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- W2017984129 abstract "Scope We have previously demonstrated that oleuropein ( OL ) and hydroxytyrosol ( HT ) reduce 17β‐estradiol‐mediated proliferation in MCF ‐7 breast cancer ( BC ) cells without affecting the classical genomic action of estrogen receptor ( ER ), but activating instead the ERK 1/2 pathway. Here, we hypothesized that this inhibition could be mediated by a G ‐protein‐coupled receptor named GPER / GPR 30. Using the ER ‐negative and GPER ‐positive SKBR 3 BC cells as experimental model, we investigated the effects of OL and HT on GPER ‐mediated activation of downstream pathways. Methods and results Docking simulations and ligand‐binding studies evidenced that OL and HT are able to bind GPER . MTT cell proliferation assays revealed that both phenols reduced SKBR 3 cell growth; this effect was abolished silencing GPER . Focusing on OL and HT GPER ‐mediated pathways, using W estern blot analysis we showed a sustained ERK 1/2 activation triggering an intrinsic apoptotic pathway. Conclusion Showing that OL and HT work as GPER inverse agonists in ER ‐negative and GPER ‐positive SKBR 3 BC cells, we provide novel insights into the potential of these two molecules as tools in the therapy of this subtype of BC ." @default.
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- W2017984129 date "2013-09-09" @default.
- W2017984129 modified "2023-10-04" @default.
- W2017984129 title "Oleuropein and hydroxytyrosol activate GPER/ GPR30-dependent pathways leading to apoptosis of ER-negative SKBR3 breast cancer cells" @default.
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- W2017984129 doi "https://doi.org/10.1002/mnfr.201300323" @default.
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