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Updated: Aug 19, 2026

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay
11:49

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay

Published on: July 28, 2014

Rho GTPase-dependent transformation by G protein-coupled receptors

I P Whitehead1, I E Zohn, C J Der

  • 1Department of Microbiology and Molecular Genetics, UMDNJ-New Jersey Medical School, Newark, New Jersey, NJ 07103-2714, USA.

Oncogene
|April 21, 2001
PubMed

Insights

Certain G protein-coupled receptors (GPCRs) can drive cancer development. These GPCR oncoproteins activate specific cellular pathways, leading to uncontrolled cell growth and tumor formation.

Area of Science:

  • Molecular Biology
  • Cell Biology
  • Oncology

Background:

  • G protein-coupled receptors (GPCRs) are a vast family of cell surface receptors involved in signal transduction.
  • While typically regulating metabolism in differentiated cells, some GPCRs are implicated in cell proliferation and oncogenesis.
  • Activating mutations and overexpression of GPCRs are linked to human tumors.

Purpose of the Study:

  • To review the signaling and transforming properties of GPCR oncoproteins.
  • To highlight the role of specific GPCRs (Mas, G2A, PAR-1) in oncogenic transformation.
  • To elucidate the molecular mechanisms underlying GPCR-mediated oncogenesis.

Main Methods:

  • Review of existing literature on GPCRs, oncogenes, and cell signaling.
  • Analysis of expression screening data identifying transforming GPCRs.
  • Summary of studies investigating GPCR signaling pathways and their link to cancer.

Main Results:

  • GPCRs, including Mas, G2A, and PAR-1, can induce oncogenic transformation of cells.
  • These transforming GPCRs activate Rho family small GTPases.
  • Aberrant activation of these GTPases leads to dysregulated cell growth.

Conclusions:

  • GPCRs represent a significant class of oncoproteins.
  • GPCR-mediated oncogenesis involves the activation of specific GTPase signaling cascades.
  • Targeting these pathways may offer therapeutic strategies for GPCR-driven cancers.

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