1. Structural model of Y764_V765insHH.
Structural model of Y764_V765insHH. A, Alignments of EGFR wild-type, Y764_V765insHH, V765H+M766H, and M766_A767insAA. The catalytically indispensable Glu762 is shown in the blue box. B, Superimposition of different EGFR-TKIs on the structural model of EGFR Y764_V765insHH. Key residues on EGFR for kinase catalysis are shown as orange sticks. Leu858, a key residue for EGFR activation, is shown as yellow sticks. The inserted histidine residues are shown as magenta sticks. TKIs erlotinib, afatinib, naquotinib, and osimertinib are shown in gray, green, yellow, and cyan, respectively. Inset, chemical structures of erlotinib, afatinib, naquotinib, and osimertinib.
Toshiyuki Hirano et al. Mol Cancer Ther 2018;17:
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