Article
Structural elements that enable specificity for mutant EGFR kinase domains with next-generation small-molecule inhibitors.
Methods in enzymology - 1 Jan 2023
Damghani Tahereh, Wittlinger Florian, Beyett Tyler S, Eck Michael J, Laufer Stefan A, Heppner David E
Abstract excerpt
Specificity for a desired enzyme target is an essential property of small-molecule inhibitors. Molecules targeting oncogenic driver mutations in the epidermal growth factor receptor (EGFR) kinase domain have had a considerable clinical impact due to their selective binding to cancer-causing mutants compared to wild type. Despite the availability of clinically approved drugs for cancers driven by EGFR mutants,...
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