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

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 cl...

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Autores principales: Lempereur, Maëlle, Majewska, Claire, Brunquers, Amandine, Wongpramud, Sumalee, Valet, Bénédicte, Janssens, Philippe, Dillemans, Monique, Van Nedervelde, Laurence, Gallo, Dominique
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Hindawi Publishing Corporation 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4844874/
https://www.ncbi.nlm.nih.gov/pubmed/27190515
http://dx.doi.org/10.1155/2016/9747863
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author Lempereur, Maëlle
Majewska, Claire
Brunquers, Amandine
Wongpramud, Sumalee
Valet, Bénédicte
Janssens, Philippe
Dillemans, Monique
Van Nedervelde, Laurence
Gallo, Dominique
author_facet Lempereur, Maëlle
Majewska, Claire
Brunquers, Amandine
Wongpramud, Sumalee
Valet, Bénédicte
Janssens, Philippe
Dillemans, Monique
Van Nedervelde, Laurence
Gallo, Dominique
author_sort Lempereur, Maëlle
collection PubMed
description 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 (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 ERα transcriptional activity. Interestingly, this extract fails to compete with estradiol for ERα 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 ERα estradiol-induced recruitment of the LxxLL binding motif.
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spelling pubmed-48448742016-05-17 Tetrahydro-iso-alpha Acids Antagonize Estrogen Receptor Alpha Activity in MCF-7 Breast Cancer Cells Lempereur, Maëlle Majewska, Claire Brunquers, Amandine Wongpramud, Sumalee Valet, Bénédicte Janssens, Philippe Dillemans, Monique Van Nedervelde, Laurence Gallo, Dominique Int J Endocrinol Research Article 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 (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 ERα transcriptional activity. Interestingly, this extract fails to compete with estradiol for ERα 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 ERα estradiol-induced recruitment of the LxxLL binding motif. Hindawi Publishing Corporation 2016 2016-04-12 /pmc/articles/PMC4844874/ /pubmed/27190515 http://dx.doi.org/10.1155/2016/9747863 Text en Copyright © 2016 Maëlle Lempereur et al. https://creativecommons.org/licenses/by/4.0/ This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Article
Lempereur, Maëlle
Majewska, Claire
Brunquers, Amandine
Wongpramud, Sumalee
Valet, Bénédicte
Janssens, Philippe
Dillemans, Monique
Van Nedervelde, Laurence
Gallo, Dominique
Tetrahydro-iso-alpha Acids Antagonize Estrogen Receptor Alpha Activity in MCF-7 Breast Cancer Cells
title Tetrahydro-iso-alpha Acids Antagonize Estrogen Receptor Alpha Activity in MCF-7 Breast Cancer Cells
title_full Tetrahydro-iso-alpha Acids Antagonize Estrogen Receptor Alpha Activity in MCF-7 Breast Cancer Cells
title_fullStr Tetrahydro-iso-alpha Acids Antagonize Estrogen Receptor Alpha Activity in MCF-7 Breast Cancer Cells
title_full_unstemmed Tetrahydro-iso-alpha Acids Antagonize Estrogen Receptor Alpha Activity in MCF-7 Breast Cancer Cells
title_short Tetrahydro-iso-alpha Acids Antagonize Estrogen Receptor Alpha Activity in MCF-7 Breast Cancer Cells
title_sort tetrahydro-iso-alpha acids antagonize estrogen receptor alpha activity in mcf-7 breast cancer cells
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4844874/
https://www.ncbi.nlm.nih.gov/pubmed/27190515
http://dx.doi.org/10.1155/2016/9747863
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