Diabetes/Obesity Therapeutics

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GLP-1 AND GIP REPORTER CELL LINES Drug Development Bioassays for Diabetes and Obesity Therapeutics ADVANTAGES More sensitive than other available GIP or GLP-1 receptor expressing cell lines Contains a luciferase reporter to facilitate high-throughput drug screening Bioassay results in one day TECHNOLOGY DETAILS Researchers at the University of British Columbia have developed cell lines expressing the glucose-dependent insulintropic polypeptide (GIP) or glucagon-like peptide-1 (GLP-1) receptors, for diabetes and obesity research.  GIP is a gut hormone with obesity-promoting activities, and a promising drug target for obesity.  GLP-1 is a gut hormone with the ability to lower glucose levels, thus making it of great interest in developing diabetes therapies.  In the cell lines, the activation of the GLP-1 or GIP receptor leads to cAMP production and luciferase gene expression, enabling a bioassay of the activity of compounds targeting these receptors. These cell lines are more sensitive than other available GIP or GLP-1 cell lines.  As shown in the figure below, the GLP-1 receptor cell line can detect picomolar concentrations of activation compounds, such as GLP-1 peptides.  Moreover, the GLP-1 cell line is well suited to compound screening because it has been shown to also detect activity of modified GLP-1 peptides and small molecule compounds.  The cell lines can be used for drug development for diabetes and obesity disorders. The cell line background is human embryonic kidney 293 (HEK293) cells.  The cell lines contain a luciferase reporter vector (pHTS-CRE) made by Biomyx, Inc. in California to enable high-throughput screening. Three cell lines are available: Human GLP-1 Receptor CRE-Luciferase: suitable for screening compounds that activate or antagonize the GLP-1 receptor Human GIP Receptor CRE-Luciferase: suitable for screening compounds that activate or antagonize the GIP receptor CRE-Luciferase: suitable for use as control line for false positives