Article
Biochemical and structural basis for differential inhibitor sensitivity of EGFR with distinct exon 19 mutations.
Nature communications - 10 Nov 2022
van Alderwerelt van Rosenburgh Iris K, Lu David M, Grant Michael J, Stayrook Steven E, Phadke Manali, Walther Zenta, Goldberg Sarah B, Politi Katerina, Lemmon Mark A, Ashtekar Kumar D, Tsutsui Yuko
Abstract excerpt
Tyrosine kinase inhibitors (TKIs) are used to treat non-small cell lung cancers (NSCLC) driven by epidermal growth factor receptor (EGFR) mutations in the tyrosine kinase domain (TKD). TKI responses vary across tumors driven by the heterogeneous group of exon 19 deletions and mutations, but the molecular basis for these differences is not understood. Using purified TKDs, we compared kinetic properties of several...
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