Epidermal growth factor receptor (EGFR) (EGFR)

The Epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein and a member of the ErbB family of receptor tyrosine kinases. It plays a critical role in regulating cell growth, survival, and proliferation through the activation of downstream signaling pathways such as MAPK/ERK and PI3K/Akt (Source: UniProt P00533). In many cancers, particularly non-small cell lung cancer (NSCLC), EGFR is frequently mutated or overexpressed, leading to constitutive signaling and tumor progression. While EGFR tyrosine kinase inhibitors (TKIs) are standard-of-care treatments, clinical efficacy is often limited by the emergence of resistance. Resistance mechanisms include secondary mutations in the EGFR kinase domain (like T790M or C797S), activation of bypass signaling pathways (such as MET or HER2 amplification), or phenotypic changes like epithelial-to-mesenchymal transition (Source: PMC7066303, PubMed). Consequently, modulating these resistance pathways through combination therapies or next-generation inhibitors is a major focus of current oncological research.

Other names

ErbB-1HER1Proto-oncogene c-ErbB-1Receptor tyrosine-protein kinase erbB-1

Inhibition of the intracellular tyrosine kinase domain to block downstream signaling (small molecule TKIs) or blocking the extracellular ligand-binding domain to prevent receptor activation (monoclonal antibodies).