GLP-1R/CRE Luciferase Reporter HEK293 Cell Line
GLP-1R/CRE Luciferase Reporter HEK293 Cell Line is an engineered HEK293 cell line expressing firefly luciferase under the control of cAMP response element (CRE), and human GLP-1R (Glucagon-like peptide 1 receptor; accession number BC113493). Activation of GLP-1R in these cells can be monitored by measuring luciferase activity.
The functionality of GLP-1R/CRE Luciferase Reporter HEK293 Cell Line was validated in dose-response assays using the peptide agonists Glucagon-like peptide 1 (7-37), Exendin-4, Lixisenatide, GLP-1 moiety from dulaglutide, Semaglutide, Tirzepatide and Retatrutide. This cell line has also been validated in a dose-response assay using a small molecule agonist, Danuglipron. GLP-1R/CRE Luciferase Reporter HEK293 Cell Line responds to agonists by inducing luciferase activity in a dose-dependent manner.
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Figure 1. Illustration of mechanism of action in the GLP-1R/CRE Luciferase Reporter HEK293 Cell Line.
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Media Required for Cell Culture
| Name | Ordering Information |
| Thaw Medium 1 | BPS Bioscience #60187 |
| Growth Medium 1A | BPS Bioscience #79528 |
Materials Required for Cellular Assay
| Name | Ordering Information |
| Bovine Serum Albumin (BSA, protease free) | Sigma #A4919 |
| Exendin-4 | MedChemExpress #HY-13443 |
| GIP | GenScript #RP10795 |
| GLP-1 (7-37) | R&D Systems #5374/1 |
| GLP-1, Fc-Fusion Recombinant (GLP-1 Agonist) | BPS Bioscience #102006 |
| Lixisenatide | Selleckchem #S8517 |
| Semaglutide | MedChemExpress #HY-114118 |
| Tirzepatide | MedChemExpress #HY-P1731B |
| Retatrutide | MedChemExpress #HY-P3506 |
| Danuglipron | Selleckchem #S9851 |
| Opti-MEM reduced serum medium (Assay Medium) | ThermoFisher #31985-070 |
| ONE-Step™ Luciferase Assay System | BPS Bioscience #60690 |
| Luminometer |
The cell line has been screened to confirm the absence of Mycoplasma species.
GLP-1R, a member of the class B family of G protein-coupled receptors (GPCRs or secretin-like receptors), is a transmembrane protein primarily found in pancreatic β cells and brain neurons and is activated by the peptide hormone glucagon-like peptide 1 (GLP-1) and glucagon that is secreted from intestinal L-cells after nutrient ingestion. GLP-1R plays an important role in controlling blood sugar level by enhancing glucose-stimulated insulin secretion, glucose, lipid metabolism, and satiety. Its role in the brain seems to be in the control of appetite.
Research efforts have focused on the regulation of the GLP-1R mediated signaling pathway as a therapeutic approach to type 2 diabetes (T2DM) and have resulted in the development of several GLP-1 FDA-approved agonists. In addition to their role in insulin secretion, GLP-1R agonists can also contribute to weight management, decrease the potential for cardiovascular diseases and protect beta cells. A role in tumor development in patients with T2DM is also being investigated but further studies are required to fully understand the functions of GLP-1R and its agonists.
Zhao X., et al., 2021 Front. Endocrinol. 12:721135.
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