.
GO ID | Qualified GO term | Evidence | PubMed IDs |
---|---|---|---|
GO:0038181 | bile acid receptor activity | IDA | 12419312 |
GO:0038182 | G protein-coupled bile acid receptor activity | NAS | 12419312 |
GO ID | Qualified GO term | Evidence | PubMed IDs |
---|---|---|---|
GO:0005737 | cytoplasm | IDA | 12524422 |
GO:0005886 | plasma membrane | TAS | -- |
GO:0016020 | membrane | IEA | -- |
GO:0016021 | integral component of membrane | IEA | -- |
SuperPathway | Contained pathways | ||
---|---|---|---|
1 | Signaling by GPCR | ||
2 | Peptide ligand-binding receptors | ||
3 | G alpha (s) signalling events |
GO ID | Qualified GO term | Evidence | PubMed IDs |
---|---|---|---|
GO:0007165 | signal transduction | IEA | -- |
GO:0007186 | G protein-coupled receptor signaling pathway | TAS | -- |
GO:0038184 | cell surface bile acid receptor signaling pathway | IC | 12524422 |
GO:2000810 | regulation of bicellular tight junction assembly | IEA | -- |
Name | Status | Disease Links | Group | Role | Mechanism of Action | Clinical Trials |
---|---|---|---|---|---|---|
deoxycholic acid | Approved | Pharma | Antagonist, Full agonist, Agonist, Target | 47 | ||
chenodeoxycholic acid | Approved | Pharma | Antagonist, Full agonist, Agonist, Target | 41 | ||
cholic acid | Approved | Pharma | Full agonist, Agonist, Target | 0 | ||
cyclic amp | Experimental | Pharma | 0 | |||
Betulinic acid | Investigational | Pharma | Full agonist, Agonist | Anti-HIV and antitumor compound,pentacyclic triterpenoid | 1 |
Name | Synonyms | Role | CAS Number | PubChem IDs | PubMed IDs |
---|
Compound | Action | Cas Number |
---|---|---|
Betulinic acid | Anti-HIV and antitumor compound,pentacyclic triterpenoid | 472-15-1 |
GPBAR-A | agonist of bile acid receptor GPBAR1 | 877052-79-4 |
INT-777 | TGR5 receptor agonist, potent and selective | 1199796-29-6 |
TGR5 Receptor Agonist | TGR5 G-protein receptor agonist | 1197300-24-5 |
ExUns: | 1 | ^ | 2a | · | 2b | · | 2c | ^ | 3 | ^ | 4a | · | 4b | · | 4c |
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
SP1: | - | - | - | - | - | ||||||||||
SP2: | |||||||||||||||
SP3: | - | - | |||||||||||||
SP4: | - |
This gene was present in the common ancestor of chordates.
Organism | Taxonomy | Gene | Similarity | Type | Details |
---|---|---|---|---|---|
chimpanzee (Pan troglodytes) |
Mammalia | GPBAR1 33 32 |
|
OneToOne | |
cow (Bos Taurus) |
Mammalia | GPBAR1 33 32 |
|
OneToOne | |
dog (Canis familiaris) |
Mammalia | GPBAR1 33 32 |
|
OneToOne | |
mouse (Mus musculus) |
Mammalia | Gpbar1 17 33 32 |
|
||
rat (Rattus norvegicus) |
Mammalia | Gpbar1 32 |
|
||
oppossum (Monodelphis domestica) |
Mammalia | GPBAR1 33 |
|
OneToOne | |
lizard (Anolis carolinensis) |
Reptilia | GPBAR1 33 |
|
OneToOne | |
zebrafish (Danio rerio) |
Actinopterygii | GPBAR1 (2 of 2) 33 |
|
OneToMany | |
GPBAR1 (1 of 2) 33 |
|
OneToMany |
SNP ID | Clin | Chr 02 pos | Variation | AA Info | Type |
---|---|---|---|---|---|
rs138439621 | likely-benign, not specified | 218,263,182(+) | C/T | coding_sequence_variant, missense_variant | |
rs149245876 | likely-benign, not specified | 218,263,373(+) | G/C | coding_sequence_variant, missense_variant | |
rs150118963 | likely-benign, not specified | 218,263,360(+) | C/T | coding_sequence_variant, synonymous_variant | |
rs200857397 | likely-benign, not specified | 218,263,627(+) | G/A | coding_sequence_variant, synonymous_variant | |
rs767819043 | likely-benign, not specified | 218,262,880(+) | CTTCTTC/CTTC | coding_sequence_variant, inframe_deletion |
Disorder | Aliases | PubMed IDs |
---|---|---|
sclerosing cholangitis |
|
|
intrahepatic cholestasis of pregnancy |
|
|
ocular albinism |
|
|
cholangitis |
|
|
functional diarrhea |
|
|