The epidermal growth factor receptor (EGFR) is a transmembrane protein that is a receptor for members of the epidermal growth factor family (EGF family) of extracellular protein ligands. Mutations affecting EGFR expression or activity could result in cancer.
Erlotinib and gefitinib, tyrosine kinase inhibitors used to block EGFR (epidermal growth factor receptor) signaling in cancer, are thought to bind only the active conformation of the EGFR-TKD (tyrosine kinase domain). Through parallel computational and crystallographic studies, we show in the present study that erlotinib also binds the Inactive EGFR Tyrosine Kinase conformation, which may have significant implications for its use in EGFR-mutated cancers.
PDB ID: 4hjo