HUMAN RECOMBINANT GLP-1 RECEPTOR
MULTISCREENTM β-ARRESTIN2 STABLE CELL LINE
1 vial (2 x 106) frozen cells
Expression vector containing full-length human GLP1R cDNA (GenBank Accession Number NM_002062) with FLAG tag sequence at N-terminus and ARRB2 cDNA (GenBank Accession Number NM_004313.3)
Liquid nitrogen upon receiving
Propagation Medium: DMEM, 10% FBS, 1 μg/mL puromycin, 250 μg/mL hygromycin
Stability: In progress
Background: Glucagon-like peptide-1 receptor (GLP1R) is a G protein-coupled receptor for the endogenous insulinotropic peptide glucagon-like peptide-1 (GLP-1). GLP1R is expressed in pancreatic cells and the nervous system, and mediate the effects of GLP-1 in regulating glucose homeostasis through multiple mechanisms including direct actions on the endocrine pancreas and indirect activation of central nervous system controlling gastric emptying, satiety, and body weight. In the brain, receptor activation elicits neurotrophic actions through protection against metabolic and oxidative insults. GLP1R is also implicated in plasticity, memory, and learning. Thus, GLP1R is a potential therapeutic target for both cognitive-enhancing and neuroprotective agents and in the treatment of stroke and Parkinsonism.
Application: Functional assays
Figure 1. Dose-dependent stimulation from arrestin recruitment upon treatment with ligand, measured with MULTISCREENTM β-Arrestin Assay Kit (Multispan MSBA01). Figure 2. Dose- dependent stimulation of calcium flux upon treatment with ligand, measured with MULTISCREENTM Calcium 1.0 No Wash Assay Kit (Multispan MSCA01). No G-Protein transiently transfected. Figure 3. Dose-dependent stimulation of intracellular cAMP accumulation upon treatment with ligand, measured with MULTISCREENTM TR-FRET cAMP 1.0 No Wash Assay Kit (Multispan MSCM01). Figure 4. Receptor expression on cell surface measured by flow cytometry (FACS) using an anti-FLAG antibody. Thin line: parental cells; thick line: receptor-expressing cells.
During et al. (2003) Glucagon-like peptide-1 receptor is involved in learning and neuroprotection. Nature Med 9:1173-1179.
Dillon et al. (1993) Cloning and functional expression of the human glucagon-like peptide-1 (GLP-1) receptor. Endocrinology 133:1907-1910.
Stoffel et al. (1993) Human glucagon-like peptide-1 receptor gene: localization to chromosome band 6p21 by fluorescence in situ hybridization and linkage of a highly polymorphic simple tandem repeat DNA polymorphism to other markers on chromosome 6. Diabetes 42:1215-1218.