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Aurora KinasesAurora Kinase AAurora Kinase BAurora Kinase CProtein-Serine-Threonine KinasesSmall Molecule LibrariesProtein Kinase InhibitorsProtein KinasesMitosisPhosphatidylinositol 3-KinasesMAP Kinase Signaling SystemCell Line, TumorPhosphorylationSpindle ApparatusPiperazinesChromosome SegregationCalcium-Calmodulin-Dependent Protein KinasesProtein BindingBenzamidessrc-Family KinasesAzepinesKinetochoresMolecular Sequence DataOrganophosphatesCell Cycle ProteinsApoptosisSignal TransductionPyrimidinesAmino Acid SequenceHeLa CellsAntineoplastic AgentsCell ProliferationMutationProtein Kinase CM Phase Cell Cycle CheckpointsEnzyme Inhibitorsp38 Mitogen-Activated Protein KinasesCell CycleCyclic AMP-Dependent Protein KinasesCytokinesisModels, MolecularCentrosomeBinding SitesPolyploidyMicrotubule-Associated ProteinsMitogen-Activated Protein Kinase 1Cell LinePyrazolesDrug Evaluation, PreclinicalHistonesAneugensChondromaProtein-Tyrosine KinasesMolecular StructureBlotting, WesternJNK Mitogen-Activated Protein KinasesMitogen-Activated Protein Kinase KinasesCell Adhesion MoleculesRNA, Small InterferingCell Cycle CheckpointsCDC2 Protein Kinasep21-Activated KinasesMicrotubulesQuinazolinesMitogen-Activated Protein Kinase 3KineticsCyclin-Dependent KinasesModels, BiologicalAnaphaseProtein Structure, TertiaryNeoplasmsChromosomal Proteins, Non-HistoneCollagen Type XIMAP Kinase Kinase KinasesCreatine KinaseEnzyme ActivationBlastodiscRNA InterferenceTransfectionBase SequenceDose-Response Relationship, DrugDrug Screening Assays, AntitumorCells, CulturedXenograft Model Antitumor AssaysCasein Kinase IIPotoroidaeCell SurvivalInhibitory Concentration 50eIF-2 KinaseHigh-Throughput Screening AssaysReceptor Protein-Tyrosine KinasesCasein KinasesRNA, MessengerDrug DesignCell Physiological ProcessesNuclear ProteinsRibosomal Protein S6 KinasesPyruvate KinaseRecombinant ProteinsProto-Oncogene Proteins
InhibitorsInhibitionPhosphorylationProteinSerineMitosisBindsVitroPI3KMitoticChromosomalProliferationFamily kinasesCyclinSpindleActive conformationPathwaysApoptosisTumorsTyrosineEffectively inhibitEmbryonicCancerEGFRAssayEnzymesActivityPotent and selectiveActivateProteinsDependentMolecularAMPKTherapeuticBioactiveOverexpressionCdc2ProgressionClinicalCompoundCancersActivatorTumoursStem CellResistanceCentrosome
Inhibitors23
  • Kinase selectivity studiesshowed that AP24534 does not inhibit Aurora kinases, clearly distinguishing it from other T315I inhibitors in development. (others-signal.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)
  • This transformative new modality is expected to open a new chapter in drug discovery targeting kinases for which the development of clinical inhibitors has been difficult. (carnabio.com)
  • Several ATP-competitive inhibitors of RAF stabilize the active conformation of the kinase where the αC-helix is rotated toward the active site (αC-helix IN). (carnabio.com)
  • Thus, there are cases where conventional ATP-competitive inhibitors are unable to sufficiently suppress the functions of kinase targets simply because the targets have a kinase-activity-independent function. (carnabio.com)
  • Significant research is currently underway on protein degraders targeting kinases that have a non-catalytic function independent to kinase activity and for which conventional small molecule inhibitors have not been successful in clinical trials. (carnabio.com)
  • Finally the last section will be devoted to a new class of compounds that are able to inhibit both mTOR complexes and the new dual inhibitors that are also adding activity against the phosphatydilinositol-3-kinase (PI3K) a key component of the main opinions loop involved in this pathway. (biomasswars.com)
  • This observation has provided rationale for combining several ongoing phase I clinical trials combining mTOR PI3K or AKT inhibitors with MAP/ERK kinase (MEK) inhibitors. (biomasswars.com)
  • First generation of mTOR inhibitors The first generation inhibitors of mTOR are derivatives of Rapamycin that specifically inhibit mTORC1. (biomasswars.com)
  • Several potent Aurora kinase inhibitors derived from 5H-benzo[c][1,8]naphthyridin-6-one scaffold were identified. (rcsb.org)
  • This communication describes the discovery of a novel series of Aurora kinase inhibitors. (rcsb.org)
