background:

Glucagon-like peptide-1 receptor (GLP-1R) is a G protein-coupled receptor expressed on the surface of pancreatic β cells. Activated GLP-1R triggers the production of cAMP by stimulating the adenylate cyclase pathway, and activates downstream gene expression through the cAMP response element (CRE), thereby promoting the synthesis and release of insulin (Figure 1). GLP-1R is ^[1] .

Figure 1. GLP-1R signaling pathway ^[2]

Rhinogen ^® GLP-1R Reporter Bioassay is a bioluminescent reporter gene assay whose mechanism of action (Figure 2) is based on the cAMP/PKA signaling pathway, the main signaling pathway of the GLP-1R response, and can be used for high-throughput screening of therapeutic drugs for diabetes. This system uses engineered Chinese hamster ovary cells (CHO cells) as test cells, which stably express GLP-1R and firefly luciferase driven by the CRE response element. In this cell, activation of GLP-1R triggers the production of cAMP, which in turn activates the expression of the luciferase gene, and the activity of luciferase is quantified by bioluminescence.

Figure 2. Schematic diagram of
Rhinogen ^® GLP-1R Reporter Bioassay

Specifications:

Features:

Rhinogen ^® GLP-1R reporter gene detection system has the characteristics of simple operation (Figure 3), low variability and high sensitivity.

1. The principle is clear: based on the main signaling pathway of GLP-1R response, cAMP/PKA signaling pathway;

2. High throughput : High-throughput screening of GLP-1R agonists or antagonists, screening of GLP-1 analogs, and high-throughput drug testing can be performed in 96-well and 384-well culture plates ;

3. Fast and easy to use: The detection process is simple (Figure 3) and the detection reagents are easy to use;

4. High signal-to-noise ratio: The signal/background ratio is high.

Rhinogen ^® GLP-1R reporter gene detection system make it an effective means of screening and testing GLP-1R drugs. At the same time, this method can be used as a routine detection method for the biological activity of GLP-1R drugs and a batch release detection indicator.