Related Experiment Video

Updated: Mar 23, 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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G protein-coupled receptors as promising cancer targets

Ying Liu1, Su An1, Richard Ward2

  • 1Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming, Yunnan 650500, China.

Cancer Letters
|March 23, 2016
PubMed

Insights

G protein-coupled receptors (GPCRs) play a crucial role in cancer development and progression. Targeting these receptors offers promising therapeutic strategies for various solid cancers.

Area of Science:

  • Molecular Biology
  • Oncology
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) are vital regulators of cellular functions, including growth, metabolism, and homeostasis.
  • GPCRs are increasingly recognized for their significant involvement in cancer initiation, progression, invasion, and metastasis.
  • Their role in shaping the tumor microenvironment, influencing vasculature, signaling, and extracellular matrix, is critical.

Purpose of the Study:

  • To highlight the underappreciated role of GPCRs in cancer.
  • To review specific tumor-related GPCRs and their functions in tumorigenesis.
  • To discuss the therapeutic potential of targeting GPCRs in cancer treatment.

Main Methods:

  • Literature review focusing on recent findings on GPCRs in cancer.
  • Analysis of tissue distribution, activation mechanisms, and roles in tumorigenesis for key GPCRs.
  • Discussion of GPCR-targeted therapeutic strategies, including agonists and antagonists.

Main Results:

  • Numerous GPCRs are implicated in various stages of cancer development and progression.
  • GPCRs actively contribute to creating a pro-tumorigenic microenvironment.
  • Specific GPCRs like G protein-coupled receptor 30, lysophosphatidic acid receptors, angiotensin receptors, sphingosine 1-phosphate receptors, and gastrin-releasing peptide receptor are key players.

Conclusions:

  • GPCRs represent highly valuable drug targets for numerous solid cancers.
  • Selective ligands targeting GPCRs hold potential for novel and effective cancer therapies.
  • Several GPCR-targeting anticancer compounds are currently undergoing clinical trials.
Keywords:
ActivationCancerGPCRGPR30Mutation

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