AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPhenomena and ProcessesInformation ScienceHealth Care
Checkpoint Kinase 2Protein KinasesProtein-Serine-Threonine KinasesCell Cycle ProteinsDNA DamageAtaxia Telangiectasia Mutated ProteinsGenes, cdcG2 PhaseM Phase Cell Cycle CheckpointsMitosisCell CyclePhosphorylationCell Cycle CheckpointsS PhaseProtein Kinase Inhibitorscdc25 PhosphatasesPhosphatidylinositol 3-KinasesDNA ReplicationHydroxyureaSaccharomyces cerevisiae ProteinsCDC2 Protein KinaseSpindle ApparatusMAP Kinase Signaling SystemSchizosaccharomyces pombe ProteinsSchizosaccharomycesG2 Phase Cell Cycle CheckpointsMutationDNA-Binding ProteinsNuclear ProteinsIntracellular Signaling Peptides and ProteinsS Phase Cell Cycle CheckpointsKinetochoresTumor Suppressor ProteinsSaccharomyces cerevisiaeDNA RepairCalcium-Calmodulin-Dependent Protein KinasesSignal TransductionProtein-Tyrosine KinasesCell Line, Tumorsrc-Family KinasesNocodazoleHeLa CellsRadiation, IonizingCyclin-Dependent KinasesProtein BindingEnzyme ActivationTumor Suppressor Protein p53Cdc20 ProteinsMethyl MethanesulfonateProtein Kinase Cp38 Mitogen-Activated Protein KinasesApoptosisDNA Breaks, Double-StrandedAurora KinasesG1 PhaseRNA, Small InterferingCyclic AMP-Dependent Protein KinasesModels, BiologicalMolecular Sequence DataFungal ProteinsUltraviolet RaysCell LineCyclin BMitogen-Activated Protein Kinase 1Chromosome SegregationDNA, FungalHistonesGenomic InstabilityAmino Acid SequenceMitogen-Activated Protein Kinase KinasesProtein Structure, TertiaryJNK Mitogen-Activated Protein Kinasesp21-Activated KinasesRNA InterferenceBlotting, WesternMitogen-Activated Protein Kinase 3Cell DivisionGamma RaysSerineStaurosporineReplication Protein AMAP Kinase Kinase KinasesCell SurvivalCreatine KinaseTransfectionCasein Kinase IICell NucleusMeiosisCDC2-CDC28 KinasesChromosomal Proteins, Non-HistoneMAP Kinase Kinase 1eIF-2 KinasePhosphoproteinsImmunoblottingGene Expression Regulation, FungalCasein KinasesRecombinant Fusion ProteinsPhosphoserineEnzyme InhibitorsPyruvate Kinase
CHK1SERINEInhibitorsInhibitorProteinInternational Centre for Kinase ProfilingChk2MitoticProteinsCHEK2Control KinasesAnaplastic lymphoMps1PhosphorylationReceptorPyruvate kinaseCyclinMutationApoptosisReactive oxygenOvarian cancer2023CancerSpindle checkpointReplicationCDK2Rad53AssayChromosomesRegulateCell cycle arrestInteraction
CHK14
  • Checkpoint kinase 1 (Chk1, CHEK1) is a Ser/Thr protein kinase that plays a key role in mediating the cellular response to DNA-damage. (rcsb.org)
  • In contrast, downstream signaling from ATR directly to the checkpoint kinase Chk1 was required for survival responses for a smaller subset of the drugs tested. (ascopost.com)
  • SRA737 is a potent, highly selective, orally bioavailable small molecule inhibitor of Checkpoint kinase 1 (Chk1), a key regulator of cell cycle progression and the DNA Damage Response (DDR). (salesandmarketingnetwork.com)
  • The presence of replication stress activates the DNA damage response and downstream checkpoint proteins including ataxia telangiectasia and Rad3 related kinase (ATR), checkpoint kinase 1 (CHK1), and WEE1-like protein kinase (WEE1), which trigger cell cycle arrest while protecting and restoring stalled replication forks. (bmj.com)
SERINE1
  • It is a PROTEIN-SERINE-THREONINE KINASE that is translocated to the CELL NUCLEUS in response to light signals. (bvsalud.org)
Inhibitors4
  • Discovery of a Novel Class of Triazolones as Checkpoint Kinase Inhibitors--Hit to Lead Exploration. (rcsb.org)
  • Immunotherapy mainly includes immune checkpoint inhibitors (ICIs), such as inhibitors of PD-1 (programmed cell death 1)/programmed cell death ligand 1 (PD-L1). (nature.com)
  • Within a decade of the initial discovery, the development of small molecule kinase inhibitors of BRAF (e.g., vemurafenib and dabrafenib) and their clinical validation occurred, showing significant short-term responses in patients with ERK1 corresponds to C161 in ERK2 and C159 in Rattus norvegicus ERK2. (cell-signaling-pathways.com)
