^
    Contact us  to learn more about
    our Premium Content:  News alerts, weekly reports and conference planners
    GENE:

    CHEK1 (Checkpoint kinase 1)

    i
    Other names: CHEK1, CHK1, Checkpoint kinase 1
    4d
    Replication Stress in Cancer: Mechanistic Insights and Therapeutic Opportunities for Radiosensitization. (PubMed, Curr Issues Mol Biol)
    We summarize preclinical and emerging clinical evidence for exploiting RS for radiosensitization, and outline candidate biomarkers and functional assays for patient selection. We also highlight the links between RS, therapy-induced senescence and innate immune activation via the cGAS-STING (cyclic GMP-AMP synthase-Stimulator of Interferon Genes) pathway, and address current challenges and future directions.
    Review • Journal • PARP Biomarker
    |
    PARP1 (Poly(ADP-Ribose) Polymerase 1) • STING (stimulator of interferon response cGAMP interactor 1) • CHEK1 (Checkpoint kinase 1) • CGAS (Cyclic GMP-AMP Synthase)
    5d
    Solid dispersion of BIBR1532: A potent therapeutic for oesophageal squamous cancer. (PubMed, World J Gastrointest Oncol)
    HPMC-based SD enhances BIBR1532 solubility and bioavailability for effective ESCC treatment. Future studies should focus on pilot tests for SD fabrication.
    Journal
    |
    CHEK2 (Checkpoint kinase 2) • CHEK1 (Checkpoint kinase 1)
    |
    BIBR1532
    6d
    Herba Patriniae Component Linarin Induces Cell Cycle Arrest and Senescence in Non-Small-Cell Lung Cancer Associated with Cyclin A2 Downregulation. (PubMed, Pharmaceuticals (Basel))
    These effects are associated with the downregulation of key cell cycle regulators, including CCNA2/B1 and CHEK1. Together, these findings highlight the potential of Linarin as a promising therapeutic option for NSCLC.
    Journal
    |
    TP53 (Tumor protein P53) • CHEK2 (Checkpoint kinase 2) • CHEK1 (Checkpoint kinase 1) • CCNA2 (Cyclin A2) • CDK1 (Cyclin-dependent kinase 1)
    |
    TP53 wild-type
    6d
    From Phytochemistry to Oncology: The Role of Bakuchiol in the Treatment of Breast Cancer. (PubMed, Biomolecules)
    Exclusion criteria included works not related to BAK or its therapeutic use in breast cancer, as well as publications that did not meet basic scientific standards, such as lacking methodological rigor or presenting a low level of scientific evidence. However, current evidence is predominantly in vitro, and limitations such as poor bioavailability and lack of clinical validation underscore the need for further in vivo and translational studies before therapeutic application can be established.
    Review • Journal
    |
    ER (Estrogen receptor) • CHEK2 (Checkpoint kinase 2) • CHEK1 (Checkpoint kinase 1)
    |
    ER positive
    12d
    Identification and Validation of Prognostic Biomarker Signatures Associated with Overall Survival in Colorectal Cancer: Evidence from Bioinformatics Analysis and an in vivo Study. (PubMed, Asian Pac J Cancer Prev)
    The findings of the present study provided a set of four key genes with valid clinical utility that can serve as an alternative tool for prognosis and identification of new targets in CRC treatment.
    Preclinical • Journal
    |
    SPP1 (Secreted Phosphoprotein 1) • CHEK1 (Checkpoint kinase 1) • KIF18A (Kinesin Family Member 18A) • MAD2L1 (Mitotic Arrest Deficient 2 Like 1)
    13d
    Multi-omics analysis and functional validation of CHEK1 as an independent prognostic biomarker in Pancreatic cancer. (PubMed, PLoS One)
    Our study indicates that high CHEK1 expression could be an independent prognostic marker for pancreatic cancer and may drive cancer progression by influencing DNA replication and G2/M checkpoint pathways. These insights offer a foundation for future research and targeted precision therapy involving CHEK1.
