HUMAN RECOMBINANT GPR120 RECEPTOR
MULTISCREEN™ STABLE CELL LINES
1 vial (2 x 106) frozen cells
Sigma Freezing Medium (C-6164)
Expression vector containing full-length human GPR120 cDNA (GenBank Accession Number: BC101175.2) with FLAG tag sequence at N-terminus
Liquid nitrogen upon receiving
Propagation Medium: DMEF/12, 10% FBS, 10 μg/mL puromycin
Stable in culture for minimum of two months
Background: GPR120 is a G-protein coupled receptor and has been shown to stimulate secretion of gut hormones GLP-1 and cholecystokinin upon binding of long chain free fatty acids. Stimulation of GPR120 by FFAs results in elevation of Ca++ and activation of the ERK cascade which suggests interaction with the Gq family of G proteins. GPR120 is expressed in adipose tissue, proinflammatory macrophages and Kupffer cells . Stimulation of GPR120 with agonist causes broad anti-inflammatory effects in macrophages such as insulin sensitizing, antidiabetic effects and macrophage-induced tissue inflammation repression. Recent studies of the -3 FA treatment show inhibited inflammation and enhanced systemic insulin sensitivity in WT mice, but no effect in GPR120 knockout mice. This raises the possibility that targeting this receptor could have therapeutic potential in many inflammatory diseases including obesity and type 2 diabetes.
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. Receptor Expression on cell surface measured by flow cytometry (FACS) using an anti-FLAG antibody. Thin line: parental cells; thick line: receptor-expressing cells.
Fredriksson et al. (2003) Seven evolutionarily conserved human rhodopsin G protein-coupled receptors lacking close relatives. FEBS Lett 554:381-388.
Hirasawa et al. (2005) Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120. Nature Med 11:90-94.