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GENE:

CHEK2 (Checkpoint kinase 2)

i
Other names: CHEK2, bA444G7, CDS1, CHK2, HuCds1, PP1425, RAD53, Checkpoint kinase 2
17h
Phase II Trial of the PARP Inhibitor Niraparib and PD-1 Inhibitor Dostarlimab in Patients With Advanced Cancers With Active Progressing Brain Metastases (STARLET) (clinicaltrials.gov)
P2, N=120, Recruiting, M.D. Anderson Cancer Center | Trial completion date: Feb 2026 --> Dec 2029 | Trial primary completion date: Feb 2026 --> Dec 2029
Trial completion date • Trial primary completion date
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PD-L1 (Programmed death ligand 1) • HRD (Homologous Recombination Deficiency) • CDK12 (Cyclin dependent kinase 12) • CHEK2 (Checkpoint kinase 2) • RAD51 (RAD51 Homolog 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) • RAD54L (DNA Repair And Recombination Protein RAD54) • FANCL (FA Complementation Group L) • RAD52 (RAD52 Homolog DNA Repair Protein)
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PD-L1 expression
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Zejula (niraparib) • Jemperli (dostarlimab-gxly)
19h
Mutations with prognostic value in uveal melanoma. Analytical study of variants detected by targeted NGS. (PubMed, Can J Ophthalmol)
Mutations in BAP1, CHEK2, and DICER1 are independently associated with poorer prognosis in UM, while SF3B1 defines a distinct histologic subgroup. Routine mutational profiling by targeted NGS may aid in risk stratification and follow-up of UM patients.
Journal • Next-generation sequencing
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SF3B1 (Splicing Factor 3b Subunit 1) • BAP1 (BRCA1 Associated Protein 1) • LRP1B (LDL Receptor Related Protein 1B) • CHEK2 (Checkpoint kinase 2) • DICER1 (Dicer 1 Ribonuclease III)
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SF3B1 mutation • CHEK2 mutation
2d
Delactylation of the tumor suppressor ARHGDIB drives metastasis and chemoresistance in bladder cancer. (PubMed, Cell Rep)
Entinostat, an inhibitor of class I HDAC, synergizes with cisplatin by preventing ARHGDIB delactylation. Collectively, our findings unveil a unique paradigm in which delactylation of tumor suppressors drives metastasis and chemoresistance. Targeting lactylation dynamics with HDAC inhibitors presents an avenue for intervention of bladder cancer.
Journal
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CHEK2 (Checkpoint kinase 2) • RAC1 (Rac Family Small GTPase 1) • HDAC2 (Histone deacetylase 2) • ARHGDIB (Rho GDP Dissociation Inhibitor Beta)
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cisplatin • Jingzhuda (entinostat)
2d
Metastatic extra-axial medulloblastoma involving the trigeminal nerve: a rare prognostic entity with a comprehensive literature review. (PubMed, Front Oncol)
Around 5-6% of MBs are associated with inherited cancer predisposition syndromes, with common genetic variants including PTCH1, SUFU, TP53, and SMO. This report describes the first pediatric patient harboring a CHEK2 germline variant of uncertain significance and developing a EA- MB localized at the trigeminal nerve and subsequent CNS and EN metastases.
Review • Journal
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TP53 (Tumor protein P53) • PTCH1 (Patched 1) • CHEK2 (Checkpoint kinase 2)
4d
Olaparib and ASTX727 in BRCA1/2- and Homologous Recombination Deficient (HRD)-Mutated Tumors (clinicaltrials.gov)
P1, N=18, Recruiting, Pamela Munster | Trial completion date: Feb 2027 --> Jan 2028 | Trial primary completion date: Jan 2026 --> Jan 2028
Trial completion date • Trial primary completion date
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BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • BRCA (Breast cancer early onset) • CHEK2 (Checkpoint kinase 2)
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PALB2 mutation • CHEK2 mutation
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Lynparza (olaparib) • Inqovi (decitabine/cedazuridine)
6d
Metabolomic-driven prediction of the mutational status of healthy individuals with a family history of hereditary breast and ovarian cancer syndrome: the HRRmet study. (PubMed, Sci Rep)
The present study is the first to characterize the phenotype associated with the HRR-deficient genotype in healthy individuals with a familial history of HBOC. Metabolomic profiles may be useful for differentiating carriers from noncarriers of PVs in the HRR genes, and therefore, with potential predictive capacity of the HRR germline mutational status.
