The synergistic effect of DZ‑NEP, panobinostat and temozolomide reduces clonogenicity and induces apoptosis in glioblastoma cells

Current treatment against glioblastoma consists of surgical resection followed by temozolomide, with or without combined radiotherapy. Glioblastoma frequently acquires resistance to chemotherapy and/or radiotherapy. Novel therapeutic approaches are thus required. The inhibition of enhancer of zeste...

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Autores: De-La-Rosa, J. (Javier)|||/items/d420f6f9-e470-4a26-8fb9-4c419c32a40a, Urdiciain-Ezpeleta, A. (Alejandro)|||/items/7173bee2-0d3d-4431-a892-d92d60c667b0, Zazpe, I. (Idoya)|||/items/0b5eae6f-50f8-41ed-a4c6-d0c071a44858, Zelaya, M.V. (María Victoria)|||/items/b17ebd92-1f01-4512-b71f-4f05874ca7b3, Meléndez, B. (Bárbara)|||/items/9c1f8587-8f9d-4f08-b10e-91b3670a0ffc, Rey, J.A. (Juan A.)|||/items/b33f46ba-e920-49a9-af7e-1d6566759c16, Idoate, M.A. (Miguel Ángel)|||/items/7b905180-f34f-450d-934f-8bf7652f84d3, Saez-Castresana, J. (Javier)|||/items/52f31ab0-8555-470d-af21-e677a1b3eff8
Tipo de recurso: artículo
Fecha de publicación:2020
País:España
Institución:Universidad de Navarra
Repositorio:Dadun. Depósito Académico Digital de la Universidad de Navarra
Idioma:inglés
OAI Identifier:oai:dadun.unav.edu:10171/68389
Acceso en línea:https://hdl.handle.net/10171/68389
Access Level:acceso abierto
Palabra clave:3-deazaneplanocin A
Epigenetics
Enhancer of zeste homolog 2
Glioblastoma
Histone deacetylase
Panobinostat
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spelling The synergistic effect of DZ‑NEP, panobinostat and temozolomide reduces clonogenicity and induces apoptosis in glioblastoma cellsDe-La-Rosa, J. (Javier)|||/items/d420f6f9-e470-4a26-8fb9-4c419c32a40aUrdiciain-Ezpeleta, A. (Alejandro)|||/items/7173bee2-0d3d-4431-a892-d92d60c667b0Zazpe, I. (Idoya)|||/items/0b5eae6f-50f8-41ed-a4c6-d0c071a44858Zelaya, M.V. (María Victoria)|||/items/b17ebd92-1f01-4512-b71f-4f05874ca7b3Meléndez, B. (Bárbara)|||/items/9c1f8587-8f9d-4f08-b10e-91b3670a0ffcRey, J.A. (Juan A.)|||/items/b33f46ba-e920-49a9-af7e-1d6566759c16Idoate, M.A. (Miguel Ángel)|||/items/7b905180-f34f-450d-934f-8bf7652f84d3Saez-Castresana, J. (Javier)|||/items/52f31ab0-8555-470d-af21-e677a1b3eff83-deazaneplanocin AEpigeneticsEnhancer of zeste homolog 2GlioblastomaHistone deacetylasePanobinostatCurrent treatment against glioblastoma consists of surgical resection followed by temozolomide, with or without combined radiotherapy. Glioblastoma frequently acquires resistance to chemotherapy and/or radiotherapy. Novel therapeutic approaches are thus required. The inhibition of enhancer of zeste homolog 2 (EZH2; a histone methylase) and histone deacetylases (HDACs) are possible epigenetic treatments. Temozolomide, 3-deazaneplanocin A (DZ-Nep; an EZH2 inhibitor) and panobinostat (an HDAC inhibitor) were tested in regular and temozolomide-resistant glioblastoma cells to confirm whether the compounds could behave in a synergistic, additive or antagonistic manner. A total of six commercial cell lines, two temozolomide-induced resistant cell lines and two primary cultures derived from glioblastoma samples were used. Cell lines were exposed to single treatments of the drugs in addition to all possible two- and three-drug combinations. Colony formation assays, synergistic assays and reverse transcription-quantitative PCR analysis of apoptosis-associated genes were performed. The