Related Experiment Video

Updated: Jul 24, 2025

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
07:41

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

Published on: February 20, 2018

8.9K

The landscape of cancer rewired GPCR signaling axes

Chakit Arora1, Marin Matic1, Pierluigi DiChiaro2

  • 1Laboratorio di Biologia Bio@SNS, Scuola Normale Superiore, Piazza dei Cavalieri 7, 56126, Pisa, Italy.

Biorxiv : the Preprint Server for Biology
|July 3, 2023
PubMed

Insights

This study reveals how G protein-coupled receptor (GPCR) signaling networks are altered in cancer. Targeting these GPCR axes offers new therapeutic strategies for oncology.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) are crucial cell surface receptors involved in numerous physiological processes.
  • Dysregulation of GPCR signaling pathways is implicated in various cancer types, highlighting their potential as therapeutic targets.

Approach:

  • Analysis of cancer transcriptomics datasets to construct GPCR-ligand-enzyme interaction networks.
  • Utilized enzyme expression to infer pathway activity and GPCR ligand responses.
  • Investigated associations between GPCR signaling components and patient survival across cancer subtypes.

Key Points:

  • GPCRs and their upstream partners are differentially regulated across cancer subtypes.
  • GPCR network activity is linked to patient survival, with combined receptor-ligand/enzyme expression improving stratification.
  • Identified specific GPCR axes, including those involving neurotransmitter biosynthetic enzymes, as actionable targets.

Conclusions:

  • GPCR signaling networks play a synergistic role in modulating cancer phenotypes.
  • GPCRs targeted by existing drugs show anti-growth effects in cancer cell screens.
  • The findings provide a web-accessible resource (gpcrcanceraxes.bioinfolab.sns.it) for exploring GPCR-based cancer therapeutics.

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