Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors
Autor: | Jonas Lategahn, Hannah L. Tumbrink, Carsten Schultz-Fademrecht, Alena Heimsoeth, Lisa Werr, Janina Niggenaber, Marina Keul, Fatma Parmaksiz, Matthias Baumann, Sascha Menninger, Eldar Zent, Ina Landel, Jörn Weisner, Kirujan Jeyakumar, Leonie Heyden, Nicole Russ, Fabienne Müller, Carina Lorenz, Johannes Brägelmann, Inga Spille, Tobias Grabe, Matthias P. Müller, Johannes M. Heuckmann, Bert M. Klebl, Peter Nussbaumer, Martin L. Sos, Daniel Rauh |
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Rok vydání: | 2022 |
Předmět: | |
Zdroj: | Journal of Medicinal Chemistry. 65:6643-6655 |
ISSN: | 1520-4804 0022-2623 |
Popis: | Despite the clinical efficacy of epidermal growth factor receptor (EGFR) inhibitors, a subset of patients with non-small cell lung cancer displays insertion mutations in exon20 in EGFR and Her2 with limited treatment options. Here, we present the development and characterization of the novel covalent inhibitors LDC8201 and LDC0496 based on a 1 |
Databáze: | OpenAIRE |
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