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Article

EXEL-7647 inhibits mutant forms of ErbB2 associated with lapatinib resistance and neoplastic transformation.

Clinical cancer research : an official journal of the American Association for Cancer Research - 15 Apr 2008

Trowe Torsten, Boukouvala Sotiria, Calkins Keith, Cutler Richard E, Fong Ryan, Funke Roel, Gendreau Steven B, Kim Yong D, Miller Nicole, Woolfrey John R, Vysotskaia Valentina, Yang Jing Ping, Gerritsen Mary E, Matthews David J, Lamb Peter, Heuer Timothy S

Abstract excerpt

PURPOSE: Mutations associated with resistance to kinase inhibition are an important mechanism of intrinsic or acquired loss of clinical efficacy for kinase-targeted therapeutics. We report the prospective discovery of ErbB2 mutations that confer resistance to the small-molecule inhibitor lapatinib. EXPERIMENTAL DESIGN: We did in vitro screening using a randomly mutagenized ErbB2 expression library in Ba/F3 cells,...

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Share to Antineoplastic Agents
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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Cell Transformation, Neoplastic

Share to Drug Resistance, Neoplasm

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Share to Receptor, ErbB-2

Source

Identifiers

PMID: 18413839
DOI: 10.1158/1078-0432.CCR-07-4367

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

Source receipt: pubmed, retrieved 7 Sept 2026.

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