AnatomyOrganismsChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPhenomena and ProcessesInformation Science
Protein Kinase InhibitorsProtein Kinase CProtein KinasesCyclic AMP-Dependent Protein KinasesStaurosporinePhosphorylationEnzyme InhibitorsProtein-Serine-Threonine Kinases1-(5-Isoquinolinesulfonyl)-2-MethylpiperazineMitogen-Activated Protein KinasesCalcium-Calmodulin-Dependent Protein KinasesEnzyme Activationp38 Mitogen-Activated Protein KinasesSignal TransductionIsoquinolinesPhosphatidylinositol 3-KinasesApoptosisMAP Kinase Signaling SystemAlkaloidsIndole AlkaloidsCells, CulturedProtein-Tyrosine KinasesMitogen-Activated Protein Kinase 1Mitogen-Activated Protein Kinase KinasesCell LineCarbazolesMitogen-Activated Protein Kinase 3Tetradecanoylphorbol AcetatePiperazinesCell Line, TumorIndolesProtein Kinase C-deltaCyclic AMPProtein Kinase C-alphaCyclic GMP-Dependent Protein KinasesJNK Mitogen-Activated Protein KinasesMolecular Sequence DataTumor Cells, CulturedPyridinesCaspasessrc-Family KinasesBlotting, WesternIsoenzymesIntracellular Signaling Peptides and ProteinsKineticsDose-Response Relationship, DrugCaspase 3TransfectionProto-Oncogene ProteinsPyrimidinesAmino Acid SequenceApoptosis Regulatory ProteinsAMP-Activated Protein KinasesCyclin-Dependent KinasesCalciumRNA, MessengerGenisteinFlavonoidsProto-Oncogene Proteins c-aktCell SurvivalAntineoplastic AgentsCell DivisionImidazolesCDC2 Protein KinaseCell CycleProtein Kinase C-epsilonProtein Kinase C betaCyclin-Dependent Kinase Inhibitor p21Carrier ProteinsCyclin-Dependent Kinase Inhibitor p27Casein Kinase IIMutationPhosphoproteinsProtein BindingProto-Oncogene Proteins c-bcl-2MaleimidesCell ProliferationExtracellular Signal-Regulated MAP KinasesChromonesSulfonamidesTime FactorsMorpholinesCalcium-Calmodulin-Dependent Protein Kinase Type 2AndrostadienesRecombinant ProteinsBenzamidesDown-RegulationMAP Kinase Kinase 1Base SequenceOkadaic AcidGene Expression RegulationInhibitor of Apoptosis ProteinsRats, Sprague-DawleyPhorbol 12,13-DibutyratePhorbol EstersSerineSubstrate Specificityrho-Associated KinasesMAP Kinase Kinase KinasesAdenosine Triphosphate
Mitogen-activaInhibitionInhibitsProliferationPhosphorylationInducesAutophagyGenesTyrosine kinaseSerineMAPKPathwaysPathwayInduce apoptosisExtracellular signalSelective inhibitorsReceptorSmall moleculeInductionActivation and apoptosisApoptoticDegradationCyclinAntitumorLeukemicAnticancerMRNAGenePI3K-AKTCellularCytoplasmicNecrosisAbstractProapoptoticCellsCell-permeableAutophagicSurvivalInhibitoryTranscriptionalPreventsSelectivityArrestActivityTumourHistoneCytotoxicitySTAT1Antibody
Mitogen-activa6
  • EPCs were cultured and treated with chemerin together with the specific p38 mitogen-activated protein kinase (MAPK) inhibitor SB 203580 in a time- and dose-dependent manner. (biomedcentral.com)
  • Resveratrol, a naturally occurring stilbene with antitumor properties, caused mitogen-activated protein kinase [MAPK, extracellular signal-regulated kinase 1/2 (ERK 1/2)] activation, nuclear translocation of Ser 15-phosphorylated p53, and p53-dependent apoptosis in hormone-insensitive DU145 prostate cancer cells. (tmu.edu.tw)
  • Our previous report showed that FO inhibits HCC cell invasion via AKT-, mitogen-activated protein kinase- (MAPK-), and EMT-related signals [ 7 ]. (hindawi.com)
  • NF-E2- related factor-2(Nrf-2), as well as mitogen-activated protein kinase (MAPK), is regulated by SFN. (nih.gov)
  • The anti-inflammatory effects of SHE treatment involved blocking of the mitogen-activated protein kinase and signal transducer and activator of transcription 1 signaling pathways. (researchgate.net)
