RECOMBINANT RAT GPR40 RECEPTOR
MULTISCREEN™ MEMBRANE PREPARATION
1 vial (21.85 mg/mL, 1 mg)
20 mM Gly-Gly, 1 mM MgCl2, 25 mM Sucrose (pH 7.2)
Expression vector containing full-length rat GPR40 cDNA (GenBank Accession Number NM_153304) with FLAG tag sequence at N-terminus
Store at – 80°C. Avoid repeated freeze-thaw.
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.
Figure 1. Histogram showing 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.