The application of EFC technology to study forward trafficking of GPCRs

Version:: 2012
Year:: 2012

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DiscoveRx has pioneered a novel enzyme complementation system to monitor cellular events such as protein translocation, protein interactions, and degradation in an HTS friendly, cell-based format. This unique technology provide a basis for the generation of novel cellular assays for intractable targets, and simplify the detection of cellular signaling events using a simple one-step chemiluminescent protocol. We have recently applied this technology to monitoring receptor trafficking along biosynthetic routes, in response to pharmacochaperone activity, as well as internalization in response to agonist activation. In this work, these tools were applied to defining pharmacochaperone activity on a mutant B2AR as a proof-of-principle for the detection of molecules that would facilitate folding and trafficking of receptors to the cell surface.