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Related Experiment Video

Updated: Apr 18, 2026

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Label-free biosensor assays in GPCR screening.

Manuel Grundmann1, Evi Kostenis

  • 1Institute for Pharmaceutical Biology, University of Bonn, Nussallee 6, 53115, Bonn, Germany, grundmann@uni-bonn.de.

Methods in Molecular Biology (Clifton, N.J.)
|January 8, 2015
PubMed
Summary

Dynamic mass redistribution (DMR) assays offer a holistic approach to studying G protein-coupled receptors (GPCRs), providing insights beyond traditional methods. This guide details DMR assay optimization for investigating GPCR signaling in living cells.

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BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells

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Area of Science:

  • Pharmacology and Molecular Biology
  • Cellular Signaling and Drug Discovery

Background:

  • G protein-coupled receptors (GPCRs) are crucial transmembrane proteins targeted by approximately one-third of marketed drugs, playing vital roles in numerous physiological and pathophysiological processes.
  • Traditional biochemical and molecular biology assays, while effective for specific readouts, often fail to capture the integrated cellular responses in living systems, potentially limiting early-stage drug discovery.
  • Label-free cell-based assays, such as dynamic mass redistribution (DMR), offer a holistic approach to studying cellular processes, addressing the limitations of conventional methods.

Purpose of the Study:

  • To provide guidance on setting up and optimizing dynamic mass redistribution (DMR) assays for investigating G protein-coupled receptor (GPCR) signaling.
  • To establish a knowledge base for deciphering integrated cellular readouts using DMR technology.
  • To demonstrate a basic DMR protocol using the FFA1 receptor as a model for family A GPCRs.

Main Methods:

  • Utilized dynamic mass redistribution (DMR) technology, a label-free cell-based assay.
  • Focused on developing and optimizing a basic DMR protocol.
  • Employed the long-chain fatty acid FFA1 receptor, a family A GPCR, as a model system for investigation.

Main Results:

  • Demonstrated the utility of DMR technology for investigating GPCR signaling in a holistic manner.
  • Provided a foundational protocol for DMR assay setup and optimization.
  • Highlighted the potential of DMR for sophisticated analysis of specialized scientific questions related to GPCRs.

Conclusions:

  • Dynamic mass redistribution (DMR) assays are a powerful tool for studying GPCRs by capturing integrated cellular responses.
  • Optimized DMR protocols can overcome the limitations of traditional assays in drug discovery.
  • This work provides a basis for applying DMR to a wider range of GPCR research and drug development.