Related Experiment Video

Updated: Feb 26, 2026

Deciphering the Structural Effects of Activating EGFR Somatic Mutations with Molecular Dynamics Simulation
15:05

Deciphering the Structural Effects of Activating EGFR Somatic Mutations with Molecular Dynamics Simulation

Published on: May 20, 2020

9.4K

GPCRs and EGFR - Cross-talk of membrane receptors in cancer

Meryem Köse1

  • 1PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, D-53121 Bonn, Germany.

Bioorganic & Medicinal Chemistry Letters
|July 15, 2017
PubMed

Insights

G protein-coupled receptors (GPCRs) and receptor-tyrosine kinases (RTKs) interact to drive cancer growth. Targeting this cross-talk, particularly EGFR transactivation, offers new therapeutic strategies for cancer treatment.

Area of Science:

  • Molecular Biology
  • Oncology
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) and receptor-tyrosine kinases (RTKs) are crucial cell surface receptors and drug targets.
  • Both receptor classes regulate vital physiological processes, including cell growth and differentiation.
  • Emerging evidence highlights GPCR-mediated EGFR transactivation as a key mechanism in cancer.

Purpose of the Study:

  • To review the cross-talk between GPCRs and EGFR, focusing on scaffold proteins.
  • To provide an overview of current research, recent trends, and future directions in this field.
  • To discuss therapeutic strategies targeting GPCRs, EGFR, and their cross-talk in cancer therapy.

Main Methods:

  • Literature review of current research on GPCR-EGFR cross-talk.
  • Emphasis on intracellular scaffold proteins regulating EGFR transactivation.
  • Analysis of therapeutic strategies for cancer treatment.

Main Results:

  • GPCRs can induce EGFR activation, contributing to cancer progression.
  • Intracellular scaffold proteins play a critical role in regulating this transactivation.
  • Combined targeting of GPCRs and EGFR, or their cross-talk, shows therapeutic potential.

Conclusions:

  • The cross-talk between GPCRs and EGFR is a significant mechanism in various cancers.
  • Targeting this interaction, especially EGFR transactivation, presents promising avenues for cancer therapy.
  • Future research should focus on developing strategies that combine or specifically target these pathways.
Keywords:
Bias signalingCancerEGFR transactivationGPCRβ-Arrestin

More Related Videos

Establishing Dual Resistance to EGFR-TKI and MET-TKI in Lung Adenocarcinoma Cells In Vitro with a 2-step Dose-escalation Procedure09:38

Establishing Dual Resistance to EGFR-TKI and MET-TKI in Lung Adenocarcinoma Cells In Vitro with a 2-step Dose-escalation Procedure

Published on: August 11, 2017

9.3K
An Immunofluorescent Method for Characterization of Barrett’s Esophagus Cells08:54

An Immunofluorescent Method for Characterization of Barrett’s Esophagus Cells

Published on: July 20, 2014

14.5K

Related Concept Videos

Mitogens and the Cell Cycle02:38

Mitogens and the Cell Cycle

Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...
8.2K
Interactions Between Signaling Pathways01:19

Interactions Between Signaling Pathways

Signaling cascades usually lack linearity. Multiple pathways interact and regulate one another, allowing cells to integrate and respond to diverse environmental stimuli.
Convergence and divergence, and cross-talk between signaling pathways
Two distinct signaling pathways can converge on a single functional unit, which may either be a single protein or a complex of proteins. The response is either functionally distinct or synergistic between the two pathways but different from the response...
7.4K
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical,...
5.4K
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
7.8K
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
18.3K
Cancer-Critical Genes I: Proto-oncogenes01:33

Cancer-Critical Genes I: Proto-oncogenes

Genes usually encode proteins necessary for the proper functioning of a healthy cell. Mutations can often cause changes to the gene expression pattern, thereby altering the phenotype.
When the function of certain critical genes, especially those involved in cell cycle regulation and cell growth signaling cascades, gets disrupted, it upsets the cell cycle progression. Such cells with unchecked cell cycles start proliferating uncontrollably and eventually develop into tumors.
Such genes that act...
11.6K