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    GENE:

    CHEK1 (Checkpoint kinase 1)

    i
    Other names: CHEK1, CHK1, Checkpoint kinase 1
    2d
    KPT-330-mediated XPO1 inhibition impairs homologous recombination and enhances radiosensitivity in extranodal NK/T-cell lymphoma. (PubMed, Br J Cancer)
    XPO1 inhibition impairs HR and enhances radiosensitivity by disrupting the c-Myc-RAD51/CHEK1 axis. These findings support prospective evaluation of KPT-330-based radiosensitization in R/R ENKTL.
    Journal • IO biomarker
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    MYC (V-myc avian myelocytomatosis viral oncogene homolog) • RAD51 (RAD51 Homolog A) • CHEK1 (Checkpoint kinase 1) • XPO1 (Exportin 1)
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    Xpovio (selinexor)
    3d
    Molecular mechanisms of KMT2C alterations in gastrointestinal cancers: enhancer network destabilization, lineage plasticity, and clinical translation. (PubMed, Front Immunol)
    In this review, we integrate evidence from hepatocellular carcinoma, pancreatic ductal adenocarcinoma, cholangiocarcinoma, colorectal cancer, gastric cancer, esophageal cancer, and gallbladder cancer within a unified framework that links KMT2C domain architecture to enhancer-network destabilization, phenotypic state transitions, and clinical manifestations. We further propose a functional evaluation paradigm that reframes discrete KMT2C variants as graded states of epigenetic deficiency, coupled with a closed-loop validation strategy integrating tissue-based profiling, liquid biopsy monitoring, and spatial multi-omics analyses.
    Review • Journal • Tumor mutational burden • PARP Biomarker
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    TMB (Tumor Mutational Burden) • MSI (Microsatellite instability) • KMT2C (Lysine Methyltransferase 2C) • CHEK1 (Checkpoint kinase 1) • DRD (DNA Repair Deficiency)
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    DDR
    3d
    Uncovering the potential anti-cancer compounds from Strobilanthes cusia against colorectal cancer through network pharmacology and molecular docking. (PubMed, Sci Rep)
    In vitro validation demonstrated dose-dependent apoptosis and proliferation inhibition in both cell lines, with significantly lower IC50 values at 48 h (isolated: 10.52 ± 1.91µM; commercial: 8.96 ± 9.35µM) than at 24 h. These findings identify CHEK1 as a mechanistically relevant target and support further translational investigation of S. cusia-derived andrographolide in CRC therapy.
    Journal
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    CHEK1 (Checkpoint kinase 1)
    6d
    Clinical applications of PARP inhibitors in breast, ovarian, and prostate cancer: current insights and future directions. (PubMed, Clin Adv Hematol Oncol)
    Since the initial US Food Administration approval of olaparib in 2014, PARP inhibitors have shown efficacy across ovarian, breast, and prostate cancers, although differences in trial design and biomarker strategies have resulted in tumor-specific indications...Ongoing studies are evaluating rational combinations targeting complementary DNA damage response pathways (ATR/CHK1/WEE1, PI3K/AKT) and integrating immunotherapy or hormonal agents to extend benefit. Moving forward, harmonizing HRD testing across tumor types, accounting for germline, somatic, and liquid biopsy-derived alterations, and refining patient selection will be essential to maximize therapeutic efficacy and safely expand PARP inhibitor use beyond canonical BRCA-mutated cancers.
    Review • Journal • BRCA Biomarker • PARP Biomarker • IO biomarker
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    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • HRD (Homologous Recombination Deficiency) • BRCA (Breast cancer early onset) • CHEK1 (Checkpoint kinase 1)
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    BRCA2 mutation • BRCA1 mutation • HRD
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    Lynparza (olaparib)
    6d
    Integrated network pharmacology reveal new key curcumin-binding targets in triple-negative breast cancer. (PubMed, Discov Oncol)
    Our integrated analysis suggests that curcumin exerts multitarget inhibitory effects in TNBC by concurrently modulating mitotic regulation (via AURKA), MAPK signaling (via BRAF (V600E)), and DNA damage checkpoints (via CHEK1). Among these, CHEK1 emerged as the most thermodynamically stable and conformationally favorable binding target for curcumin, indicating its potential as a crucial mediator of curcumin's antitumor activity.
    Journal
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    BRAF (B-raf proto-oncogene) • AURKA (Aurora kinase A) • CHEK1 (Checkpoint kinase 1)
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    BRAF V600E • BRAF V600
    7d
    NCI-2017-02296: Testing Olaparib in Patients With Advanced or Metastatic (Cancer That Has Spread) Bladder Cancer and Other Genitourinary Tumors With DNA-Repair Genetic Changes (clinicaltrials.gov)
    P2, N=60, Active, not recruiting, National Cancer Institute (NCI) | Suspended --> Active, not recruiting
    Enrollment closed • Tumor mutational burden
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    TP53 (Tumor protein P53) • TMB (Tumor Mutational Burden) • ABL1 (ABL proto-oncogene 1) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • STK11 (Serine/threonine kinase 11) • NPM1 (Nucleophosmin 1) • POLE (DNA Polymerase Epsilon) • CCND1 (Cyclin D1) • BAP1 (BRCA1 Associated Protein 1) • MLH1 (MutL homolog 1) • MSH6 (MutS homolog 6) • MSH2 (MutS Homolog 2) • ATRX (ATRX Chromatin Remodeler) • CHEK2 (Checkpoint kinase 2) • SMARCB1 (SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily B, Member 1) • RAD51 (RAD51 Homolog A) • FANCA (FA Complementation Group A) • BRIP1 (BRCA1 Interacting Protein C-terminal Helicase 1) • POLD1 (DNA Polymerase Delta 1) • CHEK1 (Checkpoint kinase 1) • BARD1 (BRCA1 Associated RING Domain 1) • FANCL (FA Complementation Group L) • BRD4 (Bromodomain Containing 4) • DOT1L (DOT1 Like Histone Lysine Methyltransferase) • FANCE (FA Complementation Group E) • FANCG (FA Complementation Group G) • IKBKE (Inhibitor Of Nuclear Factor Kappa B Kinase Subunit Epsilon) • FANCC (FA Complementation Group C)
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    PALB2 mutation • BRIP1 mutation
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    FoundationOne® CDx
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    Lynparza (olaparib)
    9d
    Multiomics integration prioritizes potential drug targets for lung cancer. (PubMed, Discov Oncol)
    This multi-omics MR framework identifies genes whose genetically predicted expression is associated with increased or decreased lung cancer risk and may help prioritize candidate targets for future lung cancer drug development.
