GPCR/ß-arrestin Signaling Pathway Assays

GPCR ß-arrestin LinkLight™ Assay

BioInvenu’s proprietary LinkLight™ technology offers innovative tools for cell based protein-protein interaction assays.

G-protein coupled receptors are involved in a wide variety of physiological processes. G protein-coupled receptors have a critical role in many diseases and are the targets of approximately 30% of all modern medicinal drugs. Upon activation, GPCRs initiate distinct G-protein signal pathways involving second messengers such as cAMP, diacylglycerol and calcium. Activated GPCRs also recruit signal adaptor protein ß-arrestins to its cytoplasmic tail and initiate the G-protein-independent signal pathway. ß-arrestins do not simply desensitize receptors, but also signal through multiple mediators such as MAPKs, SRC, NF-KB, and PI3K.

ß-arrestin signaling has become an important factor in identifying functionally selective or biased ligands for G-protein-coupled receptors. GPCR ß-arrestin LinkLight™ assay consists of two components: an inactive permuted luciferase containing a Tobacco Etch Virus (TEV) protease cleavage site fused to ß-arrestin-1 or ß-arrestin-2 and a GPCR fused to the TEV protease. Active luciferase is generated when permuted luciferase fused ß-arrestin-1 or ß-arrestin-2 is recruited to the receptor upon ligand activation. BioInvenu offers comprehensive ß-arrestin LinkLight™ assay-ready cells including transient expression GPCR ß-arrestin-1 or ß-arrestin-2 assay-ready cells and GPCR ß-arrestin-2 stable monoclonal cell lines.

GPCR ß-arrestin LinkLight™ assay cells can be used for G-protein signaling assays. Multiple GPCR ß-arrestin LinkLight™ assay cells have been demonstrated in cAMP, FLIPR, and Cre-Luc assays. The TEV tag on the C-terminal of GPCRs does not alter G-protein signaling.

Advantages of LinkLight™ Assay Technology

  • G-protein independent ß-arrestin signal readout.
  • G-protein signaling pathway is not alternated in GPCR ß-arrestin LinkLight™ assay cells. GPCR ß-arrestin LinkLight™ assay cells can be used for cAMP or Calcium mobilization assays.
  • Assessing & identifying GPCR biased or functional-selective ligands.
  • Assessing & identifying GPCR allosteric modulators.
  • Screening old targets for new chemical matters.

GPCR ß-arrestin LinkLight™ assays_presentation 2012.

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