GPBAR1
GPBAR1 (G protein-coupled bile acid receptor 1) is a cell surface G protein-coupled receptor that senses bile acids and signals through G(s) proteins to raise intracellular cAMP. It is also known as TGR5, BG37, M-BAR, GPCR19 and GPR131. Browse Assay Genie's current range of GPBAR1 research reagents below, or read on for the biology behind the target.
GPBAR1 is a G protein-coupled receptor for bile acids. Binding of a bile acid causes a conformational change that triggers signalling through guanine nucleotide-binding proteins and modulates downstream effectors such as adenylate cyclase. GPBAR1 is coupled to G(s) proteins and mediates activation of adenylate cyclase. It is activated by lithocholate, deoxycholate, chenodeoxycholate and cholate, in descending order of potency. In cells expressing the receptor, bile acid treatment induces intracellular cAMP production, activation of a MAP kinase signalling pathway and internalisation of the receptor.
Bile acids have roles in dietary lipid absorption and cholesterol catabolism. They also act as signalling molecules involved in energy expenditure and tissue inflammation, and GPBAR1 is one of the receptors through which they do so. In brown adipose tissue, GPBAR1 signalling activates adenylate cyclase, leading to DIO2 activation, which promotes energy expenditure and reduces adiposity. The receptor is also involved in bile acid-promoted GLP-1 secretion, and has been implicated in the suppression of macrophage functions and in the regulation of energy homeostasis.
The GPBAR1 gene encodes a member of the G protein-coupled receptor 1 family within the wider GPCR superfamily. Alternative splicing produces multiple transcript variants that encode the same protein. Mouse and rat both have a Gpbar1 ortholog, which makes rodent models a practical route for studying the receptor. Researchers looking for a GPBAR1 antibody, GPBAR1 ELISA kit or recombinant GPBAR1 protein will often work with it under the name TGR5.
GPBAR1 responds to bile acids in a defined order of potency, making it a model for studying how bile acids act as signalling molecules.
GPBAR1 signalling in brown adipose tissue activates adenylate cyclase and DIO2, promoting energy expenditure and reducing adiposity.
GPBAR1 is involved in bile acid-promoted GLP-1 secretion, linking bile acid sensing to metabolic regulation.
The receptor is implicated in suppressing macrophage functions, and bile acids influence tissue inflammation through signalling.
GPBAR1 is a cell surface receptor for bile acids. On activation it couples to G(s) proteins and stimulates adenylate cyclase, raising cAMP. Through this signalling it promotes energy expenditure in brown adipose tissue and contributes to bile acid-promoted GLP-1 secretion.
GPBAR1 is also called TGR5, BG37, M-BAR, GPCR19, GPR131, GPCR and MGC40597. The HGNC full name is G protein-coupled bile acid receptor 1. Alternative splicing gives several transcript variants, but they all encode the same protein.
Yes. Both mouse and rat have an ortholog named Gpbar1, so the receptor can be studied in rodent models. Check the datasheet of any product for its validated reactivity before using it with a given species.
Downstream effectors, incretin pathway components and metabolic signalling targets linked to bile acid receptor biology.
Gene and protein annotations from HGNC, NCBI Gene and UniProt Q8TDU6; product specifications from Assay Genie datasheets.