  • The explanation for concentrating on the PI3K/mTOR pathway can be backed by R-121919 the association of elevated activity using a worse scientific final result.13 14 NVP-BEZ235(ref15) and GDC-0980(ref16) are small-molecule inhibitors of course I PI3K and mTOR (mTORC1 and mTORC2). (biomasswars.com)
  • However obstructing autophagy which affects cell growth is definitely synthetically lethal when combined with PI3K/mTOR inhibitors by a mechanism including receptor-interacting protein kinase 1 (RIP1)-dependent cell death. (biomasswars.com)
  • Within this review, we summarize the functions that all of the Aurora kinases has in cancer biology and mitosis, and discuss the binding modes of Aurora A kinase inhibitors, the spot elements in the binding sites and the fortunate inhibitor components. (survivinpathway.com)
  • Our report on the reported chemical scaffolds of Aurora A kinase inhibitors and their binding modes could give a of good use Letrozole ic50 framework from which new design strategies for inhibitors may be evaluated or produced. (survivinpathway.com)
  • In addition, we review the main pre-clinical and clinical studies concerning Aurora kinase inhibitors currently under investigation. (survivinpathway.com)
  • The extensive pre-clinical data supports the develop-ment of focused Aurora kinase inhibitors in certain tumefaction types. (survivinpathway.com)
  • Mount Sinai researchers have developed a novel method to identify aggressive early-stage lung cancers and target drugs known as aurora kinase inhibitors to tumors that are especially likely to respond. (bio-itworld.com)
  • The Mount Sinai team used a genomics network model to measure tumor invasiveness-distinguishing aggressive tumors from so-called "indolent" ones, which often cannot be told apart via chest CT scan-and identify those that will respond to aurora kinase inhibitors, molecules that can inhibit gene signature regulators. (bio-itworld.com)
  • They identified and tested aurora kinase inhibitors, including AMG900, as an effective treatment to intercept lung cancer progression in the models. (bio-itworld.com)
  • NTRC has developed a series of highly selective inhibitors of TTK enzyme activity that potently inhibit proliferation of human cancer cells and tumour growth in mouse models. (oncolines.com)
  • Different subclasses of PI3K/mTOR, Aurora and EZH2 inhibitors were identified that relate to different mechanisms of activity or different genetic targeting. (oncolines.com)
  • In addition, NTRC develops own novel targeted therapies based on small molecules, such as selective inhibitors of TTK (Mps1) protein kinase for chromosomal unstable tumours and inhibitors of the tryptophan metabolizing enzymes IDO1 and TDO for cancer immunotherapy. (oncolines.com)
Inhibition16
  • citation needed] Inhibition of Aurora B kinase by BI 811283 in cancer cells leads to the formation of cells with severely abnormal numbers of chromosomes (polyploid). (wikipedia.org)
  • Counterintuitively, inhibition of Aurora B kinase by BI 811283 actually causes the polyploid cells formed to continue dividing however, because these cells have severe chromosomal abnormalities, they eventually stop dividing or undergo cell death. (wikipedia.org)
  • Pre-clinical studies have demonstrated that BI 811283 selectively binds to and inhibits the Aurora B kinase protein leading to inhibition of growth and senescence in lung cancer cells in vitro. (wikipedia.org)
  • Auora kinase inhibitor MLN8054 binds to and inhibits Aurora kinase A, resulting in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregration, and inhibition of cell proliferation. (xcessbio.com)
  • 40-fold more selective inhibitory activity for Aurora A compared with Aurora B. In vitro, MLN8054 exhibits the activity of growth inhibition across various cell lines from diverse tissue origins with IC50 values ranging from 0.11 μM to 1.43 μM. (xcessbio.com)
  • Analysis of DNA content and indirect immunofluoresence demonstrates that SNS-314 induces defects in cytokinesis and spindle checkpoint that are consistent with Aurora kinase inhibition. (cogershop.com)
  • Analysis of SNS-314 treated tumors confirms that the anti-tumor activity is consistent with Aurora kinase inhibition. (cogershop.com)
