Erlotinib binds both inactive and active conformations of the EGFR tyrosine kinase domain.
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ABSTRACT:
SUBMITTER: Park JH
PROVIDER: S-EPMC3507260 | biostudies-literature | 2012 Dec
REPOSITORIES: biostudies-literature
Publications
Erlotinib binds both inactive and active conformations of the EGFR tyrosine kinase domain.
Park Jin H JH Liu Yingting Y Lemmon Mark A MA Radhakrishnan Ravi R
The Biochemical journal 20121201 3
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. ...[more]
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