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Article

Computational and Functional Analyses of HER2 Mutations Reveal Allosteric Activation Mechanisms and Altered Pharmacologic Effects.

Cancer research - 2 May 2023

Ishiyama Noboru, O'Connor Matthew, Salomatov Andrei, Romashko Darlene, Thakur Shalabh, Mentes Ahmet, Hopkins Julia F, Frampton Garrett M, Albacker Lee A, Kohlmann Anna, Roberts Christopher, Buck Elizabeth

Abstract excerpt

Amplification of HER2 can drive the proliferation of cancer cells, and several inhibitors of HER2 have been successfully developed. Recent advances in next-generation sequencing now reveal that HER2 is subject to mutation, with over 2,000 unique variants observed in human cancers. Several examples of oncogenic HER2 mutations have been described, and these primarily occur at allosteric sites outside the...

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Identifiers

PMID: 35503682
DOI: 10.1158/0008-5472.CAN-21-0940
PMCID: PMC10152233

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