  • Pfizer) plus Everolimus are underway (35 36 Furthermore preclinical data have shown that mTORC1 inhibition results in a hyperactivation of the PI3K pathway and simultaneous increase of the signaling through the mitogen-activated protein kinase kinase (MAPK) pathway (37) thus proving the presence of another opinions loop that connect the PI3K-AKT-mTOR with the MAPK pathway. (biomasswars.com)
  • In contrast simultaneous inhibition of PI3K-AKT and MAPK BIBR 953 pathways decreased cell viability and pointed towards as this combination as the most optimal way to effectively inhibit both pathways (38). (biomasswars.com)
  • Furthermore, pharmacological inhibition of MELK activity by small-molecule inhibitor OTSSP167 significantly inhibited cell proliferation, anchorage-independent colony formation, blocked cell cycle progression, and induced apoptosis in different NB cell lines including a drug-resistant cell line. (oncotarget.com)
  • Furthermore, this compound inhibited phosphorylation of histone H3 (pHH3) in mouse bone morrow upon oral administration, which is consistent with inhibition of Aurora kinase B activity. (rcsb.org)
  • It can inhibit the phosphorylation reaction through competing with adenosine triphosphate to bind to the catalytic region of the receptor tyrosine kinase, thereby blocking the down-proliferation signaling and inhibiting the activity of the tumor cell ligand-dependent HER-1/EGFR, thus achieving the inhibition of the proliferation of tumor cells. (lookchem.com)
  • We have previously demonstrated that PI3K/mTOR signaling inhibition sensitizes mesothelioma cells to medicines that are effluxed via ABCG2 transporter by inhibiting the function of ABCG2.19 With this study we aimed at identifying the underlying mechanisms responsible for sensitivity resistance towards PI3K/mTOR inhibition in a large panel of mesothelioma cell lines. (biomasswars.com)
  • 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)
  • Some studies have reported that the G2 M arrest induced by SP600125 may be due to inhibition of cyclin B Cdk1 kinase activity through an increase in p21 levels. (hsp90-inhibitors.com)
  • Description: Measuring inhibition of kinase activity in a biochemical assay. (guidetomalariapharmacology.org)
Phosphorylation7
  • The phosphorylation of IκBα by IκB kinase family have been so many identified, but the phosphorylation sites of IκBα by other kinases remain poorly understood. (researchsquare.com)
  • To identify the essential domains of IκBα for phosphorylation of IκBα by AURK, kinase assay was performed with a series of IκBα truncation mutants. (researchsquare.com)
  • Phosphorylation of Histone H3 on serine 10, a known Aurora B cellular target, is inhibited with an EC50 of ~9nM following treatment of cells with SNS-314. (cogershop.com)
  • In addition studies on HeLa cells using Plk1 siRNA interference and overexpression showed that phosphorylation of RSK1 increased upon interference and decreased after overexpression suggesting that Plk1 inhibits RSK1. (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)
  • Interestingly, knockdown of MELK expression significantly reduced the phosphorylation of target protein Retinoblastoma (pRb) and inhibited NB cell growth. (oncotarget.com)
  • At present, it remains poorly understood how DDK docks onto the helicase and how the kinase targets distal Mcm subunits for phosphorylation. (imperial.ac.uk)
Protein25
  • BI 811283 is a small molecule inhibitor of the Aurora B kinase protein being developed by Boehringer Ingelheim for use as an anti-cancer agent. (wikipedia.org)
  • The Aurora B kinase protein (also known as STK12) is one of a family of proteins that plays an essential role in the alignment, movement and separation of chromosomes during cell division. (wikipedia.org)
  • 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 is a component of the chromosomal passenger protein complex and is 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)
  • 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)
  • 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)
  • By using a direct in vivo shRNA screen, we show that liver cancer cells that have mutations in the gene encoding the tumor suppressor protein p53 (Trp53 in mice and TP53 in humans) and that are driven by the oncoprotein NRAS become addicted to MYC stabilization via a mechanism mediated by aurora kinase A (AURKA). (scite.ai)
  • MLN8054 is an aurora kinase inhibitor MLN8054, which is an orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase with potential antineoplastic activity. (xcessbio.com)
