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Transfluor Cell-Based GPCR Assay

Detects compound activity against known and/or orphan GPCR targets in a high content screening environment

The Transfluor® Assay is a cell-based fluorescence assay used to screen for G-protein coupled receptor (GPCR) ligands and other potential drugs that regulate GPCRs by deactivating or desensitizing a common pathway. By attaching a fluorescent label to beta-arrestin, the location of the receptor-arrestin complex may be monitored during receptor activation. Since desensitization only occurs with an activated receptor, monitoring beta-arrestin translocation and subsequent receptor recycling provides a method to detect the activation of any GPCR.


Studying this mechanism enables researchers to identify the impact of GPCR ligands on a variety of physiological processes including behavior, mood, inflammation, nervous system, and olfactory responses. In addition, researchers can gain insight into the complexities of receptor degradation and recycling for a given target.

Features

  • Validated with over 100 GPCRs, the Transfluor assay provides the assurance to work across all GPCR classes (Class I, II, III), regardless of interacting G-protein (Gs, Gi/o and Gq/11).
  • Single read-out is compatible with all GPCR subtypes, including Gi, Gs, Go, Gq, eliminating the need for multiple GPCR assays
  • No GPCR labeling or tagging avoids custom molecular biology that may alter your target's response. 
  • Universal format requires no prior knowledge of interacting G-protein, enabling orphan GPCR screening. 
  • GFP-based technology does not require additional substrates to monitor beta-arrestin translocation.
  • MetaXpress® Application Module automates analysis of beta-arrestin movement to the cell membrane (pits) and endocytic vesicles.
  • Ligand Independent Translocation (LITe™) Assay is an agonist-independent assay used to verify the translocation of beta-arrestin-GFP in orphan GPCRs.