Unravelling the molecular complexity of GPCR-mediated EGFR transactivation using functional genomics approaches

Amee J George, Ross Duncan Hannan, Walter Glen Thomas

Research output: Contribution to journalArticleResearchpeer-review

46 Citations (Scopus)

Abstract

To influence physiology and pathophysiology, G protein-coupled receptors (GPCRs) have evolved to appropriate additional signalling modalities, such as activation of adjacent membrane receptors. Epidermal growth factor receptors (EGFRs) mediate growth and remodelling actions of GPCRs, although the precise network of gene products and molecular cascades linking GPCRs to EGFRs (termed EGFR transactivation) remains incomplete. In this review, we describe the current view of GPCR-EGFR transactivation, identifying the established models of receptor cross-talk. We consider the limitations in our current knowledge, and propose that recent advances in molecular and cell biology technology, including functional genomics approaches, will allow a renewed focus of efforts to understand the mechanism underlying EGFR transactivation. Using an unbiased approach for identification of the molecules required for GPCR-mediated EGFR transactivation will provide a contemporary and more complete representation from which to extrapolate therapeutic control in diseases from cardiovascular remodelling to cancer.
Original languageEnglish
Pages (from-to)5258 - 5268
Number of pages11
JournalThe FEBS Journal
Volume280
Issue number21
DOIs
Publication statusPublished - 2013

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