  • Many cancers show aberrant signalling via the insulin-like growth factor (IGF) axis, activating type 1 IGF receptors (IGF-1Rs) and variant insulin receptors (INSRs) to signal via phosphatidylinositol 3-kinase-AKT-mammalian target of rapamycin (PI3K-AKT-mTOR) and mitogen-activated protein kinase kinase-extracellular signal-regulated kinases (MEK-ERK) [ 1 ]. (nature.com)
Inhibition20
  • Similar findings were made in bone marrow cells from gene-targeted mice lacking Bim and/or Puma infected with FLT3-ITD and treated with inhibitor, where loss of Puma only provided transient protection from apoptosis, but loss of Bim preserved clonal survival upon FLT3-ITD inhibition. (ashpublications.org)
  • Enzastaurin apparently inhibits tumor growth via multiple mechanisms: suppression of tumor cell proliferation, induction of tumor cell apoptosis and inhibition of tumor-induced angiogenesis. (lclabs.com)
  • NSP-B demonstrated significant growth inhibition and apoptotic induction, triggered by reduced AKT activation and downregulation of the inhibitors of apoptotic proteins and S-phase kinase protein. (bvsalud.org)
  • Exposure of these cells to epidermal growth factor (EGF) for up to 4 hours resulted in brief activation of MAPK followed by inhibition of resveratrol-induced signal transduction, p53 phosphorylation, and apoptosis. (tmu.edu.tw)
  • An inhibitor of protein kinase C (PKC)-α, -β, and -γ (CGP41251) enhanced Ser 15 phosphorylation of p53 by resveratrol in the absence of EGF and blocked EGF inhibition of the resveratrol effect. (tmu.edu.tw)
  • Inhibition of PKC activation in LNCaP cells, however, resulted in a reduction, rather than increase, in p53 activation and apoptosis, suggesting that resveratrol-induced apoptosis in these two cell lines occurs through different PKC-mediated and MAPK-dependent pathways. (tmu.edu.tw)
  • Moreover, AMPK inhibition in MLL-rearranged cell lines synergistically enhanced the antiproliferative effects of vincristine, daunorubicin, cytarabine, dexamethasone and L-asparaginase in most of the evaluated conditions. (usuhs.edu)
  • Sleeping Elegance is far more susceptible to more than expression inhibition than piggyBac and Tol2, the cargo capacity of Sleeping Attractiveness is constrained, and contrary to Tol2 and piggyBac that Inhibitors,Modulators,Libraries are lively in all mamma lian cell kinds tested, Sleeping Elegance display cell form dependent exercise. (p450inhibitors.com)
  • Activating mutations of RET, a driver oncogene in MTC that encodes a tyrosine kinase receptor, prevents apoptosis through inhibition of ATF4, a key transcriptional regulator of endoplasmic reticulum (ER) stress. (figshare.com)
  • Because of its ability to induce cell growth inhibition and apoptosis in normal and pre-malignant cells, TGFβ has been described as a potent tumor suppressor [ 8 ] [ 9 ] . (encyclopedia.pub)
  • Collectively our results set up Clinofibrate that inhibition of autophagy with CQ induces ubiquitinated protein build up and VOR potentiates CQ-mediated aggregate formation superoxide generation and apoptosis. (ampkpathway.com)
  • Inhibition of proteasomal activity with BZ or autophagy with CQ resulted in the build up of ubiquitinated proteins in colon Clinofibrate cancer cells as assessed by immunoblotting (Fig. 1B). (ampkpathway.com)
  • However inhibition of autophagy with CQ induced a much slower rate of protein accumulation as compared with proteasomal inhibition (Fig. 1C). (ampkpathway.com)
  • The end result is inhibition of DNA, ribonucleic acid (RNA), and protein synthesis. (medscape.com)
  • In addition to inducing apoptosis, caspase inhibition contributes to necroptosis and/or autophagy depending on the cell type and cellular context. (molcells.org)
  • We conclude that enhanced TRIF-RIP1-dependent autocrine action of IFNβ, rather than inhibition of ERK or Akt, is involved in TLRs/zVAD-induced autophagic and necroptotic cell death via the JAK/STAT1/ROS pathway. (molcells.org)