highest synergistic combination was DZ-Nep + panobinostat. Triple treatment was also synergistic. Reduced clonogenicity and increased apoptosis were both induced. It was concluded that the therapeutic potential of the combination of these three drugs in glioblastoma was evident and should be further explored.Spandidos publicationsDadun. Depósito Académico Digital Universidad de Navarra20242024-01-1720202020-01-0120202020-01-01journal articlehttp://purl.org/coar/resource_type/c_6501info:eu-repo/semantics/articleapplication/pdfhttps://hdl.handle.net/10171/68389reponame:Dadun. Depósito Académico Digital de la Universidad de Navarrainstname:Universidad de NavarraInglésengopen accesshttp://purl.org/coar/access_right/c_abf2info:eu-repo/semantics/openAccessoai:dadun.unav.edu:10171/683892026-06-21T12:47:57Z
dc.title.none.fl_str_mv The synergistic effect of DZ‑NEP, panobinostat and temozolomide reduces clonogenicity and induces apoptosis in glioblastoma cells
title The synergistic effect of DZ‑NEP, panobinostat and temozolomide reduces clonogenicity and induces apoptosis in glioblastoma cells
spellingShingle The synergistic effect of DZ‑NEP, panobinostat and temozolomide reduces clonogenicity and induces apoptosis in glioblastoma cells
De-La-Rosa, J. (Javier)|||/items/d420f6f9-e470-4a26-8fb9-4c419c32a40a
3-deazaneplanocin A
Epigenetics
Enhancer of zeste homolog 2
Glioblastoma
Histone deacetylase
Panobinostat
title_short The synergistic effect of DZ‑NEP, panobinostat and temozolomide reduces clonogenicity and induces apoptosis in glioblastoma cells
title_full The synergistic effect of DZ‑NEP, panobinostat and temozolomide reduces clonogenicity and induces apoptosis in glioblastoma cells
title_fullStr The synergistic effect of DZ‑NEP, panobinostat and temozolomide reduces clonogenicity and induces apoptosis in glioblastoma cells
title_full_unstemmed The synergistic effect of DZ‑NEP, panobinostat and temozolomide reduces clonogenicity and induces apoptosis in glioblastoma cells
title_sort The synergistic effect of DZ‑NEP, panobinostat and temozolomide reduces clonogenicity and induces apoptosis in glioblastoma cells
dc.creator.none.fl_str_mv De-La-Rosa, J. (Javier)|||/items/d420f6f9-e470-4a26-8fb9-4c419c32a40a
Urdiciain-Ezpeleta, A. (Alejandro)|||/items/7173bee2-0d3d-4431-a892-d92d60c667b0
Zazpe, I. (Idoya)|||/items/0b5eae6f-50f8-41ed-a4c6-d0c071a44858
Zelaya, M.V. (María Victoria)|||/items/b17ebd92-1f01-4512-b71f-4f05874ca7b3
Meléndez, B. (Bárbara)|||/items/9c1f8587-8f9d-4f08-b10e-91b3670a0ffc
Rey, J.A. (Juan A.)|||/items/b33f46ba-e920-49a9-af7e-1d6566759c16
Idoate, M.A. (Miguel Ángel)|||/items/7b905180-f34f-450d-934f-8bf7652f84d3
Saez-Castresana, J. (Javier)|||/items/52f31ab0-8555-470d-af21-e677a1b3eff8
author De-La-Rosa, J. (Javier)|||/items/d420f6f9-e470-4a26-8fb9-4c419c32a40a
author_facet De-La-Rosa, J. (Javier)|||/items/d420f6f9-e470-4a26-8fb9-4c419c32a40a
Urdiciain-Ezpeleta, A. (Alejandro)|||/items/7173bee2-0d3d-4431-a892-d92d60c667b0
Zazpe, I. (Idoya)|||/items/0b5eae6f-50f8-41ed-a4c6-d0c071a44858
Zelaya, M.V. (María Victoria)|||/items/b17ebd92-1f01-4512-b71f-4f05874ca7b3
Meléndez, B. (Bárbara)|||/items/9c1f8587-8f9d-4f08-b10e-91b3670a0ffc
Rey, J.A. (Juan A.)|||/items/b33f46ba-e920-49a9-af7e-1d6566759c16
Idoate, M.A. (Miguel Ángel)|||/items/7b905180-f34f-450d-934f-8bf7652f84d3
Saez-Castresana, J. (Javier)|||/items/52f31ab0-8555-470d-af21-e677a1b3eff8
author_role author
