Key Features:
High Sensitivity: The cell line offers high signal-to-background with over 100-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: Co-expression of the GIPR E354Q mutant and a CREB-responsive luciferase reporter facilitates the study of how this variant affects receptor signaling and ligand responses. Suitable for compound screening and dose-response studies targeting the mutant receptor.
Stable Integration: Established via co-transfection with GIPR and CRE-luciferase constructs, followed by antibiotic selection and functional screening with Tirzepatide.
 
The GIPR (E354Q)/CREB Luciferase Reporter HEK293 Stable Cell Line is derived from human embryonic kidney cells and stably expresses Gastric Inhibitory Polypeptide Receptor carrying the E354Q point mutation alongside a firefly luciferase reporter gene under the control of the cAMP response element-binding protein (CREB) response element. This dual-expression cell line is an ideal tool for monitoring the intracellular signaling events triggered by GIPR activation.

GIPR is a G protein-coupled receptor (GPCR) primarily coupled to the G proteins, leading to increased intracellular cAMP and subsequent activation of PKA and downstream effectors like CREB.  The E354Q mutation, located in the receptor’s transmembrane region, has been shown to modify ligand binding or receptor signaling properties. Activation of CREB results in luciferase expression, offering a convenient and quantitative readout of pathway activation.

This cell line is ideal for studying the functional impact of the GIPR E354Q variant, 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.