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Unravelling the molecular complexity of GPCR ‐mediated EGFR transactivation using functional genomics approaches
Author(s) -
George Amee J.,
Hannan Ross D.,
Thomas Walter G.
Publication year - 2013
Publication title -
the febs journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.981
H-Index - 204
eISSN - 1742-4658
pISSN - 1742-464X
DOI - 10.1111/febs.12509
Subject(s) - transactivation , g protein coupled receptor , computational biology , functional genomics , biology , epidermal growth factor receptor , receptor , genomics , bioinformatics , microbiology and biotechnology , signal transduction , gene , genetics , genome , gene expression
To influence physiology and pathophysiology, G protein‐coupled receptors ( GPCR s) have evolved to appropriate additional signalling modalities, such as activation of adjacent membrane receptors. Epidermal growth factor receptors ( EGFR s) mediate growth and remodelling actions of GPCR s, although the precise network of gene products and molecular cascades linking GPCR s to EGFR s (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.