GPCR Expression in Cell-Based Assays

Spending too much time and money creating stable cell lines for cell-based GPCR assays? Use transiently-transfected Assay Ready Cells to accelerate screening and drug discovery programs without stable cell line development.

Electroporation overcomes key challenges in GPCR assay development

G protein-coupled receptors are one of the most popular drug targets, accounting for at least a third of FDA-approved therapies. However, the complex structure of these proteins poses many challenges to basic scientists and early drug developers, especially when it comes to designing functional assays.

Electroporation helps overcome some of the most prevalent technical and biological barriers involved in GPCRs. MaxCyte’s ExPERT STx® with scalable Flow Electroporation® technology reproducibly transfects up to 1x1010 cells in less than 30 minutes, producing cells with high viability, transfection efficiency and membrane integrity. Transiently transfected cells can be used immediately or cryopreserved as Assay Ready Cells for future use.

Transiently transfected Assay Ready Cells cells produce quality results in functional GPCR assays such as cAMP and calcium flux assays. They also deliver comparable performance to stable cell lines, enabling assays to be developed and conducted in a fraction of the time.

Benefits of electroporation for GPCR expression

  • Develop GPCR assays in a day.
  • Express functional GPCRs with proven performance in cAMP, FLIPR® and other high-throughput assays.
  • Compatible with primary cells, stems cells or other difficult-to-transfect cell lines, electroporation enables you to use the most physiologically relevant cells.
  • Superior performance with reduced day-to-day assay variability.
  • Scalable electroporation transfects 75,000 cells in seconds up to 1x1010 cells in less than 30 minutes.
gpcr-expression-graphic

Proven performance in high-throughput screening

The development of stable cell lines can be a time-consuming bottleneck in early drug discovery. Bypassing the need to clone these cell lines, transiently transfected Assay Ready Cells can expedite your workflow while enhancing the consistency of your large-scale screenings.

β2 adrenergic receptor: cAMP assay performance comparable to a stable cell line

GPCR Activation — cAMP Assay graph

CHO K1 cells transiently transfected with DNA encoding a β2A receptor-eGFP fusion protein and stable CHO cells expressing an unmodified β2A receptor were stimulated with isoproterenol and assayed using a commercially available cAMP kit.

A range of cell-based assays for precise development

Our ExPERT team will provide you with the equipment and support you need for your specific application in assay development, running the gamut from high-content screening to mammalian display.