HUMAN RECOMBINANT GPR40 RECEPTOR
MULTISCREENTM β-ARRESTIN2 STABLE CELL LINE
1 vial (2 x 106) frozen cells
Expression vector containing full-length human GPR40 cDNA (GenBank Accession Number NM_005303) with FLAG tag sequence at N-terminus and ARRB2 cDNA (GenBank Accession Number NM_004313.3)
Liquid nitrogen upon receiving
Propagation Medium: DMEM-F12, 10% FBS, 10 µg/mL puromycin, 800 µg/mL G418
Stability: Stable after minimum of two months continuous growth
Background: G-protein coupled receptor 40 (GPR40 or FFA1) is specifically expressed in brain and pancreas. In pancreas, abundant GPR40 is localized to insulin-producing beta cells. Long-chain FFAs amplify glucose-stimulated insulin secretion from pancreatic beta cells by activating GPR40, indicating that GPR40 agonists and/or antagonists have potential for the development of new anti-diabetic drugs. GPR40 overexpression in breast cancer cells amplified oleate-induced proliferation, whereas silencing the GPR40 gene decreased it. These results suggest that GPR40 is implicated in the control of breast cancer cell growth by fatty acids and that GPR40 may provide a link between fat and cancer.
Application: Functional assays
Figure 1. Dose-dependent stimulation of calcium flux upon treatment with ligand, measured with MULTISCREENTM Calcium 1.0 No Wash Assay Kit (Multispan MSCA01). Figure 2. Dose-dependent stimulation from arrestin recruitment upon treatment with ligand, measured with MULTISCREENTM β-Arrestin Assay Kit (Multispan MSBA01). Figure 3. Receptor expression on cell surface measured by flow cytometry (FACS) using an anti-FLAG antibody. Thin line: parental cells; thick line: receptor-expressing cells.
Briscoe CP et al. (2003) The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids. J Biol Chem 278:11303-11311.
Steneberg P et al. (2005) The FFA receptor GPR40 links hyperinsulinemia, hepatic steatosis, and impaired glucose homeostasis in mouse. Cell Metab 1:245-258.
Hardy S et al. (2005) Oleate promotes the proliferation of breast cancer cells via the G protein-coupled receptor GPR40. J Biol Chem 280:13285-13291.