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    GENE:

    CHEK1 (Checkpoint kinase 1)

    i
    Other names: CHEK1, CHK1, Checkpoint kinase 1
    1d
    Synergistic Effects of DNA-PKcs Inhibition and Radiotherapy in Esophageal Squamous Cell Carcinoma. (PubMed, FASEB J)
    In vitro, ESCC cell lines (TE13 and Eca9706) were co-treated with DNA-dependent protein kinase catalytic subunit (DNA-PKcs) inhibitors (AZD7648 or NU7741) or PRKDC-targeting siRNA plus irradiation...Our study reveals a novel mechanism by which DNA-PKcs inhibition augments radiosensitivity in ESCC. Targeting DNA-PKcs could represent a promising strategy to improve the efficacy of radiotherapy in ESCC, offering a potential therapeutic approach to overcome radioresistance.
    Journal
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    CHEK2 (Checkpoint kinase 2) • CHEK1 (Checkpoint kinase 1) • CASP3 (Caspase 3) • CDK1 (Cyclin-dependent kinase 1) • PRKDC (Protein Kinase, DNA-Activated, Catalytic Subunit)
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    AZD7648
    3d
    Integrated Multi-Omics and Machine Learning Framework Identifies Diagnostic Signatures and Druggable Targets in Breast Cancer. (PubMed, Genes (Basel))
    The study identified CHEK1 as a key diagnostic gene for BC through 127 ML algorithms and SMR causal inference. By combining AI-assisted virtual screening and molecular docking, computational candidate compounds targeting CHEK1 were prioritized. These findings represent hypothesis-generating in silico predictions and require experimental validation before any therapeutic conclusions can be drawn.
    Journal • BRCA Biomarker • PARP Biomarker
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    BRCA1 (Breast cancer 1, early onset) • CD8 (cluster of differentiation 8) • BRCA (Breast cancer early onset) • CHEK1 (Checkpoint kinase 1) • KIF23 (Kinesin Family Member 23) • MIR15A (MicroRNA 15a)
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    Lynparza (olaparib) • LY294002
    3d
    Respiratory Models Reveal DNA Damage Response Modulation by Merkel Cell Polyomavirus. (PubMed, Int J Mol Sci)
    Viral infection induced an overexpression of DDR genes, suggesting a role of the virus in manipulating DDR to favor its replication or contribute to tumor progression. These preliminary results provide in vitro models for studying the interplay between MCPyV and DDR within malignant and non-malignant contexts across the respiratory tract, laying the basis for future research exploring the clinical relevance of DDR activation in virus-driven malignancies.
    Journal
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    ATM (ATM serine/threonine kinase) • CHEK2 (Checkpoint kinase 2) • RAD51 (RAD51 Homolog A) • CHEK1 (Checkpoint kinase 1) • CDKN1A (Cyclin-dependent kinase inhibitor 1A)
    3d
    Dynamics of Postmortem Gene Expression in Normal and Neoplastic Murine Liver. (PubMed, Life (Basel))
    This pattern developed despite formally adequate RNA quality (RQN) and the absence of clear signs of progressive autolysis in histology, indicating the insufficiency of standard quality criteria for detecting postmortem changes. These findings collectively underscore the critical importance of minimizing and controlling PMI during the biobanking of oncological samples for reliable transcriptomic research.
    Preclinical • Journal • BRCA Biomarker
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    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • CDK12 (Cyclin dependent kinase 12) • CHEK2 (Checkpoint kinase 2) • CHEK1 (Checkpoint kinase 1)
    6d
    IQGAP3, the overlooked oncogenic twin of IQGAP1: mapping its interactome and functional roles across cellular signaling and cancer. (PubMed, Cell Commun Signal)
    We then highlight accumulating evidence implicating IQGAP3 dysregulation in oncogenesis, where it promotes tumor initiation, progression, and metastasis. Its contribution to therapy resistance further emphasizes its impact on clinical outcomes.In conclusion, by integrating current insights into the IQGAP3 interactome and associated signaling networks, we position IQGAP3 as a central signaling hub at the intersection of normal cellular physiology and malignant transformation.
