Structure-function of EGFR kinase domain and its inhibitors

作者: Charles Eigenbrot

DOI: 10.1007/978-1-59745-356-1_3

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摘要: The EGF receptor is a key mediator of oncogenic transformation in wide variety solid tumors. Since 2002, there has been an explosion X-ray crystallographic results that provide powerful insight into the activation and hyperactivation this its close homologues HER2, HER3, HER4. ability to catalyze phospho-transfer resides EGFR intracellular tyrosine kinase domain, which proven clinically useful target for therapeutic intervention. rapidly expanding catalogue domain structures surveyed with focus on inhibitor activities liabilities, as well control dysregulation phenomena intrinsic protein.

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