Polyoxometalate inhibition of SOX2-mediated tamoxifen resistance in breast cancer

Background Increased cancer stem cell (CSC) content and SOX2 overexpression are common features in the development of resistance to therapy in hormone-dependent breast cancer, which remains an important clinical challenge. SOX2 has potential as biomarker of resistance to treatment and as therapeutic...

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Autores: Aurrekoetxea Rodríguez, Iskander, Lee, So Young, Rabano, Miriam, Gris Cárdenas, Isabel, Gamboa Aldecoa, Virginia, Gorroño, Irantzu, Ramella Gal, Isabella, Parry, Connor, Kypta, Robert M., Artetxe Arretxe, Beñat, Gutiérrez Zorrilla López, Juan Manuel, Vivanco Ruiz, María del Mar
Tipo de recurso: artículo
Fecha de publicación:2024
País:España
Institución:Universidad del País Vasco
Repositorio:Addi. Archivo Digital para la Docencia y la Investigación
OAI Identifier:oai:addi.ehu.eus:10810/69470
Acceso en línea:http://hdl.handle.net/10810/69470
Access Level:acceso abierto
Palabra clave:breast cancer
cancer stem cells
resistance
hormone therapy
SOX2 inhibition
polyoxometalate
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network_name_str España
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dc.title.none.fl_str_mv Polyoxometalate inhibition of SOX2-mediated tamoxifen resistance in breast cancer
title Polyoxometalate inhibition of SOX2-mediated tamoxifen resistance in breast cancer
spellingShingle Polyoxometalate inhibition of SOX2-mediated tamoxifen resistance in breast cancer
Aurrekoetxea Rodríguez, Iskander
breast cancer
cancer stem cells
resistance
hormone therapy
SOX2 inhibition
polyoxometalate
title_short Polyoxometalate inhibition of SOX2-mediated tamoxifen resistance in breast cancer
title_full Polyoxometalate inhibition of SOX2-mediated tamoxifen resistance in breast cancer
title_fullStr Polyoxometalate inhibition of SOX2-mediated tamoxifen resistance in breast cancer
title_full_unstemmed Polyoxometalate inhibition of SOX2-mediated tamoxifen resistance in breast cancer
title_sort Polyoxometalate inhibition of SOX2-mediated tamoxifen resistance in breast cancer
dc.creator.none.fl_str_mv Aurrekoetxea Rodríguez, Iskander
Lee, So Young
Rabano, Miriam
Gris Cárdenas, Isabel
Gamboa Aldecoa, Virginia
Gorroño, Irantzu
Ramella Gal, Isabella
Parry, Connor
Kypta, Robert M.
Artetxe Arretxe, Beñat
Gutiérrez Zorrilla López, Juan Manuel
Vivanco Ruiz, María del Mar
author Aurrekoetxea Rodríguez, Iskander
author_facet Aurrekoetxea Rodríguez, Iskander
Lee, So Young
Rabano, Miriam
Gris Cárdenas, Isabel
Gamboa Aldecoa, Virginia
Gorroño, Irantzu
Ramella Gal, Isabella
Parry, Connor
Kypta, Robert M.
Artetxe Arretxe, Beñat
Gutiérrez Zorrilla López, Juan Manuel
Vivanco Ruiz, María del Mar
author_role author
author2 Lee, So Young
Rabano, Miriam
Gris Cárdenas, Isabel
Gamboa Aldecoa, Virginia
Gorroño, Irantzu
Ramella Gal, Isabella
Parry, Connor
Kypta, Robert M.