  • Activation of caspase-3, up-regulation of Bax, down-regulation of livin and Bcl-2, as well as inhibition of Jak-stat3 signaling pathway might be the important mechanisms for the bufalin-induced apoptosis. (biomedcentral.com)
  • Outcomes GyrB PKR, an inducible molecular procedure to block protein synthesis Previously, we found that the rapamycin, a spe cific inhibitor for mTOR, blocked NT three induced long term synapse modulation, Pharmacological inhibitors may well elicit unwanted effects together with its inhibition of pro tein synthesis, It's also unclear no matter whether rapamy cin acts pre or postsynaptically. (inhibitorkits.com)
  • Inhibition of DNA-dependent protein kinase catalytic subunit by small molecule inhibitor NU7026 sensitizes human leukemic K562 cells to benzene metabolite-induced apoptosis. (cdc.gov)
  • Mark L., Lee W. H., Villoutreix B. O., Proctor D., Blackbourn, D., Spiller B. O. and Blom A. M. (2004) KSHV complement control protein mimics human molecular mechanisms for inhibition of the complement system. (lu.se)
Inhibits10
  • A highly potent, cell-permeable, reversible, and selective inhibitor of Rho-associated protein kinase (Ki = 140 nM for p160 ROCK (ROCK-I). Also inhibits ROCK-II with almost equal potency. (sigmaaldrich.com)
  • Enzastaurin (LY317615), a protein kinase Cβ inhibitor, inhibits the AKT pathway and induces apoptosis in multiple myeloma cell lines. (lclabs.com)
  • Ideally, a drug that inhibits PKB should cause both cell cycle arrest and promote apoptosis. (justia.com)
  • Isoform 7 inhibits isoform 1-mediated apoptosis. (lsbio.com)
  • Glycyrrhizic acid is an inhibitor of lipoxygenase and cyclooxygenase, inhibits protein kinase C, and downregulates the epidermal growth factor receptor. (theinterstellarplan.com)
  • Results Chloroquine and bortezomib activate ubiquitin-conjugated protein accumulation in colon cancer cells CQ disrupts lysosomal function and inhibits the last step in the autophagic degradation process [20]. (ampkpathway.com)
  • Dabrafenib inhibits some mutated forms of BRAF kinases with in vitro IC50 values of 0.65, 0.5, and 1.84 nM for BRAF V600E, BRAF V600K, and BRAF V600D enzymes, respectively. (medscape.com)
  • Upcoming, we investigated irrespective of whether the dimerization and subsequent activation of PKR inhibits new protein synthesis. (inhibitorkits.com)
  • Trouw L., Nilsson S., Goncalvez I., Landberg G. and Blom A. M. (2005) C4b-binding protein binds to necrotic cells and DNA, which limits DNA release and inhibits complement activation. (lu.se)
  • In influenza viruses, the nonstructural protein 1 inhibits the interferon-mediated antiviral response. (cdc.gov)
Proliferation14
  • Autophagy also regulates cell proliferation, differentiation, survival, and apoptosis, highlighting its role in maintaining cellular homeostasis [ 1 ]. (hindawi.com)
  • Enzastaurin had a synergistic inhibitory effect with the EGFR inhibitor gefitinib on the proliferation of parental and gefitinib-resistant (GR) cancer cells. (lclabs.com)
  • Changes in migration, adhesion, proliferation and the apoptosis rate of EPCs were detected. (biomedcentral.com)
  • Overall, our findings demonstrated that NSP-B induces caspase-dependent apoptosis, increases cell damage, and suppresses MM cell proliferation while improving the cytotoxic impact of BTZ. (bvsalud.org)
  • Real-time cell analyzer and flow cytometry data reveal that tumor cell proliferation and apoptosis were impacted by FO. (hindawi.com)
  • DAVID bioinformatic data showed that most of the biological process GO terms are related to proliferation and apoptosis. (hindawi.com)
