• Discovery of a Novel Class of Triazolones as Checkpoint Kinase Inhibitors--Hit to Lead Exploration. (rcsb.org)
  • Therefore, compared to normal p53-proficient cells, p53-defective cells are more reliant on MK2 activity, which drives an alternative cell cycle checkpoint pathway that stabilizes the CKI inhibitors p27 Kip1 and Gadd45α in order to maintain G 1 /S and G 2 /M arrest after certain types of DNA damage 16 , 18 . (nature.com)
  • She already has a candidate in mind for the job: a new class of drugs called ATR kinase inhibitors. (yale.edu)
  • Inhibitors for c-Met and RON including small molecular weigh kinase inhibitors and neutralizing antibodies are in pre-clinical investigation and clinical trials. (oncotarget.com)
  • Several of the tyrosine kinase inhibitors have activity against both c-Met and RON kinases whereas the antibodies generally are target specific. (oncotarget.com)
  • Weighed against its homologs Plk1 (and its own connected signaling pathway) offers attracted much interest because overexpression of Plk1 can be firmly correlated with carcinogenesis (10 11 Furthermore inhibition of Plk1 using RNA disturbance (RNAi) or particular little molecule inhibitors causes development arrest or apoptosis in tumor cells (12-14). (biospraysehatalami.com)
  • Based on knowledge of kinase switch-control inhibition and using a combination of structure-based drug design and standard medicinal chemistry principles, we identified a novel series of dihydropyrimidone-based CSF1R kinase inhibitors displaying exquisite selectivity for CSF1R versus a large panel of kinases and non-kinase protein targets. (bvsalud.org)
  • Many small-molecule kinase inhibitors of CSF1R also inhibit the closely related kinases KIT, PDGFRA, PDGFRB, and FLT3, thus CSF1R suppression may be limited by off-target activity and associated adverse events. (bvsalud.org)
  • Treatment of patients with GIST with KIT kinase inhibitors generally leads to a partial response or stable disease but most patients eventually progress by developing secondary resistance mutations in KIT. (bvsalud.org)
  • 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)
  • Strategies of combining chemotherapeutics with (a) inhibitors of NF-κB or (b) inhibitors of checkpoint kinases, may therefore enhance the efficacy of current cancer therapies. (eurekaselect.com)
  • This review will be focused on recent progress made in combining traditional chemotherapeutic drugs with small molecule inhibitors of NF-κB and the checkpoint kinases, Chk1 and Chk2. (eurekaselect.com)
  • Due to the fact TRII is usually a constitutively lively kinase and TGF signaling usually requires TRI ALK activation, ALK is the principle target for designing tiny molecule inhibitors that block TGF signaling. (hifsignaling.com)
  • The G1 checkpoint is regulated by a multitude of molecules such as the retinoblastoma family of proteins, cyclins, cyclin dependent kinases (CDKs) and cyclin dependent kinase inhibitors (CDKis). (temple.edu)
  • The cyclin-dependent kinase (CDK) inhibitors p21 and p16 inhibit the activity of CDKs, such as CDK4. (medscape.com)
  • Another important class of tumor suppressor genes involved in cell cycle control and in the generation of human cancers is the cyclin-dependent kinase (CDK) inhibitors. (medscape.com)
  • N-SLIT2 amplifies reactive oxygen species production in response to the bacteria by activating p38 mitogen-activated protein kinase that in turn phosphorylates NCF1, an essential subunit of the NADPH oxidase complex. (elifesciences.org)
  • Chk1 facilitates the arrest of cell cycle progression and the inhibition of replication origin firing. (caltech.edu)
  • In human monocytic cell lines U-937 and THP-1, LeTx induced cell cycle arrest in Go-Gi phase by rapid down-regulation of cyclin D1/D2 and checkpoint kinase 1 through MEK1 inhibition. (uwo.ca)
  • When the G2 or S checkpoint is abrogated by the inhibition of Chk1, p53- deficient cancer cells undergo mitotic catastrophe and eventually apoptosis, whereas normal cells are still arrested in the G1 phase. (biovendor.com)
