Eck Lab

Dana-Farber Cancer Inst

Boston · United States

NIH-funded
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NIH R01 · 2025

Discovery and optimization of novel mutant-selective allosteric inhibitors of EGFR T790M

Abstract: Somatic mutations in the tyrosine kinase domain of the epidermal growth factor receptor (EGFR) are a common cause of lung adenocarcinoma. Despite marked advances in targeted therapies for EGFR-mutant lung cancer, treatment-acquired resistance remains a major problem. Understanding and overcoming acquired resistance to EGFR tyrosine kinase inhibitors (TKIs) and to other targeted therapies is a central problem in cancer medicine. Our long term goal is to develop more effective and better tolerated therapies for EGFR mutant lung cancer that yield durable responses. We reason that simultaneous treatment with multiple agents targeting mutant EGFR may prevent emergence of resistance…

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