Multidimensional GPCR profiling and screening using impedance-based label-free and real-time assay.

Area of Science:

• Pharmacology
• Biotechnology
• Cellular Biology

Background:

• G protein-coupled receptors (GPCRs) are key targets in drug discovery, implicated in numerous diseases.
• Approximately 40% of marketed drugs target GPCRs due to their diverse modulatory potential.
• GPCR signaling pathways are complex and context-dependent, requiring sophisticated assay methodologies.

Purpose of the Study:

• To describe an assay protocol for functional cell-based screening of GPCRs.
• To demonstrate the utility of the xCELLigence RTCA HT platform for GPCR screening.
• To address the need for integrating GPCR signaling complexity into functional assays.

Main Methods:

• Utilized the xCELLigence RTCA HT platform for impedance-based, real-time cell-based assays.
• Developed a functional assay protocol specifically for GPCR screening.
• Integrated the assessment of complex GPCR signaling pathways.

Main Results:

• The xCELLigence RTCA HT platform enables functional screening of GPCRs.
• The impedance-based assay effectively captures GPCR activity.
• The protocol facilitates the integration of complex signaling events in GPCR assays.

Conclusions:

• The described assay protocol provides a robust method for GPCR screening.
• The xCELLigence RTCA HT platform is suitable for high-throughput functional GPCR assays.
• This approach aids in the discovery of novel therapeutics targeting GPCRs.