  • A significant inhibition on cell growth, induction of apoptosis and cell cycle arrest were observed in 786-O and 769-P cells after kaempferol treatment compared with the control group. (nih.gov)
  • We show that Cdk1 inhibition leads to fatal sister chromatid alignment errors and mitotic arrest in the spindle checkpoint. (eur.nl)
  • Combined Aurora kinase and EGFR targeting using a monoclonal anti-EGFR antibody was more effective compared to single EGFR and Aurora kinase inhibition. (oncotarget.com)
  • Inhibition of CK2 activity by its selective inhibitor CX-4945 impaired the first polar body extrusion and arrested oocytes at M I stage, accompanied by the presence of BubR1 at kinetochores, indicative of activated SAC. (biomedcentral.com)
  • 6 , 7 Therefore, the inhibition of cancer cell proliferation by inducing cell cycle arrest and apoptosis is being an important preventive strategy against cancer. (jcpjournal.org)
  • The WEE-1 kinase is a key regulator of several cell cycle checkpoints including G2/M. WEE-1 inhibition can force cells in a state of arrest to continue the cell cycle, ultimately leading to cell death. (almacgroup.com)
  • Therefore, in this work investigated the effects of combined selective inhibition of tropomyosin kinase B receptor (TrkB) and epidermal growth factor receptor (EGFR) on the viability of GBM cells and in vivo GBM model. (ufrgs.br)
  • Inhibition of DNA-PKcs activity via a small interfering RNA or a kinase inhibitor results in mitosis delay, abnormal spindle formation, and chromosome misalignment. (amegroups.org)
  • All-trans retinoic acid (atRA) mediated growth inhibition results in the arrest of the cell cycle during the G1 phase in CAOV3 cells but not SKOV3 ovarian carcinoma cells. (temple.edu)
  • 2) Secondly, we sought to define how cells negatively regulate cytokinesis through investigation of Dma1p, a spindle checkpoint protein implicated in inhibition of cytokinesis. (umassmed.edu)
  • 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)
  • Replication blockages activate the ATR kinase which, in turn, activates the downstream effector kinase Chk1 through the mediator protein, Claspin. (caltech.edu)
  • ATR-Chk1-mediated protein degradation of Cdc25A protein phosphatase is also a mechanism conferring intra-S-phase checkpoint activation. (kegg.jp)
  • Check point kinase 1 (Chk1) is a serine / threonine protein kinase and a key mediator in the DNA damage-induced checkpoint network. (biovendor.com)
  • Chk1 is an evolutionarily conserved protein kinase that functions to ensure genomic integrity upon genotoxic stress. (biovendor.com)
  • The focus of this study is the role of protein kinase Chk1 and the phosphatase Cdc25A in the DNA replication checkpoint. (vt.edu)
  • In the absence of active Chk1, Cdc25A activates cyclin dependent kinases (Cdks) allowing the cell to progress into S or M phase. (vt.edu)
  • Chk1 regulates cell cycle arrest in the presence of unreplicated DNA in somatic cells by phosphorylating Cdc25A and leading to its degradation. (vt.edu)
  • In order to understand the function and regulation of Chk1 in checkpoints, the features of the MBT that activate Chk1 must be identified. (vt.edu)
  • The radiation-induced phosphorylation of p53 protein at serine 15, largely mediated by ATM kinase, was defective in AT, A(-T) and in 2/4 heterozygous carriers, while the G1 cell cycle checkpoint was disrupted in all AT and A(-T) cases, and in 3/10 AT heterozygotes. (nih.gov)
  • CK2 (casein kinase 2) is a serine/threonine-selective protein kinase that has been involved in a variety of cellular processes such as DNA repair, cell cycle control and circadian rhythm regulation. (biomedcentral.com)
  • CK2 (casein kinase 2) is an ubiquitously expressed and highly conserved serine/threonine protein kinase that forms a tetramer containing two catalytic (α and/or α´) subunits and two regulatory β subunits [ 1 ]. (biomedcentral.com)
  • A family of highly conserved serine-threonine kinases that are involved in the regulation of MITOSIS. (lookformedical.com)
