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Article

Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors.

Journal of medicinal chemistry - 12 May 2022

Lategahn Jonas, Tumbrink Hannah L, Schultz-Fademrecht Carsten, Heimsoeth Alena, Werr Lisa, Niggenaber Janina, Keul Marina, Parmaksiz Fatma, Baumann Matthias, Menninger Sascha, Zent Eldar, Landel Ina, Weisner Jörn, Jeyakumar Kirujan, Heyden Leonie, Russ Nicole, Müller Fabienne, Lorenz Carina, Brägelmann Johannes, Spille Inga, Grabe Tobias, Müller Matthias P, Heuckmann Johannes M, Klebl Bert M, Nussbaumer Peter, Sos Martin L, Rauh Daniel

Abstract excerpt

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 1H-pyrrolo[2,3-b]pyridine scaffold. They exhibited intense inhibitory...

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Identifiers

PMID: 35486541
DOI: 10.1021/acs.jmedchem.1c02080

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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