Transactivation of Epidermal Growth Factor Receptor by G Protein-Coupled Receptors: Recent Progress, Challenges and Future Research

• Published in: International Journal of Molecular Sciences Vol. 17; no. 1; p. 95
• Main Author: Wang, Zhixiang
• Format: Journal Article Book Review
• Language: English
• Published: Switzerland MDPI AG 12.01.2016; MDPI
• Subjects: Animals; cancer; Cell Line; EGF receptor; Endothelin-1 - pharmacology; Epidermal growth factor; Fibroblasts - cytology; Fibroblasts - drug effects; Fibroblasts - metabolism; G protein-coupled receptors; Humans; Lysophospholipids - pharmacology; mechanisms; Medical research; Neurons; Rats; Receptor Cross-Talk; Receptor, Epidermal Growth Factor - genetics; Receptor, Epidermal Growth Factor - metabolism; Receptors, G-Protein-Coupled - agonists; Receptors, G-Protein-Coupled - genetics; Receptors, G-Protein-Coupled - metabolism; Review; Signal Transduction; Thrombin - pharmacology; Transcriptional Activation; EGF receptor; cancer; G protein-coupled receptors; mechanisms
• ISSN: 1422-0067; 1661-6596; 1422-0067
• DOI: 10.3390/ijms17010095

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.