Unravelling G protein‐coupled receptor signalling networks using global phosphoproteomics

G protein‐coupled receptor (GPCR) activation initiates signalling via a complex network of intracellular effectors that combine to produce diverse cellular and tissue responses. Although we have an advanced understanding of the proximal events following receptor stimulation, the molecular detail of...

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Bibliographic Details
Published in:British journal of pharmacology 2024-07, Vol.181 (14), p.2359-2370
Main Authors: Pokhrel, Rina, Morgan, Alexandra L., Robinson, Harley R., Stone, Martin J., Foster, Simon R.
Format: Article
Language:English
Subjects:
Animals
G protein-coupled receptors
G protein‐coupled receptor
Humans
Intracellular signalling
ligands
mass spectrometry
Phosphoproteins - metabolism
phosphoproteomics
Proteins
Proteomics
Receptors, G-Protein-Coupled - metabolism
Signal Transduction
signalling networks
Therapeutic targets
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Summary:G protein‐coupled receptor (GPCR) activation initiates signalling via a complex network of intracellular effectors that combine to produce diverse cellular and tissue responses. Although we have an advanced understanding of the proximal events following receptor stimulation, the molecular detail of GPCR signalling further downstream often remains obscure. Unravelling these GPCR‐mediated signalling networks has important implications for receptor biology and drug discovery. In this context, phosphoproteomics has emerged as a powerful approach for investigating global GPCR signal transduction. Here, we provide a brief overview of the phosphoproteomic workflow and discuss current limitations and future directions for this technology. By highlighting some of the novel insights into GPCR signalling networks gained using phosphoproteomics, we demonstrate the utility of global phosphoproteomics to dissect GPCR signalling networks and to accelerate discovery of new targets for therapeutic development. LINKED ARTICLES This article is part of a themed issue Therapeutic Targeting of G Protein‐Coupled Receptors: hot topics from the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists 2021 Virtual Annual Scientific Meeting. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v181.14/issuetoc
ISSN:0007-1188
1476-5381
1476-5381
DOI:10.1111/bph.16052