  • Aurora A is involved with centrosome readiness, spindle assembly, and uneven protein localization throughout mitosis. (others-signal.com)
  • Immune system Nevertheless, nuclear launch of Bora isn't the only system by which its service of Aurora A is controlled since the bora mutant phenotype can be rescued by Bora fused to a signal, which keeps the protein in the cytoplasm, or fused to a localization signal, which maintains the protein in the nucleus until nuclear envelope breakdown. (others-signal.com)
  • 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)
  • The announcement that Kymera Therapeutics, a company pioneering targeted protein degradation, entered into a strategic collaboration with Sanofi to develop and commercialize first-in-class protein degrader therapies targeting IRAK4 in patients with immune-inflammatory diseases highlights the growing interest in clinical applications of small molecule mediated kinase degradation. (carnabio.com)
  • Most of the protein degraders currently under development are heterobifunctional molecules which contain one moiety that binds a desired target protein and another that binds an E3 ligase, joined by a linker. (carnabio.com)
  • Targeting of kinases that have a non-kinase catalytic function by protein degradation creates the potential to discover new therapeutic opportunities. (carnabio.com)
  • DREADD receptors (Designer Receptor Exclusively Activated by Designer Drugs) are engineered G-protein receptors which are exclusively activated by the inert-molecule CNO (clozapine-N-oxide) and to a lesser degree clozapine. (uw.edu)
  • The Aurora kinases really are a group of three highly homologous Ser/ Thr protein kinases, including Aurora A, B and C. (survivinpathway.com)
  • Patients characterized by elevated EGFR and elevated Aurora-A protein expression in tumor tissue represent a risk group with poor disease-free and overall survival (EGFR low Aurora-A low versus EGFR high Aurora-A high , p=0.024). (oncotarget.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)
  • Serine/threonine-protein kinase component of the chromosomal passenger complex (CPC), a complex that acts as a key regulator of mitosis. (nih.gov)
  • Dorsomorphin dihydrochloride is a potent inhibitor of AMP-activated protein kinase (AMPK) (K i = 109 nM). (tocris.com)
  • Dorsomorphin dihydrochloride also inhibits bone morphogenetic protein (BMP) type I receptors (ALK2, ALK3 and ALK6), promotes cardiomyogenesis in mouse embryonic stem cells (ESCs) in vitro and promotes neural differentiation of hPSCs as part of a chemical cocktail. (tocris.com)
  • Role of AMP-activated protein kinase in mechanism of MetF. (tocris.com)
  • The protein kinase TTK is a component of the spindle assembly checkpoint, a protein machinery that regulates correct segregation of chromosomes over daughter cells during cell division. (oncolines.com)
  • A substance that inhibits that activity of the Hsp90 heat shock protein. (hsp90-inhibitors.com)
Serine5
  • A family of highly conserved serine-threonine kinases that are involved in the regulation of MITOSIS. (lookformedical.com)
  • A family of serine/threonine kinase Aurora constitutes a key regulator in the orchestration of mitotic events. (lookformedical.com)
  • AURK significantly promotes activation of IκBα at serine 32, but not serine 36 residues, unlike IκB kinase (IKK) family proteins activate both IκBα serine residues. (researchsquare.com)
  • Aurora kinases constitute a family of serine-threonine kinases that are strongly associated with cancer. (cogershop.com)
  • Development through mitosis depends upon three major regulatory systems, each involving several serine/threonine kinases, referred to as mitotic kinases. (survivinpathway.com)
Mitosis8
  • An aurora kinase that localizes to the CENTROSOME during MITOSIS and is involved in centrosome regulation and formation of the MITOTIC SPINDLE. (lookformedical.com)
  • Aurora A localizes in mitosis to the spindle poles and to spindle microtubules and is thought to regulate spindle assembly. (xcessbio.com)
  • Contrary to cells treated with a siRNA, cells treated with siRNAs against Bora often displayed multipolar spindles in mitosis, a phenotype that is also seen upon TPX2 RNAi Geneticin distributor and after injection of antibodies blocking Aurora A function. (others-signal.com)
