HUMAN RECOMBINANT GPBA MUTANT 4 RECEPTOR
MULTISCREEN™ STABLE CELL LINES
Mutant Clone Number:
1 vial (2 x 106) frozen cells
Sigma Freezing Medium (C-6164)
Expression vector containing full-length human GPBAR1 cDNA with Y89A mutation (GenBank Accession Number NM_170699) with FLAG tag sequence at N- terminus
Liquid nitrogen upon receiving
Propagation Medium: DMEM/F12, 10% FBS, 10 μg/mL puromycin
Background: 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.
Application: Functional assays
Figure 1. Dose-dependent increase of intracellular cAMP upon treatment with ligand, measured with cAMP HiRange kit (Cisbio 62AM6PEC). Figure 2. Receptor expression on cell surface measured by flow cytometry (FACS) using an anti-FLAG antibody. Thin line: parental cells; thick line: receptor- expressing cells.
Maruyama et al. (2002) Identification of membrane-type receptor for bile acids (M-BAR). Biochem Biophys Res Commun 298:714-719.
Katsuma et al. (2005) Bile acids promote glucagon-like peptide-1secretion through TGR5 in a murine enteroendocrine cell line STC-1. Biochem Biophys Res Commun 329:386-390.