GLP1R Functional Cell-based Agonist Assay for compound screening and profiling via cAMP release measured by FRET technology.
GLP1R is the receptor for glucagon-like peptide-1 (GLP-1), an incretin hormone released postprandially from intestinal L-cells. Upon activation by GLP-1, GLP1R stimulates adenylate cyclase, increasing intracellular cAMP levels. This leads to enhanced glucose-dependent insulin secretion, suppressed glucagon release, delayed gastric emptying, and increased satiety. These effects contribute to glycemic control and weight regulation. Therapeutic ligands such as Liraglutide or Semaglutide are pharmaceutically developed to treat type 2 diabetes mellitus and obesity.
GLP1R
Glucagon-like peptide 1 receptor
HEK293
Transfected
HEK293 cells were transduced with a human Glucagon-like peptide 1 receptor (GLP1R). Stimulation of these cells with Liraglutide, an artificial long-acting GLP-1 analog, results in agonistic activation of cAMP release, which can be measured by FRET technology, resulting in signal reduction upon cAMP release. The assay has been validated based on flow detection of target expression on cells and response to known GLP1R agonists.
Induction of cAMP release
| Compound | EC50 |
|---|---|
| Liraglutide | 3.95 pM |
Freiburg
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Reference compound activation of GLP1R
Liraglutide is known to specifically activate the cAMP response as agonist of glucagon-like peptide-1 receptor (GLP1R). cAMP levels were measured by FRET technology. The agonist was included for the validation process and the cellular GLP1R assay generating highly reproducible EC50 values. The graph shows a representative result.