Related Experiment Video

Updated: Jan 13, 2026

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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GPCR Biased Signaling in Cancer

Ariella C Avigad1,2,3, Melody Zhou1,2,3, Chengyu Sun1,2,3

  • 1Allegheny Health Network Cancer Institute, Allegheny Health Network, Pittsburgh, PA, USA.

Handbook of Experimental Pharmacology
|October 29, 2025
PubMed

Insights

G protein-coupled receptors (GPCRs) are key cell surface proteins. Understanding biased GPCR signaling in cancer offers new therapeutic avenues for oncology drug discovery.

Area of Science:

  • Molecular Biology
  • Oncology
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) are the largest cell surface receptor family, crucial for physiological processes.
  • Dysregulated GPCR signaling is implicated in cancer development, including tumor growth, angiogenesis, metastasis, and immune modulation.
  • Biased GPCR signaling, where ligands activate specific pathways, complicates cancer progression and treatment resistance.

Purpose of the Study:

  • To review recent advances in GPCR biased signaling in cancer biology.
  • To explore the therapeutic potential of targeting biased GPCR signaling in oncology.
  • To provide a framework for understanding beta-arrestin-mediated signaling in cancer, integrating literature and proteomics data.

Main Methods:

  • Literature review of GPCR biased signaling in cancer.
  • Integration of proteomics data on GPCR and beta-arrestin function.
  • Analysis of beta-arrestin-mediated signaling pathways in cancer contexts.

Main Results:

  • Biased GPCR signaling is a dynamic factor in cancer development, progression, and resistance.
  • Beta-arrestin-mediated signaling plays a significant role in cancer pathogenesis.
  • The study provides a preliminary framework for understanding these complex interactions.

Conclusions:

  • Understanding biased GPCR signaling is crucial for advancing cancer biology.
  • Targeting GPCRs and their biased signaling pathways holds therapeutic promise for cancer treatment.
  • This work lays the foundation for future research and drug discovery in oncology.
Keywords:
CancerGPCRGPCR biased signalingβ-arrestinβ-arrestin-mediated signaling

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