    Journal
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    FLT4 (Fms-related tyrosine kinase 4) • CHEK1 (Checkpoint kinase 1)
    13d
    Differential DNA damage response to WRN inhibition identifies a targetable vulnerability in ARID1A-mutated cancers. (PubMed, Sci Adv)
    The antitumor efficacy of WRN inhibition alone and in combination with p21 inhibition was validated using cell line-based xenograft and patient-derived xenograft mouse models. Our findings define WRN as a selective therapeutic target in ARID1A-mutated cancers and suggest a combinatorial strategy of WRN and p21 inhibition as a therapeutic approach.
    Journal
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    ARID1A (AT-rich interaction domain 1A) • CHEK2 (Checkpoint kinase 2) • CHEK1 (Checkpoint kinase 1) • WRN (WRN RecQ Like Helicase) • CDKN1A (Cyclin-dependent kinase inhibitor 1A)
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    ARID1A mutation
    14d
    MK3475-A53: Study of SBRT/Olaparib Followed by Pembrolizumab/Olaparib in Gastric Cancers (clinicaltrials.gov)
    P2, N=9, Completed, University of Colorado, Denver | Active, not recruiting --> Completed | Trial completion date: Dec 2028 --> Jan 2026
    Trial completion • Trial completion date
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    HER-2 (Human epidermal growth factor receptor 2) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • PTEN (Phosphatase and tensin homolog) • HRD (Homologous Recombination Deficiency) • BAP1 (BRCA1 Associated Protein 1) • KMT2D (Lysine Methyltransferase 2D) • ATRX (ATRX Chromatin Remodeler) • CHEK2 (Checkpoint kinase 2) • FANCA (FA Complementation Group A) • BRIP1 (BRCA1 Interacting Protein C-terminal Helicase 1) • RAD50 (RAD50 Double Strand Break Repair Protein) • MLL2 (Myeloid/lymphoid or mixed-lineage leukemia 2) • CHEK1 (Checkpoint kinase 1) • BARD1 (BRCA1 Associated RING Domain 1) • NBN (Nibrin Nijmegen Breakage Syndrome 1 (Nibrin)) • WRN (WRN RecQ Like Helicase) • FANCG (FA Complementation Group G) • ABRAXAS1 (Abraxas 1 BRCA1 A Complex Subunit 2) • SLX4 (SLX4 Structure-Specific Endonuclease Subunit)
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    HRD
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    Keytruda (pembrolizumab) • Lynparza (olaparib)
    14d
    A RHNO1-ATR/Chk1 positive feedback loop sustains the DNA replication stress response. (PubMed, bioRxiv)
    Together, our data reveals a novel positive feedback loop wherein ATR/Chk1 signaling activation stabilizes RHNO1, which, in turn, is required to sustain the signal and thus the replication stress response. This work identifies RHNO1 as a key component in the cellular replication stress response and highlights its potential as a therapeutic target for tumor cells reliant on ATR/Chk1 signaling.
    Journal
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    CHEK1 (Checkpoint kinase 1) • ERCC4 (ERCC Excision Repair 4, Endonuclease Catalytic Subunit) • RPA2 (Replication Protein A2)
    16d
    Green synthesis of ZnO nanoparticles using bioactive compounds from the Amycolatopsis roodepoortensis strain EA7 and their effects in the HT-29 cell line. (PubMed, Sci Rep)
    Flow-cytometric analysis revealed apoptosis induction (P ≤ 0.001) and cell cycle arrest in G0/G1 phase in the HT-29 cells. Given the results presented, this research could be an important step towards further investigations and the development of novel antimicrobial and anticancer therapeutics.
    Preclinical • Journal • IO biomarker
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    BCL2 (B-cell CLL/lymphoma 2) • CHEK2 (Checkpoint kinase 2) • CHEK1 (Checkpoint kinase 1) • MMP9 (Matrix metallopeptidase 9)
    16d
    KEYNOTE-F86: A Study of PARG Inhibitor IDE161 in Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=216, Active, not recruiting, IDEAYA Biosciences | Recruiting --> Active, not recruiting
    Enrollment closed
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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) • CHEK2 (Checkpoint kinase 2) • FANCA (FA Complementation Group A) • 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) • NBN (Nibrin Nijmegen Breakage Syndrome 1 (Nibrin)) • RAD54L (DNA Repair And Recombination Protein RAD54) • FANCL (FA Complementation Group L) • PPP2R2A (Protein Phosphatase 2, Regulatory Subunit B, Alpha)
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    HRD
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    Keytruda (pembrolizumab) • IDE161