Artetxe Arretxe, Beñat
Gutiérrez Zorrilla López, Juan Manuel
Vivanco Ruiz, María del Mar
author2_role author
author
author
author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv breast cancer
cancer stem cells
resistance
hormone therapy
SOX2 inhibition
polyoxometalate
topic breast cancer
cancer stem cells
resistance
hormone therapy
SOX2 inhibition
polyoxometalate
description Background Increased cancer stem cell (CSC) content and SOX2 overexpression are common features in the development of resistance to therapy in hormone-dependent breast cancer, which remains an important clinical challenge. SOX2 has potential as biomarker of resistance to treatment and as therapeutic target, but targeting transcription factors is also challenging. Here, we examine the potential inhibitory effect of different polyoxometalate (POM) derivatives on SOX2 transcription factor in tamoxifen-resistant breast cancer cells. Methods Various POM derivatives were synthesised and characterised by infrared spectra, powder X-ray diffraction pattern and nuclear magnetic resonance spectroscopy. Estrogen receptor (ER) positive breast cancer cells, and their counterparts, which have developed resistance to the hormone therapy tamoxifen, were treated with POMs and their consequences assessed by gel retardation and chromatin immunoprecipitation to determine SOX2 binding to DNA. Effects on proliferation, migration, invasion and tumorigenicity were monitored and quantified using microscopy, clone formation, transwell, wound healing assays, flow cytometry and in vivo chick chorioallantoic membrane (CAM) models. Generation of lentiviral stable gene silencing and gene knock-out using CRISPR-Cas9 genome editing were applied to validate the inhibitory effects of the selected POM. Cancer stem cell subpopulations were quantified by mammosphere formation assays, ALDEFLUOR activity and CD44/CD24 stainings. Flow cytometry and western blotting were used to measure reactive oxygen species (ROS) and apoptosis. Results POMs blocked in vitro binding activity of endogenous SOX2. [P2W18O62]6− (PW) Wells-Dawson-type anion was the most effective at inhibiting proliferation in various cell line models of tamoxifen resistance. 10 µM PW also reduced cancer cell migration and invasion, as well as SNAI2 expression levels. Treatment of tamoxifen-resistant cells with PW impaired tumour formation by reducing CSC content, in a SOX2-dependent manner, which led to stem cell depletion in vivo. Mechanistically, PW induced formation of reactive oxygen species (ROS) and inhibited Bcl-2, leading to the death of tamoxifen-resistant cells. PW-treated tamoxifen-resistant cells showed restored sensitivity to tamoxifen. Conclusions Together, these observations highlight the potential use of PW as a SOX2 inhibitor and the therapeutic relevance of targeting SOX2 to treat tamoxifen-resistant breast cancer.
publishDate 2024
dc.date.none.fl_str_mv 2024
2024
2024
dc.type.none.fl_str_mv info:eu-repo/semantics/article
format article
dc.identifier.none.fl_str_mv http://hdl.handle.net/10810/69470
url http://hdl.handle.net/10810/69470
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv info:eu-repo/grantAgreement/MICINN/PID2022-139530NB-I00/
info:eu-repo/grantAgreement/MICINN/CEX2021-001136-S/
info:eu-repo/grantAgreement/MICINN/PID2020-118464RB-I00/
info:eu-repo/grantAgreement/MICINN/PID2020-117649RB-100/
https://biosignaling.biomedcentral.com/articles/10.1186/s12964-024-01800-w
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
http://creativecommons.org/licenses/by-nc-nd/3.0/es/
Atribución-NoComercial-SinDerivadas 3.0 España
eu_rights_str_mv openAccess
rights_invalid_str_mv http://creativecommons.org/licenses/by-nc-nd/3.0/es/
Atribución-NoComercial-SinDerivadas 3.0 España
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv BMC
publisher.none.fl_str_mv BMC
dc.source.none.fl_str_mv reponame:Addi. Archivo Digital para la Docencia y la Investigación
instname:Universidad del País Vasco
instname_str Universidad del País Vasco
reponame_str Addi. Archivo Digital para la Docencia y la Investigación
collection Addi. Archivo Digital para la Docencia y la Investigación
repository.name.fl_str_mv
repository.mail.fl_str_mv
