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Article

Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR.

Bioorganic & medicinal chemistry - 1 Apr 2008

Michalczyk Anja, Klüter Sabine, Rode Haridas B, Simard Jeffrey R, Grütter Christian, Rabiller Matthias, Rauh Daniel

Abstract excerpt

Resistance to kinase-targeted cancer drugs has recently been linked to a single point mutation in the ATP binding site of the kinase. In EGFR, the crucial Thr790 gatekeeper residue is mutated to a Met and prevents reversible ATP competitive inhibitors from binding. Irreversible 4-(phenylamino)qui...

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Identifiers

PMID: 18316192
DOI: 10.1016/j.bmc.2008.02.053

Genes

EGFR

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 2 Sept 2026. Prepared record publication-18316192-2026-09-02.2. Manifest publication-graph-cohort-2026-09-02.2.

Source receipt: PubMed via Helena Literature Corpus, retrieved 2 Sept 2026.

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