  • An serine-threonine protein kinase that requires the presence of physiological concentrations of CALCIUM and membrane PHOSPHOLIPIDS. (lookformedical.com)
  • Mammalian aurora-A belongs to a multigenic family of mitotic serine/threonine kinases comprising two other members: aurora-B and aurora-C. In this review we will focus on aurora-A that starts to localize to centrosomes only in S phase as soon as centrioles have been duplicated, the protein is then degraded in early G1. (lookformedical.com)
  • A family of serine/threonine kinase Aurora constitutes a key regulator in the orchestration of mitotic events. (lookformedical.com)
  • 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)
  • Cycloheximide or Chk2 inhibitor pretreatment abrogated not only activation of Chk2 but also G 2 /M arrest and apoptosis mediated by DIM. (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 were further confirmed in Chk2 knockout DT40 lymphoma cells, in which DIM failed to cause cell cycle 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)
  • In response to DNA damage, the checkpoint kinase ATM phosphorylates and activates Chk2, which in turn directly phosphorylates and activates p53 tumor suppressor protein. (kegg.jp)
  • Whereas damage signals of cells activate p53 via CHK2 to repair damaged DNA, leading to cell cycle arrest. (jcpjournal.org)
  • The protein is phosphorylated in mitosis and in response to activation of the spindle checkpoint, and disappears when cells transition to G1 phase. (wikipedia.org)
  • In addition cells have evolved a damage-sensing checkpoint system whereby the cells delay entry into mitosis until the break has been repaired. (brandeis.edu)
  • We found that Plk1 suppressed the activity of RSK1 during embryonic mitosis and that Plk1 was inhibited during embryonic diapause and mitotic arrest. (biospraysehatalami.com)
  • In Xenopus laevis, early embryonic development consists of twelve rapid cleavage cycles between DNA replication (S) and mitosis (M) without checkpoints or gap phases. (vt.edu)
  • The model was updated with additional interactions, such as those including Myt1, a second inhibitor kinase, and lamin proteins, which become phosphorylated at the onset of nuclear envelope breakdown (NEB) at entry into mitosis. (vt.edu)
  • The checkpoint original model represents the activity of Cdc25 phosphatase on the mitosis promoting factor (MPF) that leads the cell into mitosis. (vt.edu)
  • Aurora kinase C is a chromosomal passenger protein that interacts with aurora kinase B in the regulation of MITOSIS. (lookformedical.com)
  • An aurora kinase that localizes to the CENTROSOME during MITOSIS and is involved in centrosome regulation and formation of the MITOTIC SPINDLE. (lookformedical.com)
  • An aurora kinase that is a component of the chromosomal passenger protein complex and is involved in the regulation of MITOSIS. (lookformedical.com)
  • Growth-inhibitory effects of DIM were mediated by cell cycle arrest in G 2 /M phase in all the three cell lines. (aspetjournals.org)
  • This gene encodes a cytoplasmic protein implicated in regulation of the mitotic spindle checkpoint, a regulatory pathway that monitors chromosome segregation during cell division to ensure the proper distribution of chromosomes to daughter cells. (wikipedia.org)
  • In this model, 16e was shown to abrogate topotecan-induced cell cycle arrest in a dose dependent manner. (rcsb.org)
  • Aging kidney and CKD share many common characteristic features with increased cellular senescence, a conserved program characterized by an irreversible cell cycle arrest with altered transcriptome and secretome. (frontiersin.org)
  • Cellular senescence is characterized by an irreversible and permanent cell cycle arrest coupled with altered transcriptome and secretome. (frontiersin.org)
  • In response to DNA damage, a synthetic lethal relationship exists between the cell cycle checkpoint kinase MK2 and the tumor suppressor p53. (nature.com)
  • These findings establish a mechanism for co-targeting DNA damage-induced cell cycle checkpoints in combination with repair of cisplatin-DNA lesions in vivo using RNAi nanocarriers, and motivate further exploration of ASL as a generalized strategy to improve cancer treatment. (nature.com)