  • Hypothyroidism may also occur in patients taking amiodarone or other iodine-containing drugs, in patients taking interferon-alfa, and in patients being treated for cancer with checkpoint inhibitors or some tyrosine kinase inhibitors. (msdmanuals.com)
Inhibitor7
  • Cycloheximide or Chk2 inhibitor pretreatment abrogated not only activation of Chk2 but also G 2 /M arrest and apoptosis mediated by DIM. (aspetjournals.org)
  • The oral FAK kinase inhibitor VS-4718, currently in Phase I clinical evaluation, was tested to determine if it could overcome the immunosuppressive tumor microenvironment of PDAC. (biomedcentral.com)
  • SRA141 is a potent, selective, orally bioavailable small molecule inhibitor of Cell division cycle 7 kinase (Cdc7). (salesandmarketingnetwork.com)
  • New findings suggest that first-line therapy with a combination of a tyrosine kinase inhibitor (TKI) and an immune checkpoint inhibitor improved outcomes in patients with metastatic renal cell carcinoma (mRCC) when compared with the current standard of care. (medscape.com)
  • Because of these results, researchers are suggesting that this combination of a TKI and an immune checkpoint inhibitor may well represent the new standard of care and is likely to be incorporated into guidelines in the near future. (medscape.com)
  • Participants have received one prior platinum-based chemotherapy and one prior immune checkpoint inhibitor therapy either in combination or in sequence. (who.int)
  • Exclusion criteria: --Participants who have previously received docetaxel, KRAS G12C inhibitor, or any other systemic therapy for their locally advanced or metastatic NSCLC other than one platinum-based chemotherapy and one prior immune checkpoint inhibitor therapy. (who.int)
Protein5
  • In contrast, incubation of each protein with DNTB revealed one or more surface accessible cysteines (Supplementary Fig.?12 and Supplementary Table?2). (cell-signaling-pathways.com)
  • Lipocalin 10 is essential for protection against inflammation-triggered vascular leakage by activating LDL receptor-related protein 2-slingshot homologue 1 signalling pathway. (uc.edu)
  • Ku70/80 forms a complex with the DNA-dependent protein kinase catalytic subunit (DNA-PKcs) to form the full DNA-dependent protein kinase, DNA-PK [7]. (termedia.pl)
  • Checkpoint kinase 2 (CHEK2), a cell cycle checkpoint regulator gene, codes for a kinase protein activated in response to radiation and other agents that cause breaks in the DNA. (termedia.pl)
  • The protein encoded by this gene is a cell cycle checkpoint regulator and putative tumor suppressor. (affbiotech.com)
International Centre for Kinase Profiling1
  • At the International Centre for Kinase Profiling (ICKP) we understand that ascertaining how your compound behaves in relation to the multitude of related enzymes is critical. (mrc.ac.uk)
Chk24
  • G 2 /M arrest was associated with DNA damage as indicated by phosphorylation of H 2 A.X at Ser139 and activation of checkpoint kinase 2 (Chk2) in all the three cell lines. (aspetjournals.org)
  • To further establish the involvement of Chk2 in DIM-mediated G 2 /M arrest, cells were transfected with dominant-negative Chk2 (DN-Chk2). (aspetjournals.org)
  • Blocking Chk2 activation by DN-Chk2 completely protected cells from DIM-mediated G 2 /M arrest. (aspetjournals.org)
  • These results clearly indicate the requirement of Chk2 activation to cause G 2 /M arrest by DIM in ovarian cancer cells. (aspetjournals.org)
Mitotic3
  • These checkpoints may stop the cell cycle after DNA damage, loss of DNA replication or disruption of the mitotic spindle, in order for repair processes to take place. (tocris.com)
