The Glucagon-like peptide-1 receptor (GLP-1R) is a receptor protein found on pancreatic cells and neurons in the brain. In humans, it is synthesized from the GLP1R gene located on chromosome 6. It is a member of the glucagon-like peptide receptor family in G protein-coupled receptors.Activated GLP-1R stimulates the adenylyl cyclase pathway, leading to increased insulin synthesis and release. As a result, GLP-1R has been a target for developing diabetes treatment drugs (commonly known as GLP1R agonists). GLP-1R is also expressed in the brain, involved in appetite control.GLP-1R is a multifunctional G protein-coupled receptor that recognizes specific ligands at the N-terminus and regulates cell pathways by coupling with various G proteins (Gαs, Gαi, Gαo, and Gαq/11). When bound to GLP-1, the G protein α subunit dissociates from the β, γ subunits, coupling with Gαs protein, activating adenylyl cyclase (cAMP), increasing cAMP levels in the cell, and raising protein kinase A (PKA) content to activate downstream signaling pathways, leading to increased insulin gene transcription.GLP1R Reporter HEK-293 Cell Line is a luciferase reporter cell line based on the cAMP-PKA signaling pathway. When GLP-1 binds to its receptor, the subunits dissociate, Gαs protein couples, activates adenylyl cyclase, increases cAMP levels in the cell, and raises PKA content. This activates downstream signaling pathways, ultimately leading to the expression of luciferase. Luciferase readout represents the activation effect of the signaling pathway, making it suitable for evaluating the in vitro effects of GLP1R-related drugs.