  • Aurora A and B are essential in mitosis. (cogershop.com)
  • however, Aurora C can complement Aurora B kinase activity in mitosis. (cogershop.com)
  • 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)
  • Mechanistically, we show that YK-4-279 inhibits the formation of kinetochore microtubules, with treated cells showing a broad range of abnormalities including multipolar, fragmented and unseparated spindles, together leading to disrupted progression through mitosis. (researcher-app.com)
  • Our results strongly support the idea that SP600125 inhibits cell proliferation by inhibiting mitosis through extended tubulin polymerization. (hsp90-inhibitors.com)
Binds4
  • BI 811283 is a small molecule drug that selectively binds to the ATP binding pocket of Aurora B kinase, inhibiting its function in cell division. (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)
  • Methods: Previously we observed that aurora kinase (AURK) binds IκBα in the cell. (researchsquare.com)
  • Substantial reductions will be anticipated to require at least two modifications at nonproximal residues?a forecast consistent with findings from our mutagenesis screen, though mutations that destabilize the inactive conformation of ABL to which AP24534 binds, including T315I and E255V, lead to small reductions in binding affinity. (others-signal.com)
Vitro3
  • Bora can activate Aurora A in vitro. (others-signal.com)
  • Although in Drosophila, Bora so far may be the only known activator of Aurora A, many in vitro activators of Aurora A have now been discovered in other creatures. (others-signal.com)
  • SNS-314 is an ATP-competitive, selective, and potent nanomolar inhibitor of aurora kinases in vitro. (cogershop.com)
PI3K1
  • The phosphatydilinositol-3-kinase (PI3K)/mammalian focus on of rapamycin (mTOR) pathway is a main concentrate of attention for cancers researchers before decade. (biomasswars.com)
Mitotic3
Chromosomal1
  • Abnormally elevated levels of Aurora B kinase, cause unequal chromosomal separation during cell division, resulting in the formation of cells with abnormal numbers of chromosomes, which are both a cause and driver of cancer. (wikipedia.org)
Proliferation5
  • AKI603 inhibited cell proliferation and colony formation capacities in imatinib-resistant CML cells by inducing cell cycle arrest with polyploidy accumulation. (scite.ai)
  • In addition, MLN8054 selectively inhibits Aurora A over Aurora B in cultured cells, and inhibits cell proliferation by promoting G2/M accumulation and spindle defects in multiple cultured human tumor cells lines. (xcessbio.com)
  • SNS-314 inhibits cellular proliferation in the HCT116 colorectal carcinoma cell line with an EC50 of ~5nM. (cogershop.com)
  • Inhibits MSC proliferation. (hellobio.com)
  • Selective Effects of PD-1 on Akt and Ras Pathways Regulate Molecular Components of the Cell Cycle and Inhibit T Cell Proliferation[J]. Science signaling, 2012, 5(230): ra46-ra46. (ijsciences.com)
Family kinases3
  • Some kinases are essential scientific objectives of imatinib, nilotinib, and/or dasatinib, although only dasatinib has been reported to inhibit all SRC family kinases. (others-signal.com)
  • This feature probably contributes to the relatively wide kinase specificity profile of AP24534, including VEGFR and FGFR family kinases, receptors perhaps not restricted by the three currently authorized BCR ABL drugs. (others-signal.com)
  • Mechanistic and evolutionary insights into isoform-specific 'supercharging' in DCLK family kinases. (liverpool.ac.uk)
Cyclin1
  • This compound is a highly cell-permeable purine compound that acts as an ATP-competitive inhibitor of cyclin dependent kinases (CDKs). (guidetoimmunopharmacology.org)
Spindle3
  • 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)
  • TPX2/ Aurora A binding is stimulated by the little GTPase Ran, which in turn is activated by RCC1, an exchange factor that is found on condensed chromatin and is involved with microtubule nucleation and spindle formation. (others-signal.com)
  • Therefore, unlike Bora, TPX2 appears to be specifically in charge of the spindle assembly purpose of Aurora A. To date, no TPX2 homolog has been discovered in Drosophila. (others-signal.com)
Active conformation1
  • In vertebrates, TPX2 prevents PP1 dependent dephosphorylation and therefore AZD5363 locks the kinase in its active conformation. (others-signal.com)
