Androgen receptor inhibition sensitizes glioblastoma stem cells to temozolomide by the miR-1/miR-26a-1/miR-487b signature mediated WT1 and FOXA1 silencing

Abstract Glioblastomas (GBMs) are aggressive brain tumors and challenging cancers for diagnosis and treatment. Therapeutic options include surgery followed by chemotherapy with the DNA alkylator temozolomide (TMZ) and radiotherapy. However, the patient's prognosis remains poor due to tumor hete...

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Main Authors: Ana Belén Díaz Méndez, Marta Di Giuliani, Andrea Sacconi, Elisa Tremante, Valentina Lulli, Marta Di Martile, Giulia Vari, Francesca De Bacco, Carla Boccaccio, Giulia Regazzo, Maria Giulia Rizzo
Format: Article
Language:English
Published: Nature Publishing Group 2025-05-01
Series:Cell Death Discovery
Online Access:https://doi.org/10.1038/s41420-025-02517-6
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author Ana Belén Díaz Méndez
Marta Di Giuliani
Andrea Sacconi
Elisa Tremante
Valentina Lulli
Marta Di Martile
Giulia Vari
Francesca De Bacco
Carla Boccaccio
Giulia Regazzo
Maria Giulia Rizzo
author_facet Ana Belén Díaz Méndez
Marta Di Giuliani
Andrea Sacconi
Elisa Tremante
Valentina Lulli
Marta Di Martile
Giulia Vari
Francesca De Bacco
Carla Boccaccio
Giulia Regazzo
Maria Giulia Rizzo
author_sort Ana Belén Díaz Méndez
collection DOAJ
description Abstract Glioblastomas (GBMs) are aggressive brain tumors and challenging cancers for diagnosis and treatment. Therapeutic options include surgery followed by chemotherapy with the DNA alkylator temozolomide (TMZ) and radiotherapy. However, the patient's prognosis remains poor due to tumor heterogeneity, cell infiltration and intrinsic or acquired resistance to therapy. Understanding the resistance mechanisms together with identifying new biomarkers are crucial for developing novel therapeutic strategies. MiRNAs play an important role in the biology of gliomas, they modulate tumorigenesis and therapy response. We recently identified the diagnostic/prognostic miR-1-3p, miR-26a-1-3p and miR-487b-3p signature that displays an oncosuppressive role on several glioma biological functions. In this study, we investigated the effects of the therapeutic potential of this three-miRNA signature as a regulator of response to TMZ. We found that ectopic expression of the miRNA signature in patient-derived GBM neurospheres treated with TMZ impaired cell proliferation and viability by necroptosis induction. Moreover, we identified WT1 and FOXA1, two transcription factors specifically involved in TMZ resistance, as novel direct targets of the miRNA signature. Of note, the repression of WT1 and FOXA1, elicited by the signature, caused a downregulation of the Androgen Receptor (AR) expression, an impairment of tumor-spheroid formation and reversed cancer cell stemness. These results were recapitulated using the AR inhibitor enzalutamide, confirming the involvement of the AR pathway. Our data indicate that the miR-1-3p/miR-26a-1-3p/miR-487b-3p signature, which has an impact on treatment response and cell stemness, may pave the way for miRNA-based complementary therapies in GBM patients.
