Article
Structural Basis for EGFR Mutant Inhibition by Trisubstituted Imidazole Inhibitors.
Journal of medicinal chemistry - 23 Apr 2020
Heppner David E, Günther Marcel, Wittlinger Florian, Laufer Stefan A, Eck Michael J
Abstract excerpt
Acquired drug resistance in epidermal growth factor receptor (EGFR) mutant non-small-cell lung cancer is a persistent challenge in cancer therapy. Previous studies of trisubstituted imidazole inhibitors led to the serendipitous discovery of inhibitors that target the drug resistant EGFR(L858R/T790M/C797S) mutant with nanomolar potencies in a reversible binding mechanism. To dissect the molecular basis for their...
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