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• W2028450114 abstract "Significance Late-stage estrogen receptor α (ERα)-positive breast and ovarian cancers exhibit many regulatory alterations and therefore resist therapy. Our novel ERα inhibitor, BHPI, stops growth and often kills drug-resistant ERα + cancer cells and induces rapid and substantial tumor regression in a mouse model of human breast cancer. BHPI distorts a normally protective estrogen–ERα-mediated activation of the unfolded protein response (UPR) and elicits sustained UPR activation. The UPR cannot be deactivated because BHPI, acting at a second site, inhibits production of proteins that normally help turn it off. This persistent activation converts the UPR from protective to lethal. Targeting therapy-resistant ERα-positive cancer cells by converting the UPR from cytoprotective to cytotoxic may hold significant therapeutic promise." @default.
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• W2028450114 date "2015-03-30" @default.
• W2028450114 modified "2023-10-16" @default.
• W2028450114 title "Estrogen receptor α inhibitor activates the unfolded protein response, blocks protein synthesis, and induces tumor regression" @default.
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• W2028450114 doi "https://doi.org/10.1073/pnas.1403685112" @default.
• W2028450114 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/4403155" @default.
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