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Unique Properties of PathHunter® β-Arrestin Assays for GPCR Antagonist Discovery and Characterization

Unique Properties of PathHunter® β-Arrestin Assays for GPCR Antagonist Discovery and Characterization
Version:
SBSP_0410

File Name/Number:
SBS 2010

Year:
2010

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A common feature of 7TM receptors is that upon activation, the receptors are bound by cellular Arrestin proteins. DiscoveRx has pioneered the PathHunter® β-Arrestin assay platform for monitoring these events using enzyme fragment complementation (EFC) and applied this technique to develop assays for more than 170 human GPCR targets. Unlike second messenger assays that are amplified through downstream signaling events, each arrestin protein binds to a single activated GPCR. The PathHunter® Arrestin assay is unique among arrestin assays in that it preserves the one-to-one nature of arrestin binding and directly translates the binding events to signal generation. This eliminates the receptor reserve effect and enables the interrogation of all available receptors. The work presented here focuses on how this property of the PathHunter® Arrestin platform makes it ideal for the discovery and characterization of GPCR antagonists.