  • We hypothesized that FO might regulate related genes in apoptosis and PI3K-AKT pathways to mediate the proliferation and apoptosis of liver cancer cells. (hindawi.com)
  • PKB has emerged as a crucial regulator of widely divergent cellular processes including apoptosis, proliferation, differentiation and metabolism. (justia.com)
  • Protein transport between the nuclear and the cytoplasmic compartment is a key factor for cell viability and proliferation. (massgeneral.org)
  • The findings of increased proliferation and disorganized osteoblast Inhibitors,Modulators,Libraries growth had been evident in vertebrae with modest altera tions, which might recommend that this is often an early occasion within the fusion procedure. (pkc-inhibitors.com)
  • Ectopic expression of gene BCL2 enhances the survival and proliferation of chimpanzee and pig-tailed macaque iPSCs within the pre-implantation embryo, although the identity and long-term contribution of the transplanted cells warrants further investigation. (stanford.edu)
  • Transforming growth factor β (TGFβ) is a secreted growth and differentiation factor that influences vital cellular processes like proliferation, adhesion, motility, and apoptosis. (encyclopedia.pub)
  • IM combined with IR can synergistically inhibit the proliferation, apoptosis, clonogenesis, invasion, migration and cell cycle of GIST cells. (researchsquare.com)
  • Specify the components and their interactions and set up cluding proliferation, differentiation, apoptosis, embryonic the system of equations. (lu.se)
Phosphorylation9
  • Also acts as a potent inhibitor of agonist-induced Ca 2+ sensitization of myosin phosphorylation and smooth muscle contractions (IC 50 = 700 nM for phenylephrine-induced contractions in aortic strips). (sigmaaldrich.com)
  • Also acts as a potent inhibitor of agonist-induced Ca 2+ sensitization of myosin phosphorylation and smooth muscle contraction. (sigmaaldrich.com)
  • Phosphorylation at CDK1, CDK4, and CDK9 sites on, respectively, protein phosphatase 1alpha, retinoblastoma protein, and RNA polymerase II is inhibited in neuroblastoma SH-SY5Y cells exposed to meriolins. (rcsb.org)
  • However, we could not detect any phosphorylation of RIPK-1 and mixed lineage kinase domain like pseudokinase (MLKL), as well as any necrosome formation. (spandidos-publications.com)
  • Activation of PKC by phorbol ester (phorbol 12-myristate 13-acetate) enhanced EGF action on ERK 1/2 phosphorylation without significantly altering p53 phosphorylation by resveratrol. (tmu.edu.tw)
  • Our data demonstrate that RalA and RalB are phosphorylated by different kinases, and RalB phosphorylation is necessary for in vitro cellular functions and in vivo tumor growth and metastasis. (iahrgrenoble2016.org)
  • Protein extraction and purification kits, along with rabbit anti-rat peroxisome proliferator-activated receptor-gamma (anti-PPAR-γ), IκB kinase beta phosphorylation (anti-p-IKK-β), and inhibitor κB-alfa (IκB-α) antibodies were purchased from Wuhan Boster Biological Technology, Ltd., (Hubei, China). (frontiersin.org)
  • The protein is phosphorylated in a cell-cycle dependent manner, with late prophase phosphorylation remaining through metaphase. (cancerindex.org)
  • We herein demonstrated that CADM1 interacts with Hippo pathway core kinases and enhances the phosphorylation of YAP1, and also that the membranous co-expression of CADM1 and LATS2 predicts a favorable prognosis in lung adenocarcinoma. (cancerindex.org)
Induces9
  • The protein kinase Cβ-selective inhibitor, enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts. (lclabs.com)
  • Enzastaurin induces apoptosis in multiple myeloma (MM) cell lines by inhibiting signaling through the AKT pathway, which is caspase-independent. (lclabs.com)