  • Cyclin dependent-kinase 2 (CDK2) plays important functions during the mitotic cell cycle and also facilitates several key events during germ cell development. (lu.se)
  • Strategies that increase replicative stress while lowering cell cycle checkpoint thresholds may allow unrepaired DNA damage to be inappropriately carried forward in replicating cells, leading to mitotic catastrophe and cell death. (bmj.com)
Proteins2
  • HEC is one of several proteins involved in spindle checkpoint signaling. (wikipedia.org)
  • As discussed in Supplementary Note?2, among several proteins tested, only ERK2 showed a characteristic change in the absorption spectrum, consistent with thiol addition. (cell-signaling-pathways.com)
CHEK21
  • CHEK2 is a cell cycle checkpoint regulator, and the CHEK2*1100delC germline mutation leads to loss of function and increased breast cancer risk. (nih.gov)
Control Kinases3
  • Checkpoint control kinases is a term used to describe a group of enzymes that regulate progression of a cell through the cell cycle. (tocris.com)
  • Checkpoint control kinases function to halt the cell cycle at these critical points. (tocris.com)
  • Tocris offers the following scientific literature for Checkpoint Control Kinases to showcase our products. (tocris.com)
Anaplastic lympho1
  • Participants with epidermal growth factor receptor (EGFR)-sensitizing mutation and/or anaplastic lymphoma kinase (ALK) rearrangement by local testing. (who.int)
Mps11
  • Kinetochore localization and microtubule interaction of the human spindle checkpoint kinase Mps1. (mpg.de)
Phosphorylation1
  • Rad53 phosphorylation/activation is elicited when unrepaired meiosis-specific DSBs escape the recombination checkpoint. (unimi.it)
Receptor2
  • Ephrin family members receptor tyrosine kinases are mediators of angiogenesis that may also regulate endothelial barrier function in the lung. (biospraysehatalami.com)
  • An Introduction and Overview of RON Receptor Tyrosine Kinase Signaling. (uc.edu)
Pyruvate kinase1
  • It has been reported that lung cancer cells exhibit upregulated expression of all key glycolytic enzymes [hexokinase 2 (HK2), phosphofructokinase and pyruvate kinase (PK)] ( 13 ), suggesting that the essential enzymes of the aerobic glycolytic pathway have a critical role in the development of lung carcinoma. (spandidos-publications.com)
Cyclin4
  • Other G 2 /M regulatory molecules such as Cdc25C, Cdk1, cyclin B1 were down-regulated by DIM. (aspetjournals.org)
  • Cell-cycle arrest was associated with the engagement of checkpoint kinase 2-cell division cycle 25C-cyclin-dependent kinase 1/cyclin B1 signaling. (bioone.org)
  • It was found that activation of the upstream kinase S-phase-specific cyclin-dependent kinase (Cdk) 2 was required for robust activation of ATR in response to numerous and diverse chemotherapeutic agents, and that Cdk2-mediated ATR activation promoted cell survival after treatment with many drugs. (ascopost.com)
  • It was identified that the nuclear division cycle 80, cyclin B2 and topoisomerase 2‑α may serve important roles in adrenocortical tumor development. (cancerindex.org)
Mutation1
  • Sequence analysis of these genes is being used to identify BRCA1/2 mutation carriers, though these efforts are hampered by the high frequency of variants of unknown clinical significance (VUSs). (jci.org)
Apoptosis1
  • Blocking ROS generation by N -acetyl cysteine protects the cells from DIM-mediated G 2 /M arrest and apoptosis. (aspetjournals.org)
Reactive oxygen1
  • JAM3 knockdown induced reactive oxygen species and syncytin 2 expression in trophoblasts. (bioone.org)
Ovarian cancer1
  • SRA737 is currently being investigated in two Phase 1/2 clinical trials primarily focused on patients with ovarian cancer: SRA737-01, a monotherapy study, and SRA737-02, a drug combination study evaluating SRA737 potentiated by low dose gemcitabine. (salesandmarketingnetwork.com)
20231
Cancer7
  • Checkpoint immunotherapeutics are promising agents with potential to improve patient outcomes in several cancer types. (biomedcentral.com)
  • While many factors are involved in the etiology of cancer, it has been clearly established that diet significantly impacts risk of this disease [ 1 , 2 , 3 ]. (mdpi.com)
  • Molecular portraits of cell cycle checkpoint kinases in cancer evolution, progression, and treatment responsiveness. (uc.edu)
  • Cancer Immunotherapy Agilent xCELLigence RTCA handbook 2 Table of contents What is cancer immunotherapy? (technologynetworks.com)
  • According to the latest statistical report from the American Cancer Center from 2021, lung cancer has the second-highest incidence and the highest mortality rate among all malignancies ( 2 ). (spandidos-publications.com)
  • The male-to-female ratio in head and neck cancer is 2:1. (medscape.com)
  • 2001) Genome maintenance mechanisms for Control, 2:165-8, avec l'aimable permission des Kluwer preventing cancer. (who.int)
Spindle checkpoint2
  • PICH, a Centromere-Associated SNF2 Family ATPase, Is Regulated by Plk1 and Required for the Spindle Checkpoint. (mpg.de)
  • Plk1 regulates PICH, a centromere-associated SNF2 family translocase that is required for the spindle checkpoint. (mpg.de)
Replication1
  • In the presence of errors or damage during DNA replication, cell cycle checkpoint nodes and repair machinery work in concert to retard cell cycle progression until sufficient repair has been achieved. (bmj.com)
CDK21
  • A better understanding of the CDK2 substrates will help us to gain deeper insight into the functions of this universal kinase. (lu.se)
Rad533
  • DNA damage checkpoint response to accidental DSBs during mitosis requires the Rad53 effector kinase, whereas the meiosis-specific Mek1 kinase, together with Red1 and Hop1, mediates the recombination checkpoint in response to programmed meiotic DSBs. (unimi.it)
  • Altogether, these data indicate that Rad53 prevents sister chromatid segregation in the presence of unrepaired programmed meiotic DSBs, thus providing a salvage mechanism ensuring genetic integrity in the gametes even in the absence of the recombination checkpoint. (unimi.it)
  • Role of the Saccharomyces cerevisiae Rad53 checkpoint kinase in signaling double-strand breaks during the meiotic cell cycle / H. Cartagena-Lirola, I. Guerini, N. Manfrini, G. Lucchini, M.P. Longhese. (unimi.it)
Assay2
  • A luciferase assay using a plasmid containing the PXR response elements of CYP3A4 revealed that the increased CYP3A4 induction by siNEAT1_2 or siDAZAP1 was due to the increased transactivation by PXR. (aspetjournals.org)
  • Consistent with these observations, incubation of the ERK2BI-78D3 adduct (UV spectrum is shown in Supplementary Fig.?15a) with 5?mM glutathione for 30?min failed to rescue the activity of ERK2, as determined using an in vitro kinase assay (Supplementary Fig.?15c). (cell-signaling-pathways.com)
Chromosomes1
  • For a cell to progress through the cycle and replicate, it must pass through checkpoints between phases to ensure that DNA is replicated correctly and that chromosomes segregate. (tocris.com)
Regulate1
  • Collectively, this is the first study to demonstrate that the paraspeckle components NEAT1_2 and DAZAP1 negatively regulate CYP3A4 induction by PXR. (aspetjournals.org)
Cell cycle arrest1
Interaction2
  • Immunoprecipitation assays using PXR-overexpressing HepG2 (ShP51) cells revealed that PXR interacts with not only DAZAP1 but also NEAT1_2, a long noncoding RNA included in the paraspeckle, and that the interaction between PXR and NEAT1_2 was disassociated by rifampicin. (aspetjournals.org)
  • SIGNIFICANCE STATEMENT This study revealed that PXR interacts with paraspeckle components NEAT1_2 and DAZAP1 to suppress CYP3A4 induction by PXR, and the interaction is dissociated by PXR ligands. (aspetjournals.org)