Bile Acid GPCR Family Subtypes and Products

What Are Bile Acid Receptors?

Bile acids are steroid acids synthesized within the liver, making up roughly 80% of the components of bile. The principal bile acids in humans are comprised of two subsets of bile acids, primary and secondary. Primary bile acids include cholic and chenodeoxycholic acid, and secondary bile acids include deoxycholic and lithocholic acid. The primary function of these bile acids is the digestion of fats and oils. G protein-coupled bile acid receptor (GPBA) agonists can help stimulate GLP-1 secretion, aiding in the treatment of obesity and increasing glucose homeostasis.

Bile Acid Receptor Information

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GPBA is a G-protein coupled receptor, also known as TGR5 or GPR131. Stimulation of the receptor with bile acids or other ligands induces the production of intracellular cAMP, activation of a MAP kinase signaling pathway and internalization of the receptor. Quantitative analyses for TGR5 mRNA have shown that it is abundantly expressed in monocytes/macrophages. The receptor is an attractive therapeutic target for the prevention and treatment of obesity and is highly associated with Type II diabetes and metabolic syndrome. GPBA has been implicated in inflammatory diseases, regulation of homeostasis by bile acids, as well as cardiovascular, neurological, and hepatic diseases.

Bile Acid Cell Lines

Receptor FamilyReceptorSpeciesParentalStable Cell Lines Division-Arrested Cells Membranes
Bile AcidGPBAhumanCHO-K1C1361-1DC1361-1MC1361-1
GPBA Mutant W83GhumanCHO-K1C1361-1MT1DC1361-1MT1MC1361-1MT1
GPBA Mutant W83AhumanCHO-K1C1361-1MT2DC1361-1MT2MC1361-1MT2
GPBA Mutant V88LhumanCHO-K1C1361-1MT3DC1361-1MT3MC1361-1MT3
GPBA Mutant Y89AhumanCHO-K1C1361-1MT4DC1361-1MT4MC1361-1MT4
GPBA Mutant Y89HhumanCHO-K1C1361-1MT5DC1361-1MT5MC1361-1MT5
GPBA Mutant F96AhumanCHO-K1C1361-1MT6DC1361-1MT6MC1361-1MT6
GPBA Mutant W237AhumanCHO-K1C1361-1MT7DC1361-1MT7MC1361-1MT7
GPBA Mutant W240AhumanCHO-K1C1361-1MT8DC1361-1MT8MC1361-1MT8