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Article

Inhibition of mutationally activated HER2.

Chemical biology & drug design - 1 Jan 2023

Collins Stephen J, Guo Jiaye, Rizzo Robert C, Miller W Todd

Abstract excerpt

Human epidermal growth factor receptor 2 (HER2) is an oncogenic driver and key therapeutic target for human cancers. Current therapies targeting HER2 are primarily based on overexpression of the wild-type form of HER2. However, kinase domain mutations have been identified that can increase the activity of HER2 even when expressed at basal levels. Using purified enzymes, we confirmed the hyperactivity of two HER2...

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PMID: 36029027
DOI: 10.1111/cbdd.14125
PMCID: PMC9879383

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