GLP-2R/CRE Luciferase Reporter HEK293 Cell Line

The GLP-2R/CRE Luciferase Reporter HEK293 Cell Line is a HEK293 cell line engineered to express Glucagon-like peptide 2 receptor (GLP-2R) (NM_004246.3). The construct was delivered by lentiviral transduction of CRE/CREB Luciferase Reporter HEK293 Cell Line (#60515), which express a firefly luciferase reporter driven by cAMP response elements (CRE). After activation by GLP-2, the endogenous transcription factor CREB binds to the response elements, inducing transcription of the luciferase reporter gene. This cell line has been validated to respond to GLP-2, Tirzepatide, Dapiglutide, and Teduglutide. Figure 1. Illustration of mechanism of action in the GLP-2R/CRE Luciferase Reporter HEK293 Cell Line. Glucagon-Like Peptide-2 Receptor (GLP-2R), a member of the class B G protein-coupled receptors (GPCRs), is a transmembrane protein predominately expressed in the pancreas, gut, and brain. GLP-2R is activated by the peptide hormone glucagon-like peptide 2 (GLP-2), which is rapidly secreted from endocrine L cells in response to nutrient absorption. GLP-2R plays an important role in gut health by triggering epithelial cell proliferation in the small and large intestines and suppressing apoptosis. As a result, both intestinal crypts and villi increase in size, leading to an overall expansion of the absorbative surface area in the intestines. Therapeutic strategies targeting the GLP-2 receptor are under investigation, predominantly centered on the development of long-acting receptor agonists. GLP-2 analog Teduglutide is an FDA approved injectable for the treatment of short bowel syndrome (SBS). Teduglutide reduces the need for intravenous feeding in patients with SBS by promoting intestinal cell growth and aiding in the absorption of nutrients and fluids. Other therapies include Dapiglutide, a unique dual GLP-1/GLP-2 receptor agonist that is currently in clinical trials for the treatment of obesity and associated intestinal inflammation.