Journal • BRCA Biomarker • Metabolomic study
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BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • HRD (Homologous Recombination Deficiency) • PALB2 (Partner and localizer of BRCA2) • CHEK2 (Checkpoint kinase 2) • RAD51 (RAD51 Homolog A)
6d
Male breast health and breast cancer risk. (PubMed, Maturitas)
Management strategies for male breast cancer generally parallel female protocols, despite unique biological features. By integrating considerations of benign and malignant conditions, this review underscores the importance of tailored evaluation, risk assessment, and individualized care for males, while identifying knowledge gaps to inform future research and improve outcomes in this under-recognized population.
Review • Journal • BRCA Biomarker
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BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • PALB2 (Partner and localizer of BRCA2) • CHEK2 (Checkpoint kinase 2)
7d
Risk-Reducing Mastectomy in BRCA1/2 and Other High-Risk Gene Carriers: Current Evidence and Practical Guidance. (PubMed, J Breast Cancer)
This review integrates the current evidence and evolving guidelines to clarify the benefits, limitations, and controversies surrounding RRM. By addressing existing knowledge gaps and decision-making challenges, it aims to facilitate informed patient-centered counseling for the management of hereditary breast cancer.
Review • Journal
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TP53 (Tumor protein P53) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • PTEN (Phosphatase and tensin homolog) • STK11 (Serine/threonine kinase 11) • PALB2 (Partner and localizer of BRCA2) • CDH1 (Cadherin 1) • CHEK2 (Checkpoint kinase 2)
8d
MSH2 Prevents Liver Tumorigenesis by Regulating Cell Cycle Checkpoints under Chronic Inflammation. (PubMed, Carcinogenesis)
Functional assays further demonstrated that MSH2 downregulation impaired ATM-CHK2-mediated DNA damage response and promoted cell cycle acceleration. MSH2 exerts its tumor-suppressive effects in hepatocytes not only through canonical MMR but also by regulating the cell cycle via the ATM-CHK2 axis.
Journal
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MSH2 (MutS Homolog 2) • CHEK2 (Checkpoint kinase 2)
8d
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
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CHEK2 (Checkpoint kinase 2) • CHEK1 (Checkpoint kinase 1)
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BIBR1532
9d
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
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TP53 (Tumor protein P53) • CHEK2 (Checkpoint kinase 2) • CHEK1 (Checkpoint kinase 1) • CCNA2 (Cyclin A2) • CDK1 (Cyclin-dependent kinase 1)
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TP53 wild-type
9d
Retinoic Acid and Calcitriol Protect Mouse Primordial Follicles from Cyclophosphamide Treatment-Induced Apoptosis. (PubMed, Antioxidants (Basel))
In this study, we found that intraperitoneal injection of retinoic acid (RA) and calcitriol partially reversed the cyclophosphamide and doxorubicin treatment-induced decrease in primordial follicles in neonatal mouse ovaries. Thus, RA and calcitriol protect mouse primordial follicles from cyclophosphamide treatment-induced apoptosis by inhibiting cyclophosphamide treatment-induced oocyte transcriptional activity and enhancing antioxidant capacity. Our results suggest a potential strategy for preserving ovarian reserve during chemotherapy in female cancer patients.
Preclinical • Journal
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CHEK2 (Checkpoint kinase 2) • CASP3 (Caspase 3) • GPX4 (Glutathione Peroxidase 4) • FOXO3 (Forkhead box O3)
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doxorubicin hydrochloride • cyclophosphamide