Inhibiting the RNA helicase DDX3X in Burkitt lymphoma induces oxydative stress and impedes tumor progression in xenografts

IntroductionBurkitt Lymphoma (BL), an aggressive B-cell lymphoma driven by MYC translocations, requires intensive chemotherapy treatments which deliver high effectiveness yet increase future risks of developing secondary malignancies. We have previously shown that DDX3X, an RNA helicase frequently m...

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Main Authors: Hugues Beauchemin, Zeinab Dalloul, Eva-Maria Piskor, Virginie Calderon, Andrew Chatr-aryamontri, Thierry Bertomeu, Tarik Möröy
Format: Article
Language:English
Published: Frontiers Media S.A. 2025-07-01
Series:Frontiers in Cell and Developmental Biology
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Online Access:https://www.frontiersin.org/articles/10.3389/fcell.2025.1642006/full
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author Hugues Beauchemin
Zeinab Dalloul
Eva-Maria Piskor
Eva-Maria Piskor
Virginie Calderon
Andrew Chatr-aryamontri
Thierry Bertomeu
Tarik Möröy
Tarik Möröy
Tarik Möröy
author_facet Hugues Beauchemin
Zeinab Dalloul
Eva-Maria Piskor
Eva-Maria Piskor
Virginie Calderon
Andrew Chatr-aryamontri
Thierry Bertomeu
Tarik Möröy
Tarik Möröy
Tarik Möröy
author_sort Hugues Beauchemin
collection DOAJ
description IntroductionBurkitt Lymphoma (BL), an aggressive B-cell lymphoma driven by MYC translocations, requires intensive chemotherapy treatments which deliver high effectiveness yet increase future risks of developing secondary malignancies. We have previously shown that DDX3X, an RNA helicase frequently mutated in BL, is essential for B cell lymphomagenesis in mice.Methods and resultsTo assess if DDX3X could therefore represent a promising therapeutic target for BL, we tested two DDX3X inhibitors, the well characterized RK-33 and the more potent newly developed C1, in three BL cell lines (CA46, Raji, Daudi). We found that the 3 cell lines exhibited differential sensitivities to the drugs in vitro, with Daudi being the most susceptible and Raji the most resistant. In vivo, RK-33 treatment in a xenograft BL model reduced tumor progression in all cell lines, albeit with variable efficacy compared to the clinical drug Pevonedistat, and again with the Daudi cells being the most responsive to the treatment. Transcriptomic and proteomic analyses indicated that RK-33-mediated inhibition of DDX3X, and DDX3X ablation through siRNA affects oxidative phosphorylation among other pathways and leads to an increase of intracellular reactive oxygen species (ROS). A CRISPR chemogenomic screen to identify synthetic lethalities linked to RK-33 implicated enzymes of the glutathione synthesis pathway and the Keap1-Nrf2-ARE pathway. We therefore tested the inhibition of the glutathione pathway with buthionine sulfoximine and showed that it reduced the CC50 of RK-33 in BL cells lines.ConclusionOur findings not only support DDX3X as a therapeutic target in BL but also provide evidence for a combinatorial treatment strategy to improve the efficacy of current treatments.
