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
Rok vydání:	2022
Předmět:	Mice Mutagenesis Insertional Lung Neoplasms Carcinoma Non-Small-Cell Lung Mutation Drug Discovery Animals Humans Molecular Medicine Protein Kinase Inhibitors
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
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::114ce4ea37084352d24970d9460967e4 https://doi.org/10.1021/acs.jmedchem.1c02080 Zobrazit plný text záznamu