    Journal
    |
    CHEK1 (Checkpoint kinase 1)
    18d
    Targeting matrix metalloproteinase-14 disrupts DNA repair and reduces viability in adrenocortical carcinoma. (PubMed, bioRxiv)
    Mechanistically, MMP-14 translocates to the nucleus and binds to chromatin following DNA damage induced by ionizing radiation or cisplatin...These findings reveal a novel nuclear function for MMP-14 in DNA repair and identify MMP-14 as a promising therapeutic target in ACC. Targeting MMP-14 may sensitize ACC tumors to DNA-damaging chemotherapy by impairing the repair of therapy-induced lesions.
    Journal
    |
    CHEK1 (Checkpoint kinase 1) • MMP14 (Matrix Metallopeptidase 14)
    |
    cisplatin
    18d
    Novel therapeutic potential of the PARP inhibitor talazoparib in synovial sarcoma and its combined effect with ATR inhibitor. (PubMed, Discov Oncol)
    Talazoparib combined with ATR inhibitor possesses potential application as a therapeutic option for SS.
    Journal • PARP Biomarker
    |
    CHEK1 (Checkpoint kinase 1) • ANXA5 (Annexin A5)
    |
    Talzenna (talazoparib) • ceralasertib (AZD6738)
    21d
    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, Recruiting, National Cancer Institute (NCI) | Trial completion date: Dec 2025 --> Dec 2026 | Trial primary completion date: Dec 2025 --> Dec 2026
    Trial completion date • Trial primary completion date • Tumor mutational burden
    |
    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)
    |
    PALB2 mutation • BRIP1 mutation
    |
    FoundationOne® CDx • FoundationOne® Liquid CDx
    |
    Lynparza (olaparib)
    24d
    Network Pharmacology and Molecular Docking Identify Medicarpin as a Potent CASP3 and ESR1 Binder Driving Apoptotic and Hormone-Dependent Anticancer Activity. (PubMed, Int J Mol Sci)
    Although CASP3 and ESR1 expression alone lacked prognostic significance, their network interplay suggests synergistic relevance. Medicarpin exhibits multitarget anticancer potential in OC by modulating kinase-driven and hormone-dependent pathways, warranting further experimental validation.
    Journal • PARP Biomarker
    |
    ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • ABL1 (ABL proto-oncogene 1) • CCND1 (Cyclin D1) • CDK4 (Cyclin-dependent kinase 4) • PARP1 (Poly(ADP-Ribose) Polymerase 1) • CHEK1 (Checkpoint kinase 1) • CASP3 (Caspase 3)
    25d
    HMGB1 Assists in Overcoming Cisplatin Resistance in Chemoresistant Human Ovarian Cancer Cells. (PubMed, Mol Carcinog)
    Notably, DNA immunoblot and modified alkaline comet assay results demonstrated that HMGB1 depletion stimulated cisplatin-DNA adduct formation and impaired the removal of cisplatin-DNA adducts, particularly in the cisplatin-resistant cells. Collectively, these findings uncover novel functions of HMGB1 in mediating cisplatin sensitivity, emphasizing its potential as a therapeutic target to overcome cisplatin resistance in ovarian cancer.
    Journal
    |
    CHEK2 (Checkpoint kinase 2) • CHEK1 (Checkpoint kinase 1) • HMGB1 (High Mobility Group Box 1)
    |
    cisplatin
    26d
    APOBEC3C coordinates DDX5 in R-loop resolution and dynamic control of Chk1-mediated stress-responsive circuitry as a prerequisite for gemcitabine resistance in p53-deficient cells. (PubMed, Cell Death Dis)
    Knockdown of DDX5 in A3C-proficient H1299 cells attenuated gemcitabine-induced Chk1 activation and enhanced the therapeutic index of gemcitabine by promoting R-loop accumulation. Therefore, we conclude that A3C/DDX5/R-loop complex may impair the sensitivity of gemcitabine by modulating Chk1 dynamics and DNA replication/damage response machinery.
    Journal
    |
    CHEK1 (Checkpoint kinase 1) • DDX5 (DEAD-Box Helicase 5)
    |
    gemcitabine