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spelling doaj-art-cab8bdd9bcf345d6b14a92af67fa8f792025-08-20T03:25:27ZengFrontiers Media S.A.Frontiers in Cell and Developmental Biology2296-634X2025-07-011310.3389/fcell.2025.16420061642006Inhibiting the RNA helicase DDX3X in Burkitt lymphoma induces oxydative stress and impedes tumor progression in xenograftsHugues Beauchemin0Zeinab Dalloul1Eva-Maria Piskor2Eva-Maria Piskor3Virginie Calderon4Andrew Chatr-aryamontri5Thierry Bertomeu6Tarik Möröy7Tarik Möröy8Tarik Möröy9Institut de Recherches Cliniques de Montréal (IRCM), Université de Montréal, Montréal, QC, CanadaInstitut de Recherches Cliniques de Montréal (IRCM), Université de Montréal, Montréal, QC, CanadaInstitut de Recherches Cliniques de Montréal (IRCM), Université de Montréal, Montréal, QC, CanadaDepartment of Medicine, Division of Clinical and Translational Research, McGill University, Montreal, QC, CanadaInstitut de Recherches Cliniques de Montréal (IRCM), Université de Montréal, Montréal, QC, CanadaThe ChemoGenix Platform, Institut de Recherche en Immunologie et Cancer (IRIC), Université de Montréal, Montreal, QC, CanadaThe ChemoGenix Platform, Institut de Recherche en Immunologie et Cancer (IRIC), Université de Montréal, Montreal, QC, CanadaInstitut de Recherches Cliniques de Montréal (IRCM), Université de Montréal, Montréal, QC, CanadaDepartment of Medicine, Division of Clinical and Translational Research, McGill University, Montreal, QC, CanadaDépartement de Microbiologie, Infectiologie et Immunologie, Faculty of Medicine, Université de Montréal, Montreal, QC, CanadaIntroductionBurkitt Lymphoma (BL), an aggressive B-cell lymphoma driven by MYC translocations, requires intensive chemotherapy treatments which deliver high effectiveness yet increase future risks of developing secondary malignancies. We have previously shown that DDX3X, an RNA helicase frequently mutated in BL, is essential for B cell lymphomagenesis in mice.Methods and resultsTo assess if DDX3X could therefore represent a promising therapeutic target for BL, we tested two DDX3X inhibitors, the well characterized RK-33 and the more potent newly developed C1, in three BL cell lines (CA46, Raji, Daudi). We found that the 3 cell lines exhibited differential sensitivities to the drugs in vitro, with Daudi being the most susceptible and Raji the most resistant. In vivo, RK-33 treatment in a xenograft BL model reduced tumor progression in all cell lines, albeit with variable efficacy compared to the clinical drug Pevonedistat, and again with the Daudi cells being the most responsive to the treatment. Transcriptomic and proteomic analyses indicated that RK-33-mediated inhibition of DDX3X, and DDX3X ablation through siRNA affects oxidative phosphorylation among other pathways and leads to an increase of intracellular reactive oxygen species (ROS). A CRISPR chemogenomic screen to identify synthetic lethalities linked to RK-33 implicated enzymes of the glutathione synthesis pathway and the Keap1-Nrf2-ARE pathway. We therefore tested the inhibition of the glutathione pathway with buthionine sulfoximine and showed that it reduced the CC50 of RK-33 in BL cells lines.ConclusionOur findings not only support DDX3X as a therapeutic target in BL but also provide evidence for a combinatorial treatment strategy to improve the efficacy of current treatments.https://www.frontiersin.org/articles/10.3389/fcell.2025.1642006/fullRNA helicaseDDX3 as a potential targetBurkitt lymphoma (BL)DDX3 inhibitorxenograftATP-dependent RNA helicase
spellingShingle Hugues Beauchemin
Zeinab Dalloul
Eva-Maria Piskor
Eva-Maria Piskor
Virginie Calderon
Andrew Chatr-aryamontri
Thierry Bertomeu
Tarik Möröy
Tarik Möröy
Tarik Möröy
Inhibiting the RNA helicase DDX3X in Burkitt lymphoma induces oxydative stress and impedes tumor progression in xenografts
Frontiers in Cell and Developmental Biology
RNA helicase
DDX3 as a potential target
Burkitt lymphoma (BL)
DDX3 inhibitor
xenograft
ATP-dependent RNA helicase
title Inhibiting the RNA helicase DDX3X in Burkitt lymphoma induces oxydative stress and impedes tumor progression in xenografts
title_full Inhibiting the RNA helicase DDX3X in Burkitt lymphoma induces oxydative stress and impedes tumor progression in xenografts
title_fullStr Inhibiting the RNA helicase DDX3X in Burkitt lymphoma induces oxydative stress and impedes tumor progression in xenografts
title_full_unstemmed Inhibiting the RNA helicase DDX3X in Burkitt lymphoma induces oxydative stress and impedes tumor progression in xenografts
title_short Inhibiting the RNA helicase DDX3X in Burkitt lymphoma induces oxydative stress and impedes tumor progression in xenografts
title_sort inhibiting the rna helicase ddx3x in burkitt lymphoma induces oxydative stress and impedes tumor progression in xenografts
topic RNA helicase
DDX3 as a potential target
Burkitt lymphoma (BL)
DDX3 inhibitor
xenograft
ATP-dependent RNA helicase
url https://www.frontiersin.org/articles/10.3389/fcell.2025.1642006/full
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