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spelling doaj-art-43a563d7d1594c0ba7691e266ac970bb2025-08-20T03:48:18ZengNature Publishing GroupCell Death Discovery2058-77162025-05-0111111010.1038/s41420-025-02517-6Androgen receptor inhibition sensitizes glioblastoma stem cells to temozolomide by the miR-1/miR-26a-1/miR-487b signature mediated WT1 and FOXA1 silencingAna Belén Díaz Méndez0Marta Di Giuliani1Andrea Sacconi2Elisa Tremante3Valentina Lulli4Marta Di Martile5Giulia Vari6Francesca De Bacco7Carla Boccaccio8Giulia Regazzo9Maria Giulia Rizzo10Department of Research, Advanced Diagnostics and Technological Innovation, Translational Oncology Research Unit, IRCCS Regina Elena National Cancer InstituteDepartment of Research, Advanced Diagnostics and Technological Innovation, Translational Oncology Research Unit, IRCCS Regina Elena National Cancer InstituteClinical Trial Center, Biostatistics and Bioinformatics Unit, IRCCS Regina Elena National Cancer InstituteDepartment of Research, Advanced Diagnostics and Technological Innovation, Translational Oncology Research Unit, IRCCS Regina Elena National Cancer InstituteDepartment of Oncology and Molecular Medicine, Istituto Superiore di SanitàPreclinical Models and New Therapeutic Agents Unit, IRCCS Regina Elena National Cancer InstituteDepartment of Research, Advanced Diagnostics and Technological Innovation, Translational Oncology Research Unit, IRCCS Regina Elena National Cancer InstituteLaboratory of Cancer Stem Cell Research, Candiolo Cancer Institute, FPO-IRCCSLaboratory of Cancer Stem Cell Research, Candiolo Cancer Institute, FPO-IRCCSDepartment of Research, Advanced Diagnostics and Technological Innovation, Translational Oncology Research Unit, IRCCS Regina Elena National Cancer InstituteDepartment of Research, Advanced Diagnostics and Technological Innovation, Translational Oncology Research Unit, IRCCS Regina Elena National Cancer InstituteAbstract Glioblastomas (GBMs) are aggressive brain tumors and challenging cancers for diagnosis and treatment. Therapeutic options include surgery followed by chemotherapy with the DNA alkylator temozolomide (TMZ) and radiotherapy. However, the patient's prognosis remains poor due to tumor heterogeneity, cell infiltration and intrinsic or acquired resistance to therapy. Understanding the resistance mechanisms together with identifying new biomarkers are crucial for developing novel therapeutic strategies. MiRNAs play an important role in the biology of gliomas, they modulate tumorigenesis and therapy response. We recently identified the diagnostic/prognostic miR-1-3p, miR-26a-1-3p and miR-487b-3p signature that displays an oncosuppressive role on several glioma biological functions. In this study, we investigated the effects of the therapeutic potential of this three-miRNA signature as a regulator of response to TMZ. We found that ectopic expression of the miRNA signature in patient-derived GBM neurospheres treated with TMZ impaired cell proliferation and viability by necroptosis induction. Moreover, we identified WT1 and FOXA1, two transcription factors specifically involved in TMZ resistance, as novel direct targets of the miRNA signature. Of note, the repression of WT1 and FOXA1, elicited by the signature, caused a downregulation of the Androgen Receptor (AR) expression, an impairment of tumor-spheroid formation and reversed cancer cell stemness. These results were recapitulated using the AR inhibitor enzalutamide, confirming the involvement of the AR pathway. Our data indicate that the miR-1-3p/miR-26a-1-3p/miR-487b-3p signature, which has an impact on treatment response and cell stemness, may pave the way for miRNA-based complementary therapies in GBM patients.https://doi.org/10.1038/s41420-025-02517-6
spellingShingle Ana Belén Díaz Méndez
Marta Di Giuliani
Andrea Sacconi
Elisa Tremante
Valentina Lulli
Marta Di Martile
Giulia Vari
Francesca De Bacco
Carla Boccaccio
Giulia Regazzo
Maria Giulia Rizzo
Androgen receptor inhibition sensitizes glioblastoma stem cells to temozolomide by the miR-1/miR-26a-1/miR-487b signature mediated WT1 and FOXA1 silencing
Cell Death Discovery
title Androgen receptor inhibition sensitizes glioblastoma stem cells to temozolomide by the miR-1/miR-26a-1/miR-487b signature mediated WT1 and FOXA1 silencing
title_full Androgen receptor inhibition sensitizes glioblastoma stem cells to temozolomide by the miR-1/miR-26a-1/miR-487b signature mediated WT1 and FOXA1 silencing
title_fullStr Androgen receptor inhibition sensitizes glioblastoma stem cells to temozolomide by the miR-1/miR-26a-1/miR-487b signature mediated WT1 and FOXA1 silencing
title_full_unstemmed Androgen receptor inhibition sensitizes glioblastoma stem cells to temozolomide by the miR-1/miR-26a-1/miR-487b signature mediated WT1 and FOXA1 silencing
title_short Androgen receptor inhibition sensitizes glioblastoma stem cells to temozolomide by the miR-1/miR-26a-1/miR-487b signature mediated WT1 and FOXA1 silencing
title_sort androgen receptor inhibition sensitizes glioblastoma stem cells to temozolomide by the mir 1 mir 26a 1 mir 487b signature mediated wt1 and foxa1 silencing
url https://doi.org/10.1038/s41420-025-02517-6
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