  • Protein kinase C inhibitor enzastaurin induces in vitro and in vivo antitumor activity in Waldenström macroglobulinemia. (lclabs.com)
  • N- trans -Feruloyloctopamine (FO) is the extract of garlic skin, which possesses high antioxidant activity and selectively induces cell apoptosis in leukemia tumors [ 6 ]. (hindawi.com)
  • induces growth arrest or apoptosis depending on the physiological circumstances and cell type. (lsbio.com)
  • Purpose: Previous in vitro and in vivo studies have reported that 1'-S-1'-acetoxychavicol acetate (ACA) isolated from rhizomes of the Malaysian ethno-medicinal plant Alpinia conchigera Griff (Zingiberaceae) induces apoptosis-mediated cell death in tumour cells via dysregulation of the NF-κB pathway. (oncotarget.com)
  • Genome-wide analysis of ATF4 interaction sites by chromatin immunoprecipitation (ChIP) sequencing revealed that among ATF4 target genes was KLF9 (Kruppel-like factor 9), which induces MTC apoptosis. (figshare.com)
  • Active TGFβ induces the heteromeric complex formation of two single transmembrane serine/threonine kinase family receptors, i.e. (encyclopedia.pub)
  • Fig 1 CQ treatment induces ubiquitin-conjugated protein build up. (ampkpathway.com)
Autophagy16
  • Autophagy prevents NAFLD and AFLD progression through enhanced lipid catabolism and decreasing hepatic steatosis, which is characterized by the accumulation of triglycerides and increased inflammation. (hindawi.com)
  • Autophagy is a cellular catabolic process that eliminates damaged cell organelles, unfolded proteins, and various intracellular pathogens through lysosomal degradation. (hindawi.com)
  • In general, autophagy degrades long-lived damaged intracellular proteins, in contrast to the ubiquitin-proteasome system, which controls the degradation of short-lived proteins [ 2 ]. (hindawi.com)
  • Induction of canonical autophagy is mainly controlled by the AKT/mTOR and AMPK signaling pathways and relies on the activation and assembly of two macromolecular complexes, the ATG1/ULK1 and the Class III phosphatidylinositol 3-kinase (PI3K) complex (Figure 1 ) [ 5 ]. (hindawi.com)
  • The autophagophore membrane then elongates and encloses the molecules to be degraded forming an autophagosome, which occurs in two separate conjugation reactions catalyzed by autophagy-related proteins (ATGs). (hindawi.com)
  • Notably, this enhanced cytotoxicity is not mediated by the induction of apoptosis, but is accompanied by the pronounced induction of autophagy. (spandidos-publications.com)
  • IM-induced autophagy did not involve c-Abl or Bcl-2 activity but was associated with ER stress and was suppressed by depletion of intracellular Ca2+, suggesting it is mechanistically nonoverlapping with IM-induced apoptosis. (lu.se)
  • We further demonstrated that suppression of autophagy using either pharmacological inhibitors or RNA interference of essential autophagy genes enhanced cell death induced by IM in cell lines and primary CML cells. (lu.se)
  • IM, nilotinib, or dasatinib, with inhibitors of autophagy resulted in near complete elimination of phenotypically and functionally defined CML stem cells. (lu.se)
  • Together, these findings suggest that autophagy inhibitors may enhance the therapeutic effects of TKIs in the treatment of CML. (lu.se)
  • Disruption of autophagy with strongly enhanced VOR-mediated apoptosis in cancer of the colon cells CQ. (ampkpathway.com)
  • Appropriately knockdown of Clinofibrate the fundamental autophagy gene sensitized cells to VOR-induced apoptosis also. (ampkpathway.com)
  • We suggested that CQ treatment would result in an accumulation of proteins normally degraded by autophagy. (ampkpathway.com)
