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    GENE:

    CHEK1 (Checkpoint kinase 1)

    i
    Other names: CHEK1, CHK1, Checkpoint kinase 1
    1d
    Cabozantinib and Pamiparib for the Treatment of Advanced of Refractory Solid Tumors (clinicaltrials.gov)
    P1, N=44, Completed, M.D. Anderson Cancer Center | Active, not recruiting --> Completed
    Trial completion
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    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • PTEN (Phosphatase and tensin homolog) • ARID1A (AT-rich interaction domain 1A) • CHEK2 (Checkpoint kinase 2) • RAD50 (RAD50 Double Strand Break Repair Protein) • PARP1 (Poly(ADP-Ribose) Polymerase 1) • CHEK1 (Checkpoint kinase 1) • EMSY (EMSY Transcriptional Repressor BRCA2 Interacting)
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    BRCA2 mutation • BRCA1 mutation • ATM mutation • PALB2 mutation • CHEK2 mutation • CHEK1 mutation
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    Cabometyx (cabozantinib tablet) • Partruvix (pamiparib)
    1d
    Olaparib in Men With High-Risk Biochemically-Recurrent Prostate Cancer Following Radical Prostatectomy, With Integrated Biomarker Analysis (clinicaltrials.gov)
    P2, N=51, Active, not recruiting, Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins | Trial completion date: May 2026 --> May 2027
    Trial completion date
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    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • ATM (ATM serine/threonine kinase) • CDK12 (Cyclin dependent kinase 12) • 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) • 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
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    Lynparza (olaparib)
    2d
    Molecular structural and optoelectronic properties of damnacanthal derivatives: a DFT, TD-DFT, and docking approach. (PubMed, J Mol Model)
    Structure-based virtual screening was carried out by using the CHKl receptor to investigate drug-protein interactions. Docking simulations were performed to evaluate binding affinities and interaction patterns by utilizing AutoDock Vina.
    Journal
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    CHEK1 (Checkpoint kinase 1)
    2d
    AKT2 Counteracts Hypoxia-Induced Suppression of Homologous Recombination in Triple-Negative Breast Cancer: A Targeted Approach to Sensitize Tumors to PARP Inhibition. (PubMed, J Biochem Mol Toxicol)
    A cell viability assay was used to determine the sensitivity to olaparib...Although AKT2-selective inhibitors have been reported, they remain largely preclinical. Accordingly, our findings support AKT2 as a promising therapeutic target and warrant further validation using AKT2-selective pharmacologic inhibition.
    Journal • BRCA Biomarker • PARP Biomarker
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    BRCA1 (Breast cancer 1, early onset) • HIF1A (Hypoxia inducible factor 1, alpha subunit) • CHEK2 (Checkpoint kinase 2) • RAD51 (RAD51 Homolog A) • CHEK1 (Checkpoint kinase 1) • AKT2 (V-akt murine thymoma viral oncogene homolog 2)
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    Lynparza (olaparib)
    4d
    Efficacy of olaparib in advanced cancers with somatic or germline mutations in BAP1, BARD1, BRIP1 and PALB2. (PubMed, ESMO Open)
    Olaparib demonstrated meaningful clinical activity across different cancer types with somatic or germline mutations in BAP1, BARD1, BRIP1 and PALB2.
    Journal • BRCA Biomarker • PARP Biomarker
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    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • HRD (Homologous Recombination Deficiency) • ARID1A (AT-rich interaction domain 1A) • BAP1 (BRCA1 Associated Protein 1) • PALB2 (Partner and localizer of BRCA2) • CDK12 (Cyclin dependent kinase 12) • ATRX (ATRX Chromatin Remodeler) • 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) • MRE11A (MRE11 homolog, double strand break repair nuclease) • NBN (Nibrin Nijmegen Breakage Syndrome 1 (Nibrin)) • RAD21 (RAD21 Cohesin Complex Component) • DDR2 (Discoidin domain receptor 2) • ERCC4 (ERCC Excision Repair 4, Endonuclease Catalytic Subunit) • RAD52 (RAD52 Homolog DNA Repair Protein) • FANCE (FA Complementation Group E) • GEN1 (GEN1 Holliday junction 5' flap endonuclease) • SLX4 (SLX4 Structure-Specific Endonuclease Subunit)
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    BRCA2 mutation • BRCA1 mutation • HRD • ARID1A mutation • PALB2 mutation • CDK12 mutation • BRIP1 mutation • RAD51C mutation • RAD51D mutation • BARD1 mutation • CHEK1 mutation
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    Lynparza (olaparib)
    6d
    ATRX loss promotes gliomagenesis by converged actions on neural differentiation and telomere maintenance. (PubMed, Cell Signal)
    These findings support a hypothetical three-step model that reconciles the initial indolence and eventual malignant progression of ATRX-deficient gliomas. Our study clarifies species-specific differences in ATRX function and provides important mechanistic and clinical implications for the development of targeted therapies for ATRX-mutant gliomas.
    Journal
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    ATRX (ATRX Chromatin Remodeler) • CHEK2 (Checkpoint kinase 2) • CHEK1 (Checkpoint kinase 1)
    7d
    Molecular Determinants of Response and Rational Drug Combinations for Antibody-Drug Conjugates (ADCs) with Topoisomerase I (TOP1) Inhibitor payloads. (PubMed, J Mol Biol)
    Here we describe the different TOP1 poisons used a "payload" for tumor-targeted anticancer therapies in comparison with the widely used first generation TOP1 poisons: Topotecan, Irinotecan and Belotecan. We review the determinants of response to tumor-targeted TOP1 poison inhibitors (TTTis) as candidate companion diagnostic (Dx) biomarkers for precision medicine and patient selection, such as high expression of surface epitopes for ADCs (Antibody Drug Conjugates), high tumor proliferation (Ki67), Schlafen 11 (SLFN11) expression, homologous recombination deficiencies (HRD/BRCAness) and expression of drug efflux transporters such as (BCRP (MXR) encoded by ABCG2. We also summarize the mechanistic rationale for combining TTTis with small molecule inhibitors of poly(ADPribose) polymerase (PARP), ATR (Ataxia Telangiectasia and Rad3-related), CHK1 (Checkpoint Kinase 1) and ATM (Ataxia Telangiectasia Mutated).
    Review • Journal • BRCA Biomarker • PARP Biomarker • BRCA Companion diagnostic • PARP Companion diagnostic
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    HRD (Homologous Recombination Deficiency) • SLFN11 (Schlafen Family Member 11) • ABCG2 (ATP Binding Cassette Subfamily G Member 2) • ATR (Ataxia telangiectasia and Rad3-related protein) • CHEK1 (Checkpoint kinase 1)
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    HRD
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    irinotecan • topotecan • Camtobell (belotecan)
    8d
    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
    10d
    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
    10d
    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)
    10d
    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)
    13d
    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)