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Phosphoproteomic Strategy for Profiling Osmotic Stress Signaling in Arabidopsis
Published on: June 25, 2020
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In vivo brain GPCR signaling elucidated by phosphoproteomics.
Jeffrey J Liu1, Kirti Sharma1, Luca Zangrandi2
1Department of Proteomics and Signal Transduction, Max Planck Institute of Biochemistry, 82152 Martinsried, Germany.
Science (New York, N.Y.)
|June 23, 2018
Summary
Researchers used high-throughput phosphoproteomics to study kappa opioid receptor (KOR) signaling. They found inhibiting the mTOR pathway can reduce KOR-related side effects while maintaining therapeutic benefits.
Area of Science:
- Pharmacology
- Neuroscience
- Systems Biology
Background:
- G protein-coupled receptor (GPCR) signaling in vivo is crucial for developing targeted therapeutics.
- Understanding kappa opioid receptor (KOR) signaling pathways can lead to safer and more effective pain management drugs.
Purpose of the Study:
- To investigate the in vivo signaling of the kappa opioid receptor (KOR) using diverse agonists across different brain regions.
- To identify novel mechanisms of drug action and potential therapeutic targets for KOR-mediated effects.
Main Methods:
- Employed high-throughput phosphoproteomics to quantify over 50,000 phosphosites.
- Studied KOR signaling in five distinct mouse brain regions in response to various agonists.
Main Results:
- Discovered enrichment of the mechanistic target of rapamycin (mTOR) pathway by the KOR agonist U-50,488H, linked to aversion.
- Demonstrated that mTOR inhibition abolishes aversion while preserving beneficial antinociceptive and anticonvulsant effects of KOR activation.
Conclusions:
- High-throughput phosphoproteomics is a viable strategy for studying GPCR in vivo signaling.
- Modulating the mTOR pathway offers a potential method to mitigate side effects of KOR-targeting drugs.
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