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Related Experiment Video

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In-Cell Arrestin-Receptor Interaction Assays.

Chen Zheng1, Jonathan A Javitch2,3, Nevin A Lambert4

  • 1Department of Pharmacology, Vanderbilt University, Nashville, Tennessee.

Current Protocols
|October 3, 2023
PubMed
Summary

Developing novel drug screening assays is crucial for identifying biased ligands that target G protein-coupled receptors (GPCRs). These assays monitor arrestin recruitment, enabling the development of superior medications for various diseases.

Keywords:
G protein-coupled receptors (GPCRs)arrestinbioluminescence resonance energy transfer (BRET)

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Area of Science:

  • Pharmacology
  • Cell Biology
  • Biochemistry

Background:

  • G protein-coupled receptors (GPCRs) are key drug targets, mediating cellular responses through G protein and arrestin pathways.
  • Functionally selective ligands offer therapeutic advantages by preferentially activating specific signaling pathways.
  • Robust assays are needed to detect both G protein and arrestin activity for drug discovery.

Purpose of the Study:

  • To describe protocols for robust drug screening assays.
  • To monitor reversible arrestin recruitment to GPCRs in living cells.
  • To facilitate the identification of functionally selective ligands.

Main Methods:

  • Bioluminescence Resonance Energy Transfer (BRET) assays.
  • Nanoluciferase complementation (NanoLuc) assays.
  • Assays measuring arrestin recruitment to tagged GPCRs or arrestin translocation to the plasma membrane.

Main Results:

  • Protocols for BRET and NanoLuc assays to measure arrestin recruitment to GPCRs are detailed.
  • Methods for detecting arrestin translocation to the plasma membrane are presented.
  • These assays enable the study of dynamic GPCR-arrestin interactions.

Conclusions:

  • The described BRET and NanoLuc assays are powerful tools for studying GPCR-arrestin dynamics.
  • These assays are essential for identifying biased ligands with therapeutic potential.
  • The protocols support the development of novel drug screening strategies.