Irreversible inhibition of Δ16HER2 is necessary to suppress Δ16HER2-positive breast carcinomas resistant to Lapatinib.

Cancer Letters(2016)

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摘要
•Saracatinib and Dacomitinib block the oncogenic Δ16HER2/Src axis in vitro.•Erk signaling escape pathway mediates acquired resistance to Saracatinib in vivo.•Δ16HER2+ breast tumors are refractory to reversible TKI Lapatinib.•Δ16HER2+ breast tumors are responsive to irreversible TKI Dacomitinib.
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关键词
HER2 isoform,Breast cancer,Δ16HER2 mice,Targeted therapies,Drug resistances
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