author2 Urdiciain-Ezpeleta, A. (Alejandro)|||/items/7173bee2-0d3d-4431-a892-d92d60c667b0
Zazpe, I. (Idoya)|||/items/0b5eae6f-50f8-41ed-a4c6-d0c071a44858
Zelaya, M.V. (María Victoria)|||/items/b17ebd92-1f01-4512-b71f-4f05874ca7b3
Meléndez, B. (Bárbara)|||/items/9c1f8587-8f9d-4f08-b10e-91b3670a0ffc
Rey, J.A. (Juan A.)|||/items/b33f46ba-e920-49a9-af7e-1d6566759c16
Idoate, M.A. (Miguel Ángel)|||/items/7b905180-f34f-450d-934f-8bf7652f84d3
Saez-Castresana, J. (Javier)|||/items/52f31ab0-8555-470d-af21-e677a1b3eff8
author2_role author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Dadun. Depósito Académico Digital Universidad de Navarra
dc.subject.none.fl_str_mv 3-deazaneplanocin A
Epigenetics
Enhancer of zeste homolog 2
Glioblastoma
Histone deacetylase
Panobinostat
topic 3-deazaneplanocin A
Epigenetics
Enhancer of zeste homolog 2
Glioblastoma
Histone deacetylase
Panobinostat
description Current treatment against glioblastoma consists of surgical resection followed by temozolomide, with or without combined radiotherapy. Glioblastoma frequently acquires resistance to chemotherapy and/or radiotherapy. Novel therapeutic approaches are thus required. The inhibition of enhancer of zeste homolog 2 (EZH2; a histone methylase) and histone deacetylases (HDACs) are possible epigenetic treatments. Temozolomide, 3-deazaneplanocin A (DZ-Nep; an EZH2 inhibitor) and panobinostat (an HDAC inhibitor) were tested in regular and temozolomide-resistant glioblastoma cells to confirm whether the compounds could behave in a synergistic, additive or antagonistic manner. A total of six commercial cell lines, two temozolomide-induced resistant cell lines and two primary cultures derived from glioblastoma samples were used. Cell lines were exposed to single treatments of the drugs in addition to all possible two- and three-drug combinations. Colony formation assays, synergistic assays and reverse transcription-quantitative PCR analysis of apoptosis-associated genes were performed. The highest synergistic combination was DZ-Nep + panobinostat. Triple treatment was also synergistic. Reduced clonogenicity and increased apoptosis were both induced. It was concluded that the therapeutic potential of the combination of these three drugs in glioblastoma was evident and should be further explored.
publishDate 2020
dc.date.none.fl_str_mv 2020
2020-01-01
2020
2020-01-01
2024
2024-01-17
dc.type.none.fl_str_mv journal article
http://purl.org/coar/resource_type/c_6501
dc.type.openaire.fl_str_mv info:eu-repo/semantics/article
format article
dc.identifier.none.fl_str_mv https://hdl.handle.net/10171/68389
url https://hdl.handle.net/10171/68389
dc.language.none.fl_str_mv Inglés
eng
language_invalid_str_mv Inglés
language eng
dc.rights.none.fl_str_mv open access
http://purl.org/coar/access_right/c_abf2
dc.rights.openaire.fl_str_mv info:eu-repo/semantics/openAccess
rights_invalid_str_mv open access
http://purl.org/coar/access_right/c_abf2
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Spandidos publications
publisher.none.fl_str_mv Spandidos publications
dc.source.none.fl_str_mv reponame:Dadun. Depósito Académico Digital de la Universidad de Navarra
instname:Universidad de Navarra
instname_str Universidad de Navarra
reponame_str Dadun. Depósito Académico Digital de la Universidad de Navarra
collection Dadun. Depósito Académico Digital de la Universidad de Navarra
repository.name.fl_str_mv
repository.mail.fl_str_mv
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