HUMAN RECOMBINANT GPR109A RECEPTOR
MULTISCREEN™ STABLE CELL LINES
1 vial (2 x 106) frozen cells
Sigma Freezing Medium (C-6164)
Expression vector containing full-length human GPR109A cDNA (GenBank accession number NM_177551.3) with FLAG tag sequence at N-terminus
Liquid nitrogen upon receiving
DMEM/F12, 10% FBS, 10 μg/mL puromycin
Stable in culture for minimum of two months
Background: GPR109A (HM74A, PUMA-G or niacin receptor 1) is a high-affinity receptor for nicotinic acid (niacin), and is highly expressed in adipocytes, lung, macrophages, dendritic cells, microglia and neutrophils. GPR109A in adipocytes is likely to be involved in niacin- mediated inhibition of lipolysis, reduction of serum free fatty acids and triglycerides as well as elevation of high density lipoproteins. GPR109A also serves important functions in the immune system. GPR109A on Langerhans cells in the skin also mediates niacin-induced cutaneous flushing, one of the major side effects of niacin, via the massive production of prostaglandins PGD2 and PGE2 in a ligand-dependent fashion.
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 inhibition of forskolin-stimulated intracellular cAMP level upon treatment with ligand, measured with MultiscreenTM TR-FRET cAMP 1.0 No Wash Assay Kit (Multispan MSCM01). 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.
Karpe and Frayn (2004) The nicotinic acid receptor-a new mechanism for an old drug. Lancet 363:1892-1894.
Tunaru et al. (2003) PUMA-G and HM74 are receptors for nicotinic acid and mediate its anti- lipolytic effect. Nature Med 9:352-355.
Wise et al. (2003) Molecular identification of high and low affinity receptors for nicotinic acid. J Biol Chem 278:9869-9874.