Key Features:
High Sensitivity: The cell line offers high signal-to-background with over 500-fold induction, ensuring accurate and reproducible results in CREB pathway studies.
Sensitive and Quantitative: The luciferase reporter provides a direct and reliable readout of CREB activation, enabling precise measurement of pathway activity.
Mutation-Specific Applications: This cell line expresses GLP-1R with serine (S) and threonine (T) residues in the C-terminal tail mutated to alanine (A), preventing phosphorylation at these key regulatory sites. The S/T→A mutation in the receptor’s C-tail disrupts normal phosphorylation-dependent processes like receptor desensitization, internalization, and arrestin recruitment, enabling detailed study of these pathways. 
Stable Integration: Established via co-transfection with GLP1R and CRE-luciferase constructs, followed by antibiotic selection and functional screening withDanuglipron and Exendin-4.
 
The GLP-1R(C-tail S/T→A)/CREB Luciferase Reporter HEK293 Stable Cell Line is derived from human embryonic kidney cells and stably expresses glucagon-like peptide-1 receptor (GLP-1R) where key serine and threonine residues in the receptor’s C-terminal tail are mutated to alanine, alongside a firefly luciferase reporter gene under the control of the cAMP response element-binding protein (CREB) response element. 

GLP-1R is a G protein-coupled receptor (GPCR) that normally signals via cAMP/PKA and activates CREB. Phosphorylation of the C-tail normally regulates homologous desensitization and receptor internalization by controlling interactions with signaling and trafficking proteins such as arrestins. This S/T→A mutant receptor allows exploration of signaling alterations when these phosphorylation events are blocked, with resulting CREB activation monitored via luciferase expression.

This cell line is ideal for studying the functional impact of the GLP1R (C-tail S/T→A) variant on signaling, screening for GPCR modulators, and investigating cAMP/PKA/CREB pathway dynamics. It is particularly useful for drug discovery programs targeting metabolic diseases, including type 2 diabetes and obesity.
 
This versatile cell line serves as a powerful in vitro tool for both basic research and translational applications in endocrinology, pharmacology, and metabolic disease research.