  • We showed that LPS/zVAD- and poly I:C/zVAD-induced cell death in bone marrow-derived macrophages (BMDMs) was inhibited by receptor-interacting protein kinase 1 (RIP1) inhibitor necrostatin-1 and autophagy inhibitor 3-methyladenine. (molcells.org)
  • RT can directly induce cancer cell death through various mechanisms, such as apoptosis, necrosis, and autophagy. (nature.com)
  • BNIP3 promotes autophagy in response to hypoxia, along with the WDR45L related protein, WIPI 49, co localizes with the autophagic marker LC3 following amino acid depletion in autophagosomes, It is not identified if BNIP3 or putative WDR45L related autophagy success in cell survival or death. (inhibitorkits.com)
Genes9
  • Moreover, NSP-B suppressed FOXM1-regulated genes, such as Aurora Kinases A and B, CDKs 4 and 6, and PLK1. (bvsalud.org)
  • One of the activated genes is an inhibitor of cyclin-dependent kinases. (lsbio.com)
  • Structural genes encode proteins that are not involved in gene regulation. (p450inhibitors.com)
  • At fused stage, early markers for osteoblasts and chondrocytes had been upregulated whereas the osteoblast inhibitor and genes concerned in chon drocyte hypertrophy have been downregulated, success also supported by ISH. (pkc-inhibitors.com)
  • Furthermore, we identified ATF4 target genes (LZTFL1, MKNK2, and SIAH1 with known tumor suppressor function) that were synergistically upregulated with the combination of TKI and ERAD inhibitor. (figshare.com)
  • 2004). Glucocorticoid-mediated GR activation is certainly associated with cancers cell level of resistance in preclinical versions EGT1442 by activating the appearance of genes whose proteins products considerably inhibit chemotherapy-induced apoptosis (Skor et al. (bioxorio.com)
  • Like Rb protein, many of the proteins encoded by tumor suppressor genes act at specific points in the cell cycle. (medscape.com)
  • TP53 activates the expression of genes involved in apoptosis, cell cycle regulation (p21), and MDM2. (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)
Tyrosine kinase8
  • Constitutively activating internal tandem duplications (ITD) of FLT3 (FMS-like tyrosine kinase 3) are the most common mutations in acute myeloid leukemia (AML) and correlate with poor prognosis. (ashpublications.org)
  • Receptor tyrosine kinase inhibitors targeting FLT3 have developed as attractive treatment options. (ashpublications.org)
  • FLT3 (FMS-like tyrosine kinase 3) is a type III receptor tyrosine kinase (RTK) closely related to the platelet-derived growth factor (PDGF) receptor and c-Kit with important functions in the regulation of early hematopoietic cells. (ashpublications.org)
  • Since epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitors, including gefitinib (GEF) have been reported to induce the apoptosis of several cancer cell lines, in the present study, we examined whether the cytotoxic effects of GEF are further enhanced under amino acid starvation (AAS) culture conditions. (spandidos-publications.com)
  • Paraptosis-like phenotype has also been described in human colorectal cancer cells following overactivation of the non-receptor tyrosine kinase c-Src suggesting potential involvement of Src-signalling in paraptosis. (wikipedia.org)
  • Imatinib mesylate (IM), a potent inhibitor of the BCR/ABL tyrosine kinase, has become standard first-line therapy for patients with chronic myeloid leukemia (CML), but the frequency of resistance increases in advancing stages of disease. (lu.se)
  • Critically, the combination of a tyrosine kinase inhibitor (TKI), i.e. (lu.se)
  • We hypothesized that the combination of a tyrosine kinase inhibitor (TKI) and an ATF4 inducer promotes cell death by triggering catastrophic oxidative stress and apoptotic cell death. (figshare.com)
Serine4
