GLP1R binds specifically the glucagon-like peptide-1 (GLP1) and has much lower affinity for related peptides such as the gastric inhibitory polypeptide and glucagon. GLP1R is known to be expressed in pancreatic beta

cells. Activated GLP1R stimulates the adenylyl cyclase pathway which results in increased insulin synthesis

and release of insulin.  Consequently, GLP1R has been suggested as a potential target for the treatment of

diabetes. GLP1R is also expressed in the brain where it is involved in the control of appetite. Furthermore, mice

which over express GLP1R display improved memory and learning.

HEK293

GLP-1

Functional assay for GLP1R receptor

Figure 1. GLP-1 (7-37)-induced concentration-dependent stimulation of intracellular luciferase in HEK293/GLP1R/Luc and HEK293 cells.

After stimulation with GLP1 receptor agonist, GLP-1 (7-37), the cells are checked with BrightGlo™Luciferase Assay System and the relative luminescence units (RLU) of

luciferase were recorded on a FlexStation. The RLU were plotted against the log of the cumulative doses (10 -fold dilution) of GLP-1 (7-37) (Mean ± SD, n = 2). The EC50 of GLP-1 (7-37) co-expressing with Luc

in HEK293 cells was 4.91 nM.