HUMAN RECOMBINANT GLUCAGON RECEPTOR
MULTISCREEN™ STABLE CELL LINES
1 vial (2 x 106) frozen cells
Sigma Freezing Medium (C-6164)
Expression vector containing full-length human GCGR cDNA (GenBank Accession Number NM_000160) with FLAG tag sequence at N-terminus
Liquid nitrogen upon receiving
Propagation Medium: DMEM/F12, 10% FBS, 10 µg/mL puromycin
Background: The human glucagon receptor GCGR mediates the action of the pancreatic peptide hormone glucagon. Glucagon regulates blood glucose via control of hepatic glycogenolysis and gluconeogenesis and via regulation of insulin release from the β cell. Type 2 diabetes is characterized by inappropriate regulation of hepatic glucose production, which is due to an imbalance in the bihormonal relationship between plasma levels of glucagon and insulin. The glucose-lowering effects of glucagon peptide antagonists and anti-glucagon antibodies have demonstrated the potential of glucagon receptor antagonism as a treatment for type 2 diabetes. Glucagon also elicits various effects in extrahepatic tissues, including adipose tissue, kidney, heart, pancreatic β cells, gastrointestinal tract, thyroid and central nervous system.
Application: Functional assays
Figure 1. 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 2. Receptor expression on cell surface measured by flow cytometry (FACS) using an anti-FLAG antibody. Thin line: parental cells; gray line: receptor-expressing cells.
Lok et al. (1994) The human glucagon receptor encoding gene: structure, cDNA sequence and chromosomal localization. Gene 140:203-209.
Sloop et al. (2005) Glucagon as a target for the treatment of Type 2 diabetes. Expert Opin Ther Targets 9:593-600.