  • The presence of necrostatin-1, an inhibitor of receptor-interacting serine/threonine-protein kinase 1 (RIPK‑1), but not that of Z-VAD-fmk, attenuated the cytotoxic effects of GEF under AAS culture conditions. (spandidos-publications.com)
  • The serine/threonine kinase AMP-activated protein kinase (AMPK) and its downstream effectors, including endothelial nitric oxide synthase and BCL-2, are hyperactivated in B-cell precursor-acute lymphoblastic leukemia (BCP-ALL) cells with MLL gene rearrangements. (usuhs.edu)
  • Development through mitosis depends upon three major regulatory systems, each involving several serine/threonine kinases, referred to as mitotic kinases. (survivinpathway.com)
  • The protein encoded by this gene is a putative serine/threonine kinase that localizes to the mitotic apparatus and complexes with cell cycle controller CDC2 kinase in early mitosis. (cancerindex.org)
MAPK1
  • The data showed that chemerin enhanced the adhesion and migration abilities of EPCs, and reduced the apoptosis ratio and that this effect might be mediated through the p38 MAPK pathway. (biomedcentral.com)
Pathways7
  • As such, paraptosis can be prevented by inhibiting specific protein kinases of these pathways. (wikipedia.org)
  • Elimination of BCR/ABL-dependent intracellular signals triggers apoptosis, but it is unclear whether this activates additional cell survival and/or death pathways. (lu.se)
  • RESULTS: NSP-B induced apoptosis in CTCL cells by activating mitochondrial signaling pathways and caspases. (bvsalud.org)
  • Protein kinases are involved in signal transduction pathways linking growth factors, hormones and other cell regulation molecules to cell growth, survival and metabolism under both normal and pathological conditions. (justia.com)
  • What pathways are this gene/protein implicaed in? (cancerindex.org)
  • 2011). In vitro and in vivo tests claim that activation from the GR in ER-negative pre-malignant breasts epithelial and cancers cells initiates cell success pathways under usually apoptosis-inducing circumstances (e.g. chemotherapy, rays, and growth KIAA1516 aspect deprivation) (Wu et al. (bioxorio.com)
  • breasts cancers cells by preventing stress-mediated cell survival pathways that could in any other case counteract chemotherapy-induced apoptosis in tumor cells. (bioxorio.com)
Pathway6
  • Inactivation of the PI3-kinase pathway, but not of Ras-mitogen-activated protein (MAP) kinase signaling, was essential to elicit cytotoxic responses. (ashpublications.org)
  • Compound C-induced apoptosis was associated with mitochondrial membrane depolarization, reactive oxygen species production, cytochrome c release and caspases cleavage, indicating intrinsic apoptosis pathway activation. (usuhs.edu)
  • Taken together, these results indicate that the activation of the AMPK pathway directly contributes to the survival of MLL-rearranged BCP-ALL cells and AMPK inhibitors could represent a new therapeutic strategy for this high-risk leukemia. (usuhs.edu)
  • PI3K inhibitors block the PI3K/AKT/mTOR pathway and thus slow down cancer growth. (pi3k-inhibitors.com)
  • The purpose of the research is to investigate the roles of Jak-STAT3 signaling pathway in bufalin-induced apoptosis in colon cancer SW620 cells. (biomedcentral.com)
  • Western Blot was used to determine the protein expression of the apoptosis inhibitors livin and caspase-3, the apoptosis-related proteins Bax and Bcl-2, as well as the key protein kinases in the Jak-stat3 signaling pathway, stat3 and p-stat3. (biomedcentral.com)
Induce apoptosis2
  • Licorice polyphenols induce apoptosis in cancer cells. (theinterstellarplan.com)
  • The protein professional duct of NGFRAP1 interacts with p75, Collectively they process caspase 2 and caspase three to energetic kinds, and promote apoptosis in selelck kinase inhibitor