  • 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 is required for checkpoint mediated cell cycle arrest in response to DNA damage or the presence of unreplicated DNA. (caslab.com)
  • The ATR kinase communicates DNA damage to the cell and activates DNA damage checkpoints, which arrest the cell cycle to provide time for repairs. (yale.edu)
  • Eukaryotic cells respond to DNA damage by activating signaling pathways that promote cell cycle arrest and DNA repair. (kegg.jp)
  • 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)
  • 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)
  • 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)
  • However, THP-1 cells adaptively adjusted to LeTx and overrode cell cycle arrest by activating the PI3K/Akt signaling pathway. (uwo.ca)
  • Recovery from cell cycle arrest was required before recovering from on-going MEK1 cleavage and suppression of TNF-a production. (uwo.ca)
  • Flow cytometry analysis showed that VALD-3 triggered cell cycle arrest and induced apoptosis of breast cancer cells. (researchsquare.com)
  • This study is the first to show that VALD-3 induces apoptosis and cell cycle arrest in human breast cancer cells by suppressing Wnt/β-catenin signaling, indicating that it could be a potential drug for the treatment of breast cancer. (researchsquare.com)
  • Cell department is controlled through cooperation of different kinases. (biospraysehatalami.com)
  • cell cycle arrest. (biospraysehatalami.com)
  • Here we show that encysted embryos (cysts) of the primitive crustacean are ideal for such research because they undergo WNT7A complete cell cycle arrest when they enter diapause (a state of obligate dormancy). (biospraysehatalami.com)
  • You can find six phosphorylation sites in RSK1 that are crucial for its activation and its own subsequent part in substrate phosphorylation (21 22 Of the phosphorylation of Ser-380 can be very important to RSK1 activation traveling functions such as for example rules of gene manifestation and protein synthesis and cell cycle regulation as a downstream Nisoxetine hydrochloride kinase in the Mos-MAPK pathway (23). (biospraysehatalami.com)
  • however commonly used animal models are limited in that cell cycle arrest must be induced by treatment with drugs. (biospraysehatalami.com)
  • 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)
  • It is also involved in cell cycle arrest and apoptosis [17]. (termedia.pl)
  • It also directly binds to BubR1, a kinetochore-associated kinase implicated in the mitotic checkpoint, the major cell cycle control pathway in which unattached kinetochores prevent anaphase onset. (rupress.org)
  • This work adds to the elucidation of the molecular mechanisms behind cell cycle arrest preceding tumor cell apoptosis induced by ASncmtRNA knockdown. (uandes.cl)
  • Kaempferol has been shown to inhibit cell growth, induce apoptosis and cell cycle arrest in several tumors, but not in renal cell carcinoma (RCC). (nih.gov)
  • Cyclin-dependent kinase 1 (Cdk1) is absolutely essential for cell division. (eur.nl)
  • Downregulation of UCK2 induced cell cycle arrest and activated the TNFα/NFκB signalling pathway-related senescence-associated secretory phenotype to modify the tumour microenvironment. (biomedcentral.com)
  • In the present study, we found that knockdown of UCK2 induced cell cycle arrest through dual mechanisms in HCC and that targeting UCK2 promoted the secretory features involved in the senescence-associated secretory phenotype (SASP) and inflammasomes. (biomedcentral.com)
  • Cinobufotalin impedes Sw.71 cytotrophoblast cell line function via cell cycle arrest and apoptotic signaling. (tamu.edu)
  • When unreplicated or damaged DNA is present, cell cycle checkpoint pathways cause cell cycle arrest by inhibiting cyclin-dependent kinases (Cdks). (vt.edu)
  • During the cell cycle, there are two main checkpoints that regulate entrance into S and M phases. (vt.edu)