    Review • Journal
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    CTNNB1 (Catenin (cadherin-associated protein), beta 1) • CHEK2 (Checkpoint kinase 2) • CHEK1 (Checkpoint kinase 1) • TGFB1 (Transforming Growth Factor Beta 1) • IQGAP1 (IQ Motif Containing GTPase Activating Protein 1)
    9d
    CX-5461-04: Study of CX-5461 in Patients With Solid Tumours and BRCA1/2, PALB2 or Homologous Recombination Deficiency (HRD) Mutation (clinicaltrials.gov)
    P1, N=52, Recruiting, Senhwa Biosciences, Inc. | Trial completion date: Dec 2026 --> Mar 2027 | Trial primary completion date: Dec 2025 --> Mar 2027
    Trial completion date • Trial primary completion date
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    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • CCNE1 (Cyclin E1) • KMT2D (Lysine Methyltransferase 2D) • CDK12 (Cyclin dependent kinase 12) • KMT2C (Lysine Methyltransferase 2C) • SLFN11 (Schlafen Family Member 11) • CHEK2 (Checkpoint kinase 2) • CREBBP (CREB binding protein) • RAD51 (RAD51 Homolog A) • FANCA (FA Complementation Group A) • RAD51B (RAD51 Paralog B) • BRIP1 (BRCA1 Interacting Protein C-terminal Helicase 1) • RAD51C (RAD51 paralog C) • RAD50 (RAD50 Double Strand Break Repair Protein) • RAD51D (RAD51 paralog D) • CHEK1 (Checkpoint kinase 1) • BARD1 (BRCA1 Associated RING Domain 1) • NBN (Nibrin Nijmegen Breakage Syndrome 1 (Nibrin)) • RAD54L (DNA Repair And Recombination Protein RAD54) • FANCF (FA complementation group F) • FANCL (FA Complementation Group L) • RBBP8 (RB Binding Protein 8, Endonuclease) • XRCC2 (X-Ray Repair Cross Complementing 2) • ERCC4 (ERCC Excision Repair 4, Endonuclease Catalytic Subunit) • FANCI (FA Complementation Group I) • FANCM (FA Complementation Group M) • MAD2L2 (Mitotic Arrest Deficient 2 Like 2) • CDC25C (Cell Division Cycle 25C) • FANCD2 (FA Complementation Group D2) • FANCE (FA Complementation Group E) • FANCG (FA Complementation Group G) • MUS81 (MUS81 Structure-Specific Endonuclease Subunit) • CDC25A (Cell Division Cycle 25A) • FANCB (FA Complementation Group B) • FANCC (FA Complementation Group C) • GNRP (Ras-Specific Guanine Nucleotide-Releasing Factor 1) • RAD17 (RAD17 Checkpoint Clamp Loader Component) • SLX4 (SLX4 Structure-Specific Endonuclease Subunit)
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    BRCA2 mutation • BRCA1 mutation • PALB2 mutation
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    pidnarulex (CX-5461)
    10d
    PICDGI: A framework for predicting cancer driver genes through dynamic gene-gene interaction modeling of single-cell data. (PubMed, PLoS Comput Biol)
    We further validated PICDGI on an independent pediatric acute myeloid leukemia (AML) scRNA-seq cohort, where it consistently recovered known drivers and relapse-associated regulatory programs under fixed model parameters. By integrating interaction-informed dynamic modeling with single-cell resolution data, PICDGI provides a generalizable and biologically grounded framework for identifying rare and context-specific regulatory drivers of cancer progression, with broad applicability across tumor types.
    Journal
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    CHEK1 (Checkpoint kinase 1)
    13d
    FLASH Radiotherapy Mitigates Radiation-Induced Lymphopenia and Prevents Immunosuppression via Chk1-STAT3 Axis Modulation in a Preclinical Thoracic Irradiation Model. (PubMed, Int J Radiat Oncol Biol Phys)
    FLASH RT mitigates RIL, reduces lymphocyte apoptosis, and prevents long-term immunosuppression by reduced activation of the Chk1-STAT3 pathway. These findings suggest FLASH RT may confer immunological advantages over CONV RT to enhance therapeutic efficacy.
    Preclinical • Journal • PD(L)-1 Biomarker • IO biomarker
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    PD-L1 (Programmed death ligand 1) • CD8 (cluster of differentiation 8) • PD-1 (Programmed cell death 1) • PTPRC (Protein Tyrosine Phosphatase Receptor Type C) • CHEK1 (Checkpoint kinase 1) • ANXA5 (Annexin A5)
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    PD-L1 expression
    14d
    Checkpoint kinase 1 protein as a diagnostic marker for pleural mesothelioma. (PubMed, J Am Soc Cytopathol)
    Immunohistochemical assessment of CHK1 expression may be useful for distinguishing PM from NNMC. Robust diagnostic sensitivity was observed across both epithelioid and nonepithelioid PM, independent of specimen type. These support CHK1 as a potential pan-mesothelioma diagnostic biomarker. Further validation is warranted in larger, independent cohorts.
    Journal
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    CHEK1 (Checkpoint kinase 1)
    15d
    A Phase I/II Study of Sacituzumab Govitecan Plus Berzosertib in Small Cell Lung Cancer, Extra-Pulmonary Small Cell Neuroendocrine Cancer and Homologous Recombination-Deficient Cancers Resistant to PARP Inhibitors (clinicaltrials.gov)
    P1/2, N=35, Active, not recruiting, National Cancer Institute (NCI) | Recruiting --> Active, not recruiting | N=120 --> 35
    Enrollment closed • Enrollment change
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    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • HRD (Homologous Recombination Deficiency) • CDK12 (Cyclin dependent kinase 12) • BRCA (Breast cancer early onset) • CHEK2 (Checkpoint kinase 2) • RAD51B (RAD51 Paralog B) • BRIP1 (BRCA1 Interacting Protein C-terminal Helicase 1) • RAD51C (RAD51 paralog C) • RAD51D (RAD51 paralog D) • CHEK1 (Checkpoint kinase 1) • BARD1 (BRCA1 Associated RING Domain 1) • RAD54L (DNA Repair And Recombination Protein RAD54) • FANCL (FA Complementation Group L) • PPP2R2A (Protein Phosphatase 2, Regulatory Subunit B, Alpha)
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    BRCA1 mutation • ATM mutation • PALB2 mutation • CDK12 mutation • CHEK2 mutation • BRIP1 mutation • RAD51C mutation • RAD51D mutation • RAD51B mutation • BARD1 mutation • CHEK1 mutation • RAD54L mutation
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    berzosertib (M6620) • Trodelvy (sacituzumab govitecan-hziy)
    15d
    ATR and TopBP1 oppose to control dormant origin activity and global replication dynamics, providing a first defense against replication stress. (PubMed, Nucleic Acids Res)
    Instead, the function of TopBP1 in replisome assembly, which remains unclear in mammalian cells where the protein is not essential, well-accounts for our results positing that TopBP1 locks dormant origins at the pre-initiation stage, an intermediate in the assembly process, and that ATR activation allows assembly to resume. TopBP1 engagement in the pre-initiation complex would thus serve as a switch linking replisome assembly to the stress response.
    Journal
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    CHEK1 (Checkpoint kinase 1)