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Article

Discovery of Potent and Selective Covalent Inhibitors of HER2WT and HER2YVMA.

Journal of medicinal chemistry - 13 Jun 2024

Hicken Erik J, Brown Karin, Dwulet Natalie C, Gaudino John J, Hansen Erik P, Hartley Dylan P, Kowalski John P, Laird Ellen R, Lazzara Nicholas C, Li Bin, Mou Tung-Chung, Mutryn Marie F, Oko Lauren, Pajk Spencer, Pipal Robert W, Rosen Rachel Z, Shelp Russell, Singh Anurag, Wang Jing, Wise Courtney E, Wong Christina, Wong Jim Y

Abstract excerpt

HER2 overexpression and amplification have been identified as oncogenic drivers, and the development of therapies to treat tumors harboring these markers has received considerable attention. Activation of HER2 signaling and subsequent cell growth can also be induced by HER2 mutations, including the common YVMA insertion in exon 20 within the kinase domain. Enhertu is currently the only approved treatment for HER2...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 38820338
DOI: 10.1021/acs.jmedchem.4c00978

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 6 Sept 2026.

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