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Tetrahydro-iso-alpha acids commonly called THIAA or Tetra are modified hop acids extracted from hop ( Humulus lupulus  L.) 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 (ER α ) 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 (ER α -positive breast cancer cells). Besides, we show that it inhibits ER α  transcriptional activity. Interestingly, this extract fails to compete with estradiol for ER α  binding 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 ER α  estradiol-induced recruitment of the LxxLL binding motif.

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