HUMAN RECOMBINANT GPR142 RECEPTOR
MULTISCREEN™ STABLE CELL LINES
1 vial (2 x 106) frozen cells
Sigma Freezing Medium (C-6164)
Expression vector containing full-length human GPR142 cDNA (GenBank Accession Number NM_181790.1) with FLAG tag sequence at N-terminus
Liquid nitrogen upon receiving
Propagation Medium: DMEM, 10% FBS, 1 μg/mL puromycin
Background: GPR142 belongs to the family of class A (rhodopsin-like) orphan G protein-coupled receptors. Research has linked GPR142 to type 2 diabetes mellitus. GPR142 is reported to be highly expressed in pancreatic β-cells, and upon ligand binding and also in the presence of a high concentration of blood glucose, can stimulate insulin secretion. It has been hypothesized that GPR142 agonists can provide a benefit over existing type 2 diabetes therapies because of a greatly reduced risk of hypoglycemia.
Application: Functional assays
Figure 1. Dose response of intracellular IP1 accumulation upon treatment with ligand, measured with IP-one Tb kit (Cisbio 62IPAPEC). 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 R et al. (2003). “Seven evolutionarily conserved human rhodopsin G protein coupled receptors lacking close relatives”. FEBS Lett 554(3):381-8.
Lizarzaburu M et al. (2012). “Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus”. Bioorganic & Medicinal Chemistry Letters