Article
Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites.
Journal of medicinal chemistry - 27 Jan 2022
Wittlinger Florian, Heppner David E, To Ciric, Günther Marcel, Shin Bo Hee, Rana Jaimin K, Schmoker Anna M, Beyett Tyler S, Berger Lena M, Berger Benedict-Tilman, Bauer Nicolas, Vasta James D, Corona Cesear R, Robers Matthew B, Knapp Stefan, Jänne Pasi A, Eck Michael J, Laufer Stefan A
Abstract excerpt
Inhibitors targeting the epidermal growth factor receptor (EGFR) are an effective therapy for patients with non-small cell lung cancer harboring drug-sensitive activating mutations in the EGFR kinase domain. Drug resistance due to treatment-acquired mutations has motivated the development of successive generations of inhibitors that bind in the ATP site. The third-generation agent osimertinib is now a first-line...
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