Pathways3
  • The term "oncotarget" encompasses all molecules, pathways, cellular functions, cell types, and even tissues that can be viewed as targets relevant to cancer as well as other diseases. (oncotarget.com)
  • After transfection, we treated transfected cells with 1µM of CNO or VEH (a control) for 5-30min and then lysed the cells with RIPA Buffer, and prepared samples for western blotting to detect activation of proteins of interest in the GPCR non-canonical signaling pathways (example: kinases and transcription factors). (uw.edu)
  • Farnesyltransferase inhibitor tipifarnib is well leurocristine tolerated, induces stabilization of disease, and inhibits farnesylation and oncogenic tumor survival pathways in patients with advanced multiple myeloma. (hsp90-inhibitors.com)
Apoptosis3
Tumors1
  • A genomic network model is used to identify aurora kinase inhibitor-sensitive lung tumors, new Illumina Accelerator start-ups are announced, AI algorithms are being used to improve prostate cancer identification and treatment, and a blood-based DNA methylation test can detect liver cancer. (bio-itworld.com)
Tyrosine1
Effectively inhibit1
  • Conclusion: Interfere of PD-1 expression can effectively inhibit the growth of hepatocarcinoma cell H22 in mice. (ijsciences.com)
Embryonic1
  • Maternal embryonic leucine zipper kinase (MELK) is known to modulate intracellular signaling and control cellular processes. (oncotarget.com)
Cancer12
  • the levels of Aurora B kinase are abnormally raised in many types of cancer. (wikipedia.org)
  • non-small cell lung, brain, head and neck, colorectal and ovarian cancer, where it is associated with worse treatment outcome and poorer overall survival. (wikipedia.org)
  • Furthermore, BI 811283 also inhibits the growth of pancreatic, colorectal and non-small cell lung cancer cells in vivo leading to tumour shrinkage. (wikipedia.org)
  • A class of exceptionally bioactive molecules known as reactive oxygen species (ROS) have been widely studied in the context of cancer. (bvsalud.org)
  • A recent study shows that MLN8054 sensitizes androgen-resistant prostate cancer to radiation by inhibiting Aurora A kinase, which is associated with sustained DNA double-strand breaks. (xcessbio.com)
  • SNS-314 is a potent small-molecule inhibitor of Aurora kinase that is being developed as a novel anti-cancer therapeutic agent. (cogershop.com)
  • Jones D, Noble M, Wedge SR, Robson CN, Gaughan L. Aurora A regulates expression of AR-V7 in models of castrate resistant prostate cancer . (ncl.ac.uk)
  • is known to exert anticancer effects, such as inducing cell cycle arrest, inhibiting metastasis, and overcoming immunotherapy resistance in breast cancer cells. (hindawi.com)
  • Clinically, it is mainly used in the treatment of incurable locally advanced or metastatic non-small cell lung cancer (NSCLC) and being used in combination with gemcitabine for first-line treatment of locally advanced unresectable or metastatic pancreatic cancer. (lookchem.com)
  • In November 2004, the product was first approved in the United States for the treatment of local advanced or metastatic non-small cell lung cancer (NSCLC) which has been undergone at least one time of chemotherapy failure. (lookchem.com)
  • Gefitinib is a kind of highly-specific anti-tumor targeted therapy drugs developed by the United Kingdom AstraZeneca, being the first molecular targeted drug for the treatment of non-small cell lung cancer. (lookchem.com)
  • Pembrolizumab versus Chemotherapy for PD-L1-Positive Non-Small-Cell Lung Cancer[J]. New England Journal of Medicine, 2016, 375(19): 1823-1833. (ijsciences.com)
EGFR1
Assay1
  • A comprehensive kinase interaction map for dasatinib was recently described, though assay differences preclude direct comparison of the kinase users of AP24534 and dasatinib. (others-signal.com)
Enzymes1
  • The molecules upon which enzymes may act are called substrates, and the enzyme converts the substrates into different molecules known as products. (hellobio.com)
Activity6
  • One such example is IRAK4, which has a non-catalytic function independent of kinase activity in addition to a catalytic function as a kinase. (carnabio.com)
  • FAK is an example where an important scaffolding function exists independently of kinase activity. (carnabio.com)
