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Published on: May 20, 2020
Transactivation of Epidermal Growth Factor Receptor by G Protein-Coupled Receptors: Recent Progress, Challenges and
1The Department of Medical Genetics and Signal Transduction Research Group, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, AB T6G 2H7, Canada. zhixiang.wang@ualberta.ca.
Abstract:
Both G protein-coupled receptors (GPCRs) and receptor-tyrosine kinases (RTKs) regulate large signaling networks, control multiple cell functions and are implicated in many diseases including various cancers. Both of them are also the top therapeutic targets for disease treatment. The discovery of the cross-talk between GPCRs and RTKs connects these two vast signaling networks and complicates the already complicated signaling networks that regulate cell signaling and function. In this review, we focus on the transactivation of epidermal growth factor receptor (EGFR), a subfamily of RTKs, by GPCRs. Since the first report of EGFR transactivation by GPCR, significant progress has been made including the elucidation of the mechanisms underlying the transactivation. Here, we first provide a basic picture for GPCR, EGFR and EGFR transactivation by GPCR. We then discuss the progress made in the last five years and finally provided our view of the future challenge and future researches needed to overcome these challenges.
Insights
G protein-coupled receptors (GPCRs) transactivate the epidermal growth factor receptor (EGFR), a receptor-tyrosine kinase (RTK). This review details GPCR-mediated EGFR transactivation mechanisms and future research directions.
Area of Science:
- Cellular signaling pathways
- Molecular biology
- Cancer research
Background:
- G protein-coupled receptors (GPCRs) and receptor-tyrosine kinases (RTKs) are crucial regulators of cellular functions and are implicated in diseases like cancer.
- Both GPCRs and RTKs are significant therapeutic targets.
- The cross-talk between these receptor families adds complexity to cellular signaling networks.
Purpose of the Study:
- To review the transactivation of epidermal growth factor receptor (EGFR) by GPCRs.
- To elucidate the mechanisms underlying GPCR-mediated EGFR transactivation.
- To discuss recent advancements and future challenges in this field.
Main Methods:
- Literature review focusing on GPCR-mediated EGFR transactivation.
- Analysis of signaling pathways involved in the cross-talk.
- Synthesis of current research findings and future perspectives.
Main Results:
- GPCRs can transactivate EGFR, a key RTK subfamily.
- Significant progress has been made in understanding the mechanisms of this transactivation.
- Recent research has elucidated intricate details of the cross-talk between GPCRs and EGFR.
Conclusions:
- GPCR-mediated EGFR transactivation is a critical area of study in cell signaling.
- Understanding these mechanisms is vital for developing targeted cancer therapies.
- Future research should focus on overcoming current challenges to further unravel this complex signaling network.
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