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G-Protein Coupled Receptor (GPCR) Screening Assays

The seven-transmembrane α-helix structure of a GPCR

G-protein-coupled receptors (GPCRs) draw much attention as drug targets because more than 40% of the approximately 500 clinically marketed drugs are targeting GPCRs. Functional assays for GPCRs are indispensable platforms for drug screening and ligand hunting. We provide assay systems which cover calcium flux, cAMP level and reporter assay for our customers to carry out high-throughput screening (HTS).

Four major routes of the GPCR Signaling Pathway

GPCRs transmit extracellular signals across the plasma membrane via intracellular coupling with heterotrimeric G proteins. Heterotrimeric G proteins are classified into four subfamilies based on their Gα subunits, Gs, Gi, Gq and G12. Current methods employed in GPCR screening assays measure G protein signaling by determining change in second messengers such as cAMP, inositol trisphosphate (IP3), and intracellular Ca2+ mobilizations, which demands different assay platforms and requires specialized instrumentation for each pathway which could be costly. Our proprietary GPCR assay platform is designed to report GPCR activation. These assays are used for potency rankings of GPCR modulators and for high throughput screening. The advantage of our GPCR screening assays is that they give you a cost-effective screening approach before you spend time and resource to narrow down individual GPCRs before you are not sure which subtypes of GPCRs are involved.

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