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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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G Protein-Coupled Receptors in Cancer

Rachel Bar-Shavit1, Myriam Maoz2, Arun Kancharla3

  • 1Sharett Institute of Oncology, Hadassah-Hebrew University Medical Center, Jerusalem 91120, Israel. Rachelbar@ekmd.huji.ac.il.

International Journal of Molecular Sciences
|August 17, 2016
PubMed

Insights

G protein-coupled receptors (GPCRs) play a crucial role in cancer development, influencing tumor growth and spread. Understanding GPCR signaling is key to developing targeted cancer therapies.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) are vital for physiological processes but their role in cancer is often overlooked.
  • GPCRs significantly influence tumorigenesis, affecting immune responses, cell proliferation, invasion, and metastasis.
  • Technological advancements reveal GPCR alterations in human tumors, including mutations, overexpression, and epigenetic silencing.

Purpose of the Study:

  • To highlight the underappreciated role of GPCRs in tumor biology.
  • To emphasize the need for elucidating signaling pathways of cancer-driving GPCRs.
  • To explore the implications of functional selectivity and biased agonism for drug development.

Main Methods:

  • Review of current evidence associating GPCRs with cancer growth and development.
  • Analysis of technological findings on GPCR modifications in human tumors.
  • Discussion of emerging concepts like functional selectivity and biased agonism.

Main Results:

  • GPCRs are implicated in various aspects of cancer, from immune modulation to metastatic potential.
  • GPCR alterations such as mutations, overexpression, and methylation are common in human cancers.
  • The concept of "one drug per GPCR target" is evolving towards identifying multiple drug options due to functional selectivity.

Conclusions:

  • Elucidating cancer-driving GPCR signaling pathways is imperative.
  • Understanding context-dependent GPCR conformations and alterations is crucial for targeted cancer therapy development.
  • GPCRs represent promising targets for novel cancer therapeutics, necessitating a nuanced approach to drug discovery.
Keywords:
CXCR4G protein-coupled receptors (GPCRs)Hippo/YAPLPA(1-6)PH-domainWnt/β-catenincanceroncogenesproteaseprotease-activated receptorprotease-activated receptors (PARs)

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