HTS238L - ChemiBrite™ GPBA Bile Acid Receptor Stable Cell Line

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    The bile acid lithocolic acid acts as an agonist on the GPBA GPCR, also known as GPR131 or TGR5, to increase intracellular cAMP in cells that express the receptor (Maruyama et al., 2002). Bile acids and other GPBA ligands increase glucagon-like peptide-1 (GLP-1) secretion from intestinal cells. Although Type II diabetics have impaired ability to secrete GLP-1, their responsiveness to this compound, which enhances the effects of insulin, is normal. Thus GPBA agonists are of interest in developing therapeutics for diabetes. Interestingly, it has been suggested that the anti-diabetic effect of olive leaves could in part be mediated by agonist activity at GPBA receptors by oleanolic acid (Sato et al. 2007). Eurofins' cloned human GPBA receptor-expressing ChemiBrite cells are made by stable transfection of HEK293 cells with ChemiBrite clytin, receptor and clytin and a promiscuous G protein to couple the receptor to the calcium signaling pathway. These stability-tested cells are ready for luminescent analysis of agonists, antagonists and modulators at the GPBA receptor.

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    Item Unit of Measure: PK
    Contents: 2 vials of mycoplasma-free cells, 1 ml per vial.
    Storage: Vials are to be stored in liquid N2.
    Applications: Calcium Flux Assay, cAMP Accumulation
    Entrez Gene Number: NM_170699
    Host Cell: HEK293
    Exogenous Gene Expression: GPBAR1 cDNA (Accession Number: NM_170699; see CODING SEQUENCE below) and a proprietary mutant clytin photoprotein, and promiscuous G protein each expressed in a bicistronic vector
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Maruyama et al. (2002) Identification of membrane-type receptor for bile acids (M-BAR). Biochem Biophys Res Commun 298:714-719
    Reference 2: 2. Sato et al. (2007) Anti-hyperglycemic activity of a TGR5 agonist isolated from Olea europaea. Biochem Biophys Res Commun 362:793-798