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. 

Figure: Standard curve of the GLP-1 receptor cell line for activation by GLP-1.  

 

 

 

 

 

 

 

 

 

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