Targeting Chk1 and Wee1 kinases enhances radiosensitivity of 2D and 3D head and neck cancer models to X-rays and low/high-LET protons

Abstract Ionising radiation causes the introduction of DNA damage, more specifically double strand breaks (DSBs) and complex DNA damage (CDD), that induces cancer cell death leading to the therapeutic effect. To combat this, cells activate arrest at the G2/M checkpoint to allow for effective DNA dam...

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Main Authors: Emma Melia, Anne-Sophie Fisch, Ingeborg Tinhofer, Jason L. Parsons
Format: Article
Language:English
Published: Nature Publishing Group 2025-02-01
Series:Cell Death and Disease
Online Access:https://doi.org/10.1038/s41419-025-07435-0
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author Emma Melia
Anne-Sophie Fisch
Ingeborg Tinhofer
Jason L. Parsons
author_facet Emma Melia
Anne-Sophie Fisch
Ingeborg Tinhofer
Jason L. Parsons
author_sort Emma Melia
collection DOAJ
description Abstract Ionising radiation causes the introduction of DNA damage, more specifically double strand breaks (DSBs) and complex DNA damage (CDD), that induces cancer cell death leading to the therapeutic effect. To combat this, cells activate arrest at the G2/M checkpoint to allow for effective DNA damage repair, coordinated by the Chk1 and Wee1 protein kinases. Therefore, Chk1 and Wee1 are considered promising therapeutic targets to enhance the effectiveness of radiotherapy in cancer cell killing. Here, we have analysed the response of head and neck squamous cell carcinoma (HNSCC) cell lines, spheroids and patient-derived organoids to X-rays and proton beam therapy (PBT) in the presence of either a Chk1 (MK-8776) or a Wee1 (MK-1775) inhibitor. We demonstrate that inhibitors of Chk1 or Wee1 can significantly enhance the radiosensitivity of both 2D and 3D models of HNSCC to X-rays and PBT (performed at both low and high ionisation densities), and that this effect is caused through abrogation of the G2/M checkpoint causing the persistence of DSBs. Our results therefore suggest that targeting Chk1 and Wee1 kinases in combination with X-rays and PBT could represent a promising therapeutic avenue to enhance the clinical efficacy of HNSCC treatment.
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series Cell Death and Disease
spelling doaj-art-4f5eb0adcd624a998a740c896bb913b32025-08-20T03:03:51ZengNature Publishing GroupCell Death and Disease2041-48892025-02-0116111010.1038/s41419-025-07435-0Targeting Chk1 and Wee1 kinases enhances radiosensitivity of 2D and 3D head and neck cancer models to X-rays and low/high-LET protonsEmma Melia0Anne-Sophie Fisch1Ingeborg Tinhofer2Jason L. Parsons3Department of Cancer and Genomic Sciences, University of Birmingham, EdgbastonDepartment of Radiooncology and Radiotherapy, Translational Radiation Oncology Research Laboratory, Charité – Universitätsmedizin Berlin, corporate member of Freie Universität Berlin and Humboldt Universität zu BerlinDepartment of Radiooncology and Radiotherapy, Translational Radiation Oncology Research Laboratory, Charité – Universitätsmedizin Berlin, corporate member of Freie Universität Berlin and Humboldt Universität zu BerlinDepartment of Cancer and Genomic Sciences, University of Birmingham, EdgbastonAbstract Ionising radiation causes the introduction of DNA damage, more specifically double strand breaks (DSBs) and complex DNA damage (CDD), that induces cancer cell death leading to the therapeutic effect. To combat this, cells activate arrest at the G2/M checkpoint to allow for effective DNA damage repair, coordinated by the Chk1 and Wee1 protein kinases. Therefore, Chk1 and Wee1 are considered promising therapeutic targets to enhance the effectiveness of radiotherapy in cancer cell killing. Here, we have analysed the response of head and neck squamous cell carcinoma (HNSCC) cell lines, spheroids and patient-derived organoids to X-rays and proton beam therapy (PBT) in the presence of either a Chk1 (MK-8776) or a Wee1 (MK-1775) inhibitor. We demonstrate that inhibitors of Chk1 or Wee1 can significantly enhance the radiosensitivity of both 2D and 3D models of HNSCC to X-rays and PBT (performed at both low and high ionisation densities), and that this effect is caused through abrogation of the G2/M checkpoint causing the persistence of DSBs. Our results therefore suggest that targeting Chk1 and Wee1 kinases in combination with X-rays and PBT could represent a promising therapeutic avenue to enhance the clinical efficacy of HNSCC treatment.https://doi.org/10.1038/s41419-025-07435-0
spellingShingle Emma Melia
Anne-Sophie Fisch
Ingeborg Tinhofer
Jason L. Parsons
Targeting Chk1 and Wee1 kinases enhances radiosensitivity of 2D and 3D head and neck cancer models to X-rays and low/high-LET protons
Cell Death and Disease
title Targeting Chk1 and Wee1 kinases enhances radiosensitivity of 2D and 3D head and neck cancer models to X-rays and low/high-LET protons
title_full Targeting Chk1 and Wee1 kinases enhances radiosensitivity of 2D and 3D head and neck cancer models to X-rays and low/high-LET protons
title_fullStr Targeting Chk1 and Wee1 kinases enhances radiosensitivity of 2D and 3D head and neck cancer models to X-rays and low/high-LET protons
title_full_unstemmed Targeting Chk1 and Wee1 kinases enhances radiosensitivity of 2D and 3D head and neck cancer models to X-rays and low/high-LET protons
title_short Targeting Chk1 and Wee1 kinases enhances radiosensitivity of 2D and 3D head and neck cancer models to X-rays and low/high-LET protons
title_sort targeting chk1 and wee1 kinases enhances radiosensitivity of 2d and 3d head and neck cancer models to x rays and low high let protons
url https://doi.org/10.1038/s41419-025-07435-0
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