Erlotinib binds both inactive and active conformations of the EGFR tyrosine kinase domain.

ABSTRACT: Erlotinib and gefitinib, tyrosine kinase inhibitors used to block EGFR (epidermal growth factor receptor) signalling 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-TKD conformation, which may have significant implications for its use in EGFR-mutated cancers.

SUBMITTER: Park JH 

PROVIDER: S-EPMC3507260 | biostudies-literature | 2012 Dec

REPOSITORIES: biostudies-literature