EGFR: Activating Mutations and Iressa Inhibition

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The growth factor receptor (GFR) is a membrane-bound kinase protein that forms pairs in response to growth factor binding, triggering the activation of its cytoplasmic kinase domain. This activates signaling pathways for critical cell processes like growth, specialization and movement. Mutations causing permanent GFR activation are linked to the development of non-small cell lung cancers (NSCLCs). This interactive tour explores key interactions maintaining the inactive GFR conformation. It then shows common mutations that cause permanent GFR activation, which is associated with NSCLCs. Finally, it explains how Iressa, a competitive blocker, prevents permanent GFR activation. References: 10.1016/j.ccr.2006.12.017, 10.1074/jbc.M207135200, 10.1158/1535-7163.MCT-12-0880