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GENE:

CHEK2 (Checkpoint kinase 2)

i
Other names: CHEK2, bA444G7, CDS1, CHK2, HuCds1, PP1425, RAD53, Checkpoint kinase 2
2d
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)
3d
Video Education With Clinical Genetic Testing Coordinators for the Rapid Evaluation of Patients With Cancers: Real-World Evidence. (PubMed, JCO Oncol Pract)
Rapid demonstrated high genetic testing uptake and effective integration into oncology workflows, enabling timely treatment decisions. Although the program optimized resource use and reduced barriers, disparities in testing remain. Future efforts should address these inequities and evaluate the long-term impact of genetic testing on patient outcomes.
Journal • HEOR • Real-world evidence • Video • BRCA Biomarker
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BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • CHEK2 (Checkpoint kinase 2)
4d
KNIGHTS: High-Risk Metachronous Oligometastatic Prostate Cancer Trial (clinicaltrials.gov)
P2, N=88, Active, not recruiting, University of Maryland, Baltimore | Recruiting --> Active, not recruiting
Enrollment closed
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TP53 (Tumor protein P53) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • ATM (ATM serine/threonine kinase) • CHEK2 (Checkpoint kinase 2) • FANCA (FA Complementation Group A) • RAD51B (RAD51 Paralog B) • BRIP1 (BRCA1 Interacting Protein C-terminal Helicase 1) • CD4 (CD4 Molecule) • RAD54L (DNA Repair And Recombination Protein RAD54)
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TP53 mutation • BRCA2 mutation • BRCA1 mutation • ATM mutation • PALB2 mutation • CHEK2 mutation • BRIP1 mutation • RAD51B mutation • RAD54L mutation
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Zejula (niraparib) • abiraterone acetate • prednisone
4d
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
6d
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)
6d
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)
7d
Ginsenoside Rb1 alleviates cerebral ischemia/reperfusion injury by suppressing oxidative stress and excessive autophagy via ATM-CHK2-Beclin 1 pathway. (PubMed, Eur J Pharmacol)
Additionally, the drug affinity response target stability (DARTS) and cellular thermal shift assay (CETSA) were also performed to suggest that GRb1 directly interacts with ATM. Collectively, these findings demonstrated that GRb1 reduced ischemic stroke-induced oxidative stress and autophagy through ATM-CHK2-Beclin 1 pathway, and GRb1 may be a protective medication for the treatment of cerebral ischemia.
Journal
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BCL2 (B-cell CLL/lymphoma 2) • CHEK2 (Checkpoint kinase 2) • PIK3R1 (Phosphoinositide-3-Kinase Regulatory Subunit 1) • BECN1 (Beclin 1)
9d
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)
10d
Enrollment change
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ER (Estrogen receptor) • ATM (ATM serine/threonine kinase) • CHEK2 (Checkpoint kinase 2)
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tamoxifen • exemestane
10d
Differential phosphorylation of PHIP phosphopeptides with implications in insulin signaling. (PubMed, BMC Mol Cell Biol)
This phosphorylation-centric study suggests the role of phosphorylated PHIP in insulin signaling pathway through modulation and co-differential phosphorylation of key proteins, paving the way for a robust and replicable approach in elucidating putative targets.
Journal
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SMARCA4 (SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily A, member 4) • CHEK2 (Checkpoint kinase 2) • IRS2 (Insulin receptor substrate 2) • IRS1 (Insulin Receptor Substrate 1)
10d
Uterine serous carcinoma and germline genetic testing: patterns of referral, completion and pathogenic variant detection. (PubMed, J Med Genet)
Given the high prevalence of PVs in this population, germline genetic testing for all patients diagnosed with USC can provide clinically meaningful benefit but is currently underused in practice.
Journal • BRCA Biomarker
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BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • MSH6 (MutS homolog 6) • PMS2 (PMS1 protein homolog 2) • CHEK2 (Checkpoint kinase 2) • BRIP1 (BRCA1 Interacting Protein C-terminal Helicase 1)
12d
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)