Related Experiment Video

Updated: Nov 27, 2025

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

Published on: February 20, 2018

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G Protein-Coupled receptors and heterotrimeric G proteins as cancer drivers

Nadia Arang1, J Silvio Gutkind1

  • 1Department of Pharmacology, Moores Cancer Center, University of California, San Diego, La Jolla, CA, USA.

FEBS Letters
|December 3, 2020
PubMed

Insights

G protein-coupled receptors (GPCRs) and G proteins are crucial in cell processes. Their dysregulation drives cancer initiation and progression, offering new therapeutic targets.

Area of Science:

  • Cellular Biology
  • Molecular Biology
  • Oncology

Background:

  • G protein-coupled receptors (GPCRs) and heterotrimeric G proteins are integral to cellular signaling.
  • Dysregulation of GPCR/G protein pathways significantly impacts cellular function and disease states.
  • These pathways are implicated in numerous human diseases, notably cancer.

Purpose of the Study:

  • To review the role of GPCRs and heterotrimeric G proteins in cancer.
  • To highlight their involvement in cancer initiation and progression.
  • To discuss their potential as antitumoural therapeutic targets.

Main Methods:

  • Literature review of research on GPCRs and G proteins in cancer.
  • Analysis of studies detailing GPCR/G protein-mediated signaling in oncogenesis.
  • Synthesis of findings on therapeutic strategies targeting these pathways.

Main Results:

  • GPCR/G protein signaling influences key oncogenic processes including angiogenesis, immune evasion, metastasis, and drug resistance.
  • Evidence supports GPCRs and G proteins as drivers of tumor development.
  • These molecules represent promising targets for novel cancer therapies.

Conclusions:

  • GPCRs and their cognate G proteins are critical regulators of cancer initiation and progression.
  • Targeting GPCR/G protein pathways offers a promising avenue for developing new cancer treatments.
Keywords:
G protein-coupled receptorsGTPasesangiogenesiscancercancer metabolismimmune therapyinflammationmetastasisprecision medicinesignal transduction

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