scholarly journals Dynamics of Protein Expression Reveals Primary Targets and Secondary Messengers of Estrogen Receptor Alpha Signaling in MCF-7 Breast Cancer Cells

2016 ◽  
Vol 15 (6) ◽  
pp. 2093-2107 ◽  
Author(s):  
Andrei P. Drabovich ◽  
Maria P. Pavlou ◽  
Christina Schiza ◽  
Eleftherios P. Diamandis
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Protein Expression ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Estrogen Receptor Alpha ◽  
Receptor Alpha ◽  
Secondary Messengers ◽  
Mcf 7

scholarly journals Tetrahydro-iso-alpha Acids Antagonize Estrogen Receptor Alpha Activity in MCF-7 Breast Cancer Cells

2016 ◽  
Vol 2016 ◽  
pp. 1-12 ◽  
Author(s):  
Maëlle Lempereur ◽  
Claire Majewska ◽  
Amandine Brunquers ◽  
Sumalee Wongpramud ◽  
Bénédicte Valet ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Estrogen Receptor Alpha ◽  
Foam Stability ◽  
Binding Motif ◽  
Brewing Industry ◽  
Receptor Alpha ◽  
Mcf 7

Tetrahydro-iso-alpha acids commonly called THIAA or Tetra are modified hop acids extracted from hop (Humulus lupulusL.) which are frequently used in brewing industry mainly in order to provide beer bitterness and foam stability. Interestingly, molecular structure of tetrahydro-iso-alpha acids is close to a new type of estrogen receptor alpha (ERα) antagonists aimed at disrupting the binding of coactivators containing an LxxLL motif (NR-box). In this work we show that THIAA decreases estradiol-stimulated proliferation of MCF-7 (ERα-positive breast cancer cells). Besides, we show that it inhibits ERαtranscriptional activity. Interestingly, this extract fails to compete with estradiol for ERαbinding and does not significantly impact the receptor turnover rate in MCF-7 cells, suggesting that it does not act like classical antiestrogens. Hence, we demonstrate that THIAA is able to antagonize ERαestradiol-induced recruitment of the LxxLL binding motif.

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