Cell-Based GPCR Reporter Assays

Cell-Based GPCR Reporter Assays

For Research Use Only. Not For Clinical Use.

G protein-coupled receptors (GPCRs), the largest superfamily of cell surface receptors, are comprised of an estimated 600-1,000 family members. As they play a key role in the regulation of many physiological processes, such as cell proliferation, metabolism, immunity, inflammation, and development, they have become the most popular therapeutic targets. However, the understanding of GPCR signaling regulation is still limited. Therefore, it is of great significance to identify the biological functions of GCPRs under physiological and pathological conditions for the discovery of novel drug targets.

Applications of Reporter Assays for Deciphering GPCR Pathways

The activation of GPCRs can induce the transcription of downstream genes by initiating a cascade of second messenger pathways. Various response elements located in the gene promoter region, including cAMP response element (CRE), nuclear factor of activated T-cells response element (NFAT-RE), serum response element (SRE) and serum response factor response element (SRF-RE), are involved in these processes.

Reporter assays provide an easy way to measure the activation of a specific signaling cascade of interests and a simple high throughput method for screening GPCR targets linked to second messenger pathways. The reporter genes commonly used include fluorescent proteins and various enzyme proteins, such as luciferases, alkaline phosphatase, β-galactosidase and β-lactamase. Among them, luciferases are widely used because of inherent sensitivity, broad dynamic range, no endogenous activity and low interference. Specific reporter systems can be used to study the ligand activity at Gαi/o, Gαs and Gαq G protein-coupled receptors.

Cell-Based GPCR Reporter AssaysFigure 1. Schematic diagram showing major GPCR signaling pathways. (Cheng Z, et al., 2010)

Our Cell-Based GPCR Reporter Assays

We provide a number of cell-based GPCR reporter systems for different applications. We have also developed reporter assays for live cell imaging.

Choose a promoter Choose a reporter Choose an application
  • cAMP response element promoter (CRE)
  • Nuclear factor of activated T cells promoter (NFAT)
  • c-fos promoter
  • AP-1 promoter
  • Serum response element promoter (SRE)
  • Gal4 upstream activating sequence
  • Luciferase reporter system
  • Secreted placental alkaline phosphatase (SPAP)
  • Green-fluorescent protein (GFP)
  • β-Lactamase reporter system
  • β-galactosidase reporter system
  • Dual-reporter system
  • Study of constitutively active GPCRs
  • Identification of second messenger pathways
  • Evaluation of cross-talk between receptors and pathways
  • Identification of orphan receptors and ligands
  • Pharmacological studies in living cells
  • High-throughput drug screening

Creative Biolabs has an experienced team of GPCR biologists who have developed a series of highly validated GPCR cell related products and cell-based assay kits for your choice to enable your research and drug discovery programs.

If you are interested in our cell-based reporter assays or have any specific needs, please feel free to contact us for more details.


  1. Cheng Z, et al. Luciferase reporter assay system for deciphering GPCR pathways. Current chemical genomics, 2010, 4: 84.
  2. Hill S J, et al. Reporter-gene systems for the study of G protein-coupled receptors. Current opinion in pharmacology, 2001, 1(5): 526-532.
  3. Kunapuli P, et al. Development of an intact cell reporter gene β-lactamase assay for G protein-coupled receptors for high-throughput screening. Analytical biochemistry, 2003, 314(1): 16-29.