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spelling Polyoxometalate inhibition of SOX2-mediated tamoxifen resistance in breast cancerAurrekoetxea Rodríguez, IskanderLee, So YoungRabano, MiriamGris Cárdenas, IsabelGamboa Aldecoa, VirginiaGorroño, IrantzuRamella Gal, IsabellaParry, ConnorKypta, Robert M.Artetxe Arretxe, BeñatGutiérrez Zorrilla López, Juan ManuelVivanco Ruiz, María del Marbreast cancercancer stem cellsresistancehormone therapySOX2 inhibitionpolyoxometalateBackground Increased cancer stem cell (CSC) content and SOX2 overexpression are common features in the development of resistance to therapy in hormone-dependent breast cancer, which remains an important clinical challenge. SOX2 has potential as biomarker of resistance to treatment and as therapeutic target, but targeting transcription factors is also challenging. Here, we examine the potential inhibitory effect of different polyoxometalate (POM) derivatives on SOX2 transcription factor in tamoxifen-resistant breast cancer cells. Methods Various POM derivatives were synthesised and characterised by infrared spectra, powder X-ray diffraction pattern and nuclear magnetic resonance spectroscopy. Estrogen receptor (ER) positive breast cancer cells, and their counterparts, which have developed resistance to the hormone therapy tamoxifen, were treated with POMs and their consequences assessed by gel retardation and chromatin immunoprecipitation to determine SOX2 binding to DNA. Effects on proliferation, migration, invasion and tumorigenicity were monitored and quantified using microscopy, clone formation, transwell, wound healing assays, flow cytometry and in vivo chick chorioallantoic membrane (CAM) models. Generation of lentiviral stable gene silencing and gene knock-out using CRISPR-Cas9 genome editing were applied to validate the inhibitory effects of the selected POM. Cancer stem cell subpopulations were quantified by mammosphere formation assays, ALDEFLUOR activity and CD44/CD24 stainings. Flow cytometry and western blotting were used to measure reactive oxygen species (ROS) and apoptosis. Results POMs blocked in vitro binding activity of endogenous SOX2. [P2W18O62]6− (PW) Wells-Dawson-type anion was the most effective at inhibiting proliferation in various cell line models of tamoxifen resistance. 10 µM PW also reduced cancer cell migration and invasion, as well as SNAI2 expression levels. Treatment of tamoxifen-resistant cells with PW impaired tumour formation by reducing CSC content, in a SOX2-dependent manner, which led to stem cell depletion in vivo. Mechanistically, PW induced formation of reactive oxygen species (ROS) and inhibited Bcl-2, leading to the death of tamoxifen-resistant cells. PW-treated tamoxifen-resistant cells showed restored sensitivity to tamoxifen. Conclusions Together, these observations highlight the potential use of PW as a SOX2 inhibitor and the therapeutic relevance of targeting SOX2 to treat tamoxifen-resistant breast cancer.The authors thank grant support from the Basque Government (IT1722-22 and Elkartek KK-2022/00045) and Spanish Ministry of Science, Innovation and Universities (MICINN, grant PID2022-139530NB-I00) (JMGZ). This research was also funded by Elkartek (KK-2022/00045) by the Basque Government (MdMV), and by the Spanish Ministry of Science and Innovation MCIN/AEI/https://doi.org/10.13039/501100011033 (to MdMV and RK: CEX2021-001136-S; PRE2018-087073 to IG; PID2020-118464RB-I00 to MdMV, and PID2020-117649RB-100 to RK).BMC202420242024info:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10810/69470reponame:Addi. Archivo Digital para la Docencia y la Investigacióninstname:Universidad del País VascoInglésinfo:eu-repo/grantAgreement/MICINN/PID2022-139530NB-I00/info:eu-repo/grantAgreement/MICINN/CEX2021-001136-S/info:eu-repo/grantAgreement/MICINN/PID2020-118464RB-I00/info:eu-repo/grantAgreement/MICINN/PID2020-117649RB-100/https://biosignaling.biomedcentral.com/articles/10.1186/s12964-024-01800-winfo:eu-repo/semantics/openAccesshttp://creativecommons.org/licenses/by-nc-nd/3.0/es/© The Author(s) 2024. This article is licensed under a Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License, which permits any non-commercial use, sharing, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if you modified the licensed material. You do not have permission under this licence to share adapted material derived from this article or parts of it. The images or other third party material in this article are included in the article’s Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by-nc-nd/4.0/.Atribución-NoComercial-SinDerivadas 3.0 Españaoai:addi.ehu.eus:10810/694702026-06-18T09:23:17Z
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