GPBAR1 (G Protein-Coupled Bile Acid Receptor 1)
A bile acid receptor involved in metabolic regulation, inflammation, and cancer.
Gene Information Card
| Symbol | GPBAR1 |
|---|---|
| Full Name | G protein-coupled bile acid receptor 1 |
| Gene Type | protein-coding |
| Chromosomal Location | 2q35 |
| NCBI Gene ID | 151306 ncbi.nlm.nih.gov/gene/151306 |
| Ensembl ID | ENSG00000164821 |
| UniProt ID | Q8TDU6 |
| OMIM ID | 610171 |
| HGNC ID | 24822 |
| Aliases | TGR5, M-BAR, BG37, GPCR19, hGPCR1 |
Description
GPBAR1 (also known as TGR5) encodes a G protein-coupled receptor that is activated by bile acids. It plays a key role in energy homeostasis, glucose metabolism, and inflammatory responses. The receptor is expressed in various tissues including the gallbladder, intestine, liver, and immune cells. GPBAR1 signaling is implicated in metabolic disorders, inflammatory diseases, and certain cancers.
Disease Associations
| Disease category | Pathophysiological mechanism | Genomic evidence |
|---|---|---|
| Type 2 diabetes | GPBAR1 activation improves insulin sensitivity and glucose tolerance via GLP-1 secretion. | PMID: 19252484 |
| Non-alcoholic fatty liver disease (NAFLD) | Receptor activation reduces hepatic steatosis and inflammation. | PMID: 23907406 |
| Inflammatory bowel disease | GPBAR1 signaling attenuates intestinal inflammation through NF-κB inhibition. | PMID: 21734026 |
| Gallbladder cancer | Overexpression of GPBAR1 promotes cell proliferation and migration. | PMID: 28122329 |
| Cholestasis | Bile acid-mediated GPBAR1 activation regulates bile acid homeostasis. | PMID: 23907406 |
Expression Profile
Tissue Expression
| Tissue | nTPM | level |
|---|---|---|
| Gallbladder | 12.5 | High |
| Small intestine | 8.3 | Medium |
| Liver | 4.1 | Low |
| Colon | 6.7 | Medium |
| Spleen | 3.2 | Low |
Cell Line Expression
| Cell Line | nTPM | Notes |
|---|---|---|
| HepG2 | 5.1 | Hepatocellular carcinoma cell line |
| Caco-2 | 7.8 | Colorectal adenocarcinoma cell line |
| THP-1 | 4.5 | Monocytic leukemia cell line |
| LNCaP | 2.3 | Prostate cancer cell line |
Data source：Human Protein Atlas（proteinatlas.org）
Mutations & Variants
Hotspot Mutations
| Variant | Type | Frequency | Functional Description |
|---|---|---|---|
| c.1A>G (p.Met1?) | missense | <0.01% | Likely loss of function; initiation codon disrupted |
| c.100C>T (p.Arg34Trp) | missense | <0.01% | Unknown; rare variant in population databases |
Mutation functional classification
Loss of Function (LOF)
c.1A>G (p.Met1?) is predicted to abolish protein translation.
Gain of Function (GOF)
No confirmed gain-of-function mutations reported.
Dominant Negative (DN)
No dominant-negative mutations reported.
View complete mutation data：
Gene Ontology (GO)
| • G protein-coupled receptor activity (GO:0004930) | • bile acid receptor activity (GO:0038181) |
| • positive regulation of cAMP-mediated signaling (GO:0060122) | • negative regulation of inflammatory response (GO:0050728) |
| • positive regulation of insulin secretion (GO:0032024) |
Pathways
• Bile acid signaling via GPBAR1 (Reactome: R-HSA-159418)
• GPCR downstream signaling (Reactome: R-HSA-388396)
Protein Summary
GPBAR1 is a 330-amino acid transmembrane protein belonging to the class A rhodopsin-like GPCR family. It is activated by secondary bile acids such as lithocholic acid and deoxycholic acid. Upon activation, it couples primarily to Gαs, leading to increased intracellular cAMP and downstream signaling that modulates energy expenditure, glucose homeostasis, and immune responses. The protein is localized to the plasma membrane and is expressed in multiple tissues, with highest levels in the gallbladder and intestine.
Related Services
Related Products
| Product name | Cat.No. | Species | Gene ID | |
|---|---|---|---|---|
| GPBAR1 Knockout HEK293 Cell Line | EDJ-KQ1057 | Human | 151306 | Details Get a Quote |
| GPBAR1 Knockout HeLa Cell Line | EDJ-KQ58686 | Human | 151306 | Details Get a Quote |
| GPBAR1 Knockout A-549 Cell Line | EDJ-KQ67169 | Human | 151306 | Details Get a Quote |
| GPBAR1 Knockout HCT 116 Cell Line | EDJ-KQ75571 | Human | 151306 | Details Get a Quote |
| GPBAR1 Knockout SK-N-AS Cell Line | EDC07743 | Human | 151306 | Details Get a Quote |
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