  • All kinases and related products sold by Carna, are manufactured in-house and delivered to you after stringent quality control, identity confirmation and activity assessment. (carnabio.com)
  • Our extensive portfolio of biotinylated kinases can be utilized not only in biochemical activity assays, but also for SPR data acquisition, binding assays using TR-FRET, AlphaScreen/AlphaLISA and other applications. (carnabio.com)
  • In particular, compound 21 (SNS-314) is a potent and selective Aurora kinase inhibitor that exhibits significant activity in pre-clinical in vivo tumor models. (rcsb.org)
  • Displays no significant activity on several structurally related kinases including ZAPK, SYK, PKC θ , PKA and JAK3. (tocris.com)
Potent and selective1
  • Subsequent SAR campaign provided a potent and selective pan Aurora inhibitor, which demonstrated potent target modulation and antiproliferative effects in the pancreatic cell line, MIAPaCa-2. (rcsb.org)
Activate1
  • For example, in the RAF family of kinases, A-RAF, B-RAF and C-RAF form homodimers or heterodimers and allosterically activate their binding partners independent of kinase activation. (carnabio.com)
Proteins1
  • IκBα inhibits the NF-κB by keeping them in a state isolated from the inactive cytoplasmic mask and the nuclear localization signal of NF-κB proteins. (researchsquare.com)
Dependent1
  • The Dbf4-dependent Cdc7 kinase (DDK) initiates replisome assembly by phosphorylating the MCM2-7 replicative helicase at the N-terminal tails of Mcm2, Mcm4 and Mcm6. (imperial.ac.uk)
Molecular3
AMPK1
  • Inhibits AMPK activation induced by AICAR (Cat. (tocris.com)
Therapeutic1
  • The identified potential therapeutic targets of HNK (PTTH) included CCND1 , SIRT2 , AURKB , VEGFA , HDAC1 , CASP9 , HSP90AA1 , and HSP90AB1 , which can potentially inhibit the cell cycle of mBCSCs. (hindawi.com)
Bioactive1
  • As a result, AP24534 also holds effectiveness against other imatinib resistant ABL mutants in bioactive small molecule library addition to ABL. (others-signal.com)
Overexpression4
  • Aurora A overexpression in many malignant tumor types suggests that it may be directly involved in NEOPLASTIC CELL TRANSFORMATION. (lookformedical.com)
  • In human, aurora-A has focused a lot of attention, since its overexpression has been found to be correlated with the grade of various solid tumours. (lookformedical.com)
  • Ectopic kinase overexpression in any culture cell line leads to polyploidy and centrosome amplification. (lookformedical.com)
  • However, overexpression of aurora-A in particular cell lines such as NIH3T3 is sufficient to induce growth on soft agar. (lookformedical.com)
Cdc21
  • The service of Aurora A by Cdc2 is PP1 independent, and, for that reason, TPX2 is impossible to participate in this particular function. (others-signal.com)
Progression1
  • The research team used a genetically engineered mouse model to define the role of aurora kinases in early progression of the disease. (bio-itworld.com)
Clinical1
  • Oss, April, 8th, 2016 - At the AACR 2016 conference, to be held in New Orleans next week, Jos de Man, Senior Investigator Chemistry at NTRC, will present on the unique binding mode of NTRC's TTK kinase inhibitor clinical candidate NTRC 0066-0. (oncolines.com)
Compound1
  • A crystal structure of Aurora kinase A in complex with an initial hit revealed a binding mode of the inhibitor within the ATP binding site and provided insight for structure-guided compound optimization. (rcsb.org)
Cancers1
Activator1
  • Taken together, our findings suggest that Bora is just a important activator of Aurora A that is functionally conserved between Drosophila and vertebrates. (others-signal.com)
Tumours1
  • Those transformed cells form tumours when implanted in immunodeficient mice, indicating that the kinase is an oncogene. (lookformedical.com)
Stem Cell1
  • Dorsomorphin dihydrochloride is also offered as part of the Tocriscreen 2.0 Max , Tocriscreen Kinase Inhibitor Library , Tocriscreen Epigenetics Library and Tocriscreen Stem Cell Library . (tocris.com)
Resistance2
  • In this study, we investigated the effect of AKI603, a novel small molecule inhibitor of Aurora kinase A (AurA) to overcome resistance mediated by BCR-ABL-T315I mutation. (scite.ai)
  • Taken together, our data demonstrate that the small molecule AurA inhibitor AKI603 may be used to overcome drug resistance induced by BCR-ABL-T315I mutation in CML. (scite.ai)
Centrosome1