Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors.

doi:10.1021/acs.jmedchem.9b01169

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Article

Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors.

Journal of medicinal chemistry - 27 Nov 2019

Engelhardt Harald, Böse Dietrich, Petronczki Mark, Scharn Dirk, Bader Gerd, Baum Anke, Bergner Andreas, Chong Eugene, Döbel Sandra, Egger Georg, Engelhardt Christian, Ettmayer Peter, Fuchs Julian E, Gerstberger Thomas, Gonnella Nina, Grimm Andreas, Grondal Elisabeth, Haddad Nizar, Hopfgartner Barbara, Kousek Roland, Krawiec Mariusz, Kriz Monika, Lamarre Lyne, Leung Joyce, Mayer Moriz, Patel Nitinchandra D, Simov Biljana Peric, Reeves Jonathan T, Schnitzer Renate, Schrenk Andreas, Sharps Bernadette, Solca Flavio, Stadtmüller Heinz, Tan Zhulin, Wunberg Tobias, Zoephel Andreas, McConnell Darryl B

Abstract excerpt

The epidermal growth factor receptor (EGFR), when carrying an activating mutation like del19 or L858R, acts as an oncogenic driver in a subset of lung tumors. While tumor responses to tyrosine kinase inhibitors (TKIs) are accompanied by marked tumor shrinkage, the response is usually not durable. Most patients relapse within two years of therapy often due to acquisition of an additional mutation in EGFR kinase...

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PMID: 31689114
DOI: 10.1021/acs.jmedchem.9b01169

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

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