  • One goal of this work is to understand the developmental role and regulation of checkpoint signaling pathways due to its monitoring of DNA integrity within the cell. (vt.edu)
  • Another means of characterizing the unreplicated DNA checkpoint is through the use of mathematical modeling of the checkpoint-signaling cascade of the cell cycle. (vt.edu)
  • Treating SCCHN cell lines with a pan-Aurora kinase inhibitor resulted in defective cytokinesis, polyploidy and apoptosis, which was effective irrespective of the EGFR status. (oncotarget.com)
  • Our results demonstrate that combined targeting of EGFR and Aurora kinases represents a therapeutic means to activate cell cycle checkpoints and apoptosis in SCCHN. (oncotarget.com)
  • To investigate the mechanism of EESR-mediated cytotoxicity, HT29 cells were treated with various concentrations of EESR and the induction of cell cycle arrest and apoptosis was analyzed by flow cytometry, 4,6-diamidino-2-phenylindole staining, and Western blot analysis. (jcpjournal.org)
  • EESR induced cell cycle arrest at G2/M phase in a dose-dependent manner by modulating cyclin B, cyclin-dependent kinase 1 (CDK1), and CDK inhibitor p21 expression. (jcpjournal.org)
  • EESR possessing antioxidant activity efficiently inhibits proliferation of HT29 cells by inducing both cell cycle arrest and apoptosis. (jcpjournal.org)
  • 8 , 9 Cell cycle program is regulated by cyclin/cyclin-dependent kinase (CDK) complexes. (jcpjournal.org)
  • TG 003 signaling dynamics and to induce cell cycle arrest and apoptosis in ERK-dependent cancers. (cell-signaling-pathways.com)
  • It is a catalytic subunit of the protein kinase complex that is important for cell cycle G1 phase progression. (thermofisher.com)
  • Ectopic kinase overexpression in any culture cell line leads to polyploidy and centrosome amplification. (lookformedical.com)
  • We suggest that these effects be mediated by the activation of a G1/S checkpoint, resulting in a cell cycle arrest, due to induced damage in the DNA molecule. (ufrgs.br)
  • Many chemotherapeutic agents and ionizing radiation induce not only apoptotic signaling pathways, but also survival responses such as DNA damage responses and cell cycle arrest, which allow for DNA repair. (eurekaselect.com)
  • Two main DNA damage responses include the activation of the anti-apoptotic transcription factor NF-κB and the activation of cell cycle checkpoint kinases. (eurekaselect.com)
  • Other authors have shown attenuated germ cell apoptosis SB-742457 kinase inhibitor following antioxidant therapy. (hifsignaling.com)
  • This effect is counteracted by Dma1p, which normally inhibits the SIN during checkpoint activation to preserve cell viability until damage is repaired. (umassmed.edu)
  • p53 is a transcription factor that participates in cell cycle checkpoint processes and apoptosis. (lu.se)
  • Treatment with the novel cyclophilin inhibitor NV651, presented a potent antiproliferative effect in HCC cell lines via cell cycle perturbations arresting cells in the mitotic phase. (lu.se)
  • For example, the TP53 gene, located on chromosome 17, encodes a 53-kd nuclear protein that functions as a cell cycle checkpoint. (medscape.com)
  • Activation of p21 or p16 therefore causes cell cycle arrest. (medscape.com)
  • The p19ARF protein, which is encoded by the same locus as p16, also leads to cell cycle arrest by inhibiting the ability of MDM2 to inactivate TP53. (medscape.com)
  • Tocris offers the following scientific literature for Checkpoint Control Kinases to showcase our products. (tocris.com)
  • It interacts with a mitotic regulator, and its expression is required to efficiently activate the spindle checkpoint. (wikipedia.org)
  • Uridine-cytidine kinase 2 (UCK2), a key regulator of pyrimidine metabolism, is elevated during hepatocellular carcinoma (HCC) development and exhibits carcinogenic effects. (biomedcentral.com)
  • Knocking out SOG1 in the fast weel background restores replication stress sensitivity, demonstrating that SOG1 is an important secondary checkpoint regulator in plants that fail to activate the intra-S-phase checkpoint. (muni.cz)
  • The mitotic kinase monopolar spindle 1 (Mps1) is a key regulator of the Spindle assembly checkpoint, which ensures the correct chromosome segregation. (lu.se)
  • Cyclin-dependent kinases (CDKs) are key regulatory enzymes, each consisting of a catalytic CDK subunit and an activating cyclin subunit. (kegg.jp)
  • All of these members contain a conserved C-terminal amino acid sequence termed the polo box domain which provides a docking site for certain proteins (1) and a kinase domain which is predicted to activate many protein kinases including Aurora A/B PKA ERK1/2 RSK1/2 Akt/PKB and MEK1 (2). (biospraysehatalami.com)
  • GSE-related anti-cancer activity mostly relies on the induced increase in reactive oxygen species, followed by the orchestrated down- and up-regulation of several key-molecular pathways, including MAPK kinases, PI3K/Akt, NF-kB, cytoskeleton proteins and metalloproteinases. (oatext.com)
  • The sensitivity of the enzyme can also be increased by PHORBOL ESTERS and it is believed that protein kinase C is the receptor protein of tumor-promoting phorbol esters. (lookformedical.com)
  • We characterized the ATM protein expression in immortalized cells from AT and AT-variant patients, and heterozygotes and correlated it with two ATM-dependent radiation responses, G1 checkpoint arrest and p53-Ser 15 phosphorylation. (nih.gov)
  • However, this limited expression of ATM protein provides no benefit regarding the ATM-dependent responses related to G1 arrest and p53-ser15 phosphorylation. (nih.gov)
  • 10] "Large-scale phosphorylation analysis of alpha-factor-arrested Saccharomyces cerevisiae. (tcdb.org)
  • This kinase was shown to be responsible for the phosphorylation of retinoblastoma gene product (Rb). (thermofisher.com)
  • This phosphorylation is regulated by the ataxia telangiectasia mutated (ATM) and the Rad3-related (ATR) kinases in response to various genotoxic stresses, making it a critical regulatory element of DNA-PKcs ( 6 , 10 ). (amegroups.org)
  • Mutations in the RON and c-Met promoters are known to enhance transcription and point mutations have been identified that enhance tyrosine kinase activity [ 19 - 21 ]. (oncotarget.com)
  • Vimseltinib (DCC-3014) is an oral, switch control tyrosine kinase inhibitor specifically designed to selectively and potently inhibit CSF1R by exploiting unique features of the switch control region that regulates kinase conformational activation. (bvsalud.org)
  • The majority of gastrointestinal stromal tumors (GIST) harbor constitutively activating mutations in KIT tyrosine kinase. (bvsalud.org)
  • In this context, tyrosine kinase receptors have a key role. (ufrgs.br)
  • In response to DNA-damaging agents, the wild-type p53-activated fragment 1 (WAF1 also known as p21) is an important downstream effector in the p53-specific growth arrest pathway. (lu.se)
  • We previously showed that the ESCRT-III subunit IST1 binds the cysteine protease CAPN7 (Calpain-7) and that CAPN7 is required for both efficient abscission and NoCut checkpoint maintenance (Wenzel <i>et al. (elifesciences.org)
  • 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)
  • DNA-dependent protein kinase catalytic subunit (DNA-PKcs), a key component of the non-homologous end-joining (NHEJ) pathway, is involved in DNA double-strand break repair, immunocompetence, genomic integrity, and epidermal growth factor receptor signaling. (amegroups.org)
  • The catalytic subunit of DNA-dependent protein kinase (DNA-PKcs) is the key component of the non-homologous end-joining (NHEJ) pathway for DNA double-strand break (DSB) repair and is required for cellular resistance to ionizing radiation (IR) ( 1 , 2 ). (amegroups.org)
  • We demonstrate that lack of FAS1 activity results in the activation of an ATAXIA TELANGIECTASIA MUTATED (ATM)- and SUPPRESSOR OF GAMMA-RESPONSE 1 (SOG1)-mediated G2/M-arrest that renders the ATR and WEE1 checkpoint regulators redundant. (muni.cz)
  • During oocyte maturation RSK both phosphorylates and down-regulates Myt1 causing prophase I arrest (24). (biospraysehatalami.com)
  • We report that CK2 is essential for porcine oocyte meiotic maturation by regulating spindle assembly checkpoint (SAC). (biomedcentral.com)
  • 1) We first sought to characterize the positive timing mechanism that signals cytokinesis though a detailed investigation of Sid1p, a protein kinase essential for activation of ring constriction. (umassmed.edu)
  • We found Sid1p is additionally controlled by Cyclin Dependent Kinase activity, uncovering an important link between mitotic events and initiation of cytokinesis. (umassmed.edu)
  • It is proposed to regulate Cdc2 kinase activity during spindle checkpoint arrest. (wikipedia.org)
  • The zinc finger domain of Tzfp binds to the tbs motif located at the upstream flanking region of the Aie1 (aurora-C) kinase gene. (lookformedical.com)
  • Therefore, we conclude that DDK regulates a largely checkpoint-independent role of Claspin function. (caltech.edu)
  • The protein encoded by this gene belongs to the Ser/Thr protein kinase family. (caslab.com)
  • Genotoxic stress which specifically affects cells in S-phase is detected by the replication checkpoint. (caltech.edu)
  • c-Met and receptor originated from nantes (RON) are structurally related transmembrane phosphotyrosine kinase receptors. (oncotarget.com)
  • We analyzed the clinical data and performed immunohistochemistry for Epidermal growth factor receptor (EGFR) and Aurora kinase A (Aurora-A) expression in 180 SCCHN patients. (oncotarget.com)
  • We characterized Xenopus Claspin as a kinase substrate of DDK which forms a stable nuclear complex with Cdc7 and Drf1 under both arrested and unperturbed replication conditions. (caltech.edu)
  • p53 and its transcriptional targets play an important role in both G1 and G2 checkpoints. (kegg.jp)
  • 12] "Proteome-wide identification of in vivo targets of DNA damage checkpoint kinases. (tcdb.org)
  • CAPN7 proteolytic activity is also required for abscission and checkpoint maintenance. (elifesciences.org)
  • Without CENP-E, diminished levels of BubR1 are recruited to kinetochores and BubR1 kinase activity remains at basal levels. (rupress.org)
  • CENP-E binds to and directly stimulates the kinase activity of purified BubR1 in vitro. (rupress.org)
  • Thus, CENP-E is required for enhancing recruitment of its binding partner BubR1 to each unattached kinetochore and for stimulating BubR1 kinase activity, implicating it as an essential amplifier of a basal mitotic checkpoint signal. (rupress.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)
  • The activity of this kinase is restricted to the G1-S phase, which is controlled by the regulatory subunits D-type cyclins and CDK inhibitor p16(INK4a). (thermofisher.com)
  • Works in various organisms have revealed that the kinase is involved in centrosome separation, duplication and maturation as well as in bipolar spindle assembly and stability. (lookformedical.com)
  • Comparing pan-Aurora kinase and Aurora-A targeting hints towards a strong and clinically relevant biological effect mediated via Aurora kinase B. Taken together, our findings characterize a new poor risk group in SCCHN patients defined by elevated EGFR and Aurora-A protein expression. (oncotarget.com)
  • Structure-guided point mutations in either CAPN7 MIT domain disrupted IST1 binding in vitro and in cells, and depletion/rescue experiments showed that the CAPN7-IST1 interaction is required for: 1) CAPN7 recruitment to midbodies, 2) efficient abscission, and 3) NoCut checkpoint arrest. (elifesciences.org)
  • The resulting impairment of the G2-M checkpoint would prevent cancer cells from repairing induced DNA damage, considerably enhancing the effect of the DNA damaging therapy and thus optimizing the therapeutic outcome. (almacgroup.com)
  • Furthermore, we found that aberrant SIN activation can override a microtubule-damage-induced spindle checkpoint arrest. (umassmed.edu)
  • Degradation of Mos inactivates p90RSK when mature metaphase II-arrested oocytes are fertilized (25-27) and Myt1 forms a complex with Plk1. (biospraysehatalami.com)