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G protein-coupled receptor (GPCR)
Luciferase Reporter Cell Lines

G Protein-Coupled Receptors (GPCRs) form the largest and most diverse family of membrane receptors, playing pivotal roles in hormone signaling, metabolic regulation, and disease progression. To support GPCR-targeted drug discovery and pathway analysis -- particularly in the areas of diabetes and obesity, Signosis offers a collection of stable cell lines engineered to express functionally active GPCRs coupled with luciferase reporters.

 

Our portfolio includes cell lines expressing clinically relevant GPCRs such as GLP-1R, GIPR, and GCGR, key targets in glucose homeostasis and energy balance. These models are validated for ligand screening, cAMP signaling, and CREB pathway activation, offering sensitive and reproducible readouts for functional assays. 

Whether you're studying insulin signaling, incretin pathways, or metabolic hormone response, our GPCR cell lines provide a robust, ready-to-use solution to accelerate your research in obesity, type 2 diabetes, and related metabolic disorders.

Principle 

The GPCR Reporter Stable Cell Lines are engineered using a luciferase-based transcriptional reporter system to enable sensitive, real-time detection of G protein-coupled receptor (GPCR) signaling. These cell lines co-express a specific GPCR of interest along with a luciferase reporter gene driven by a response element responsive to cAMP-mediated downstream signaling pathways.

Upon ligand stimulation, GPCR activation triggers intracellular signaling cascades that lead to the transcriptional activation of the luciferase reporter gene. This system enables dynamic, dose-dependent measurement of receptor activity with low basal signal and a high signal-to-noise ratio. The stable cell lines were established through antibiotic selection and validated for consistent, ligand-specific luciferase induction.

These stable cell lines have been functionally validated using both peptide and non-peptide agonists, demonstrating broad compatibility with diverse ligand classes. This makes them a robust, reproducible platform for high-throughput screening of GPCR modulators, assessment of agonists and antagonists, and detailed pharmacological profiling. These models are ideal for applications in metabolic disease research, neurobiology, immunology, oncology, and beyond.

GPCR diagram.png

Ligand binding to GLP1R, GIPR, or the CTR-RAMP3 complex activates Gs-coupled signaling, leading to increased cAMP, PKA activation, and CREB phosphorylation. Phospho-CREB drives transcription of a CRE-luciferase reporter, producing light via firefly luciferase.

G protein-coupled receptor (GPCR)
Luciferase Reporter Cell Lines

Benefits

Isoform-Specific Detection

Designed to measure the activity of GPCR, avoiding cross-reactivity seen in traditional assays.

Consistent and Reliable

Stably integrated reporter constructs ensure reproducible performance without the need for repeated transfections.

Validated and Ready to Use

Each cell line is tested for correct receptor expression, ligand response, and antibiotic selection.

Improved Accuracy

Focuses on the receptor’s ligand-binding domain (LBD), not the shared DNA-binding region, for more precise results.

Broad Agonist Responsiveness

The cell line is functionally validated to respond to both peptide and non-peptide agonists.

Signosis Firefly Luciferase Substrate 

We offer a highly sensitive Firefly Luciferase Substrate, which can accurately measure firefly luciferase activity in cells.

Ligand-Responsive Readout

Uses the cAMP luciferase system to give a strong, measurable signal only when a ligand activates the receptor.

Mechanism-Focused Research

Helps researchers better understand how specific GIPR isoforms function in different pathways or diseases.

Fast and Easy Screening

Ideal for testing drugs or compounds that target GPCR receptors.

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