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Updated: Jul 7, 2025

G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay
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G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay

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GPCR-G protein selectivity revealed by structural pharmacology

Sarah M Bernhard1,2, Jianming Han1,2, Tao Che1,2

  • 1Department of Anesthesiology, Washington University School of Medicine, St. Louis, MO, USA.

The FEBS Journal
|December 27, 2023
PubMed
Summary

G protein-coupled receptors (GPCRs) can interact with multiple G protein subtypes, a phenomenon known as promiscuity. This study reveals structural insights into kappa opioid receptor (KOR) and Gi/o subtype selectivity, aiding targeted therapeutic development.

Keywords:
G proteinGPCRbias signalingselectivitystructural pharmacology

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