Efficacy of CHK inhibitors as single agents in MYC-driven lymphoma cells
Abstract
CHK1 and CHK2 function as effectors of cell cycle checkpoint arrest following DNA damage. Small molecule inhibitors of CHK proteins are under clinical evaluation in combination with chemotherapeutic agents known to induce DNA damage. We examined whether CHK inhibitors could be effective as single agents in malignant cells with inherent DNA damage because of deregulated expression of the oncogene c-Myc. Eμ-myc lymphoma cells showed a dramatic increase in the extent of DNA damage and DNA damage response (DDR) signalling within 1 h of treatment with CHK1 inhibitors followed by caspase-dependent apoptosis and cell death. In p53 wild-type/ARF null Eμ-myc lymphoma cells, apoptotic cell death was preceded by accumulation of DNA damage and the amount of DNA damage correlated with the extent of cell death. This effect was not observed in normal B cells indicating that DNA damage accumulation following CHK inhibition was specific to Eμ-myc lymphoma cells that exhibit inherent DNA damage because of MYC-induced replication stress. Similar results were obtained with another structurally distinct CHK-inhibitor. Eμ-myc p53 null lymphoma cells were more sensitive to a dual CHK1/CHK2 inhibitor than to a CHK1-specific inhibitor. In all cases, the level of DNA damage following treatment was the most consistent indicator of drug sensitivity. Our results suggest that CHK inhibitors would be beneficial therapeutic agents in MYC-driven cancers. We propose that inhibitors of CHK can act in a synthetically lethal manner in cancers with replication stress as a result of these cancers being reliant on CHK proteins for an effective DDR and cell survival.
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CHK1 inhibitors and glutaminase inhibitors are considered potential candidates for treating Myc-overexpressing cancers.
“Similarly, checkpoint kinase 1 (CHK1) inhibitors625–627 and glutaminase (GLS) inhibitors628–634 are also considered potential candidates for treating Myc-overexpressing cancers.”
From Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials (2023) · cites this paper as [627]
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- Authors
- Ferrao, P. T., Bukczynska, E. P., Johnstone, R. W., & McArthur, G. A.
- Affiliations
- Peter MacCallum Cancer Centre (AU)
- The University of Melbourne (AU)
- Corresponding author
- Ferrao, P T
- Venue
- Oncogene
- Published
- 2011-08-15
- Volume
- 31
- Issue
- 13
- Pages
- 1661-1672
- ISSN
- 0950-9232 (ISSN-L)
- 1476-5594
- OpenAlex
- W2072763778
- Cited by
- 133
- References
- 52
- Citations by year
- 2026: 2 · 2025: 2 · 2024: 3 · 2023: 7 · 2022: 7 · 2021: 7 · 2020: 8 · 2019: 7 · 2018: 14 · 2017: 9 · 2016: 10 · 2015: 17 · 2014: 14 · 2013: 13 · 2012: 11
- FWCI
- 5.19
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Oncogene (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Pfizer
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › DNA Repair Mechanisms
- Health Sciences › Medicine › Oncology › Cancer-related Molecular Pathways
- Health Sciences › Medicine › Pathology and Forensic Medicine › Lymphoma Diagnosis and Treatment
- Keywords
- Chk1, Chk2, MYC-driven lymphoma, Eμ-Myc lymphoma, DNA damage response, replication stress, synthetic lethality, p53, caspase-dependent apoptosis, cell cycle checkpoints, monotherapy, drug sensitivity
- MeSH terms
- Checkpoint Kinase 1, Animals, Benzodiazepinones, DNA Damage, Humans, Lymphoma, Mice, Inbred C57BL, Mice, Transgenic, Neoplasm Transplantation, Protein Kinases, Pyrazoles, Genes, p53, Genes, myc, Apoptosis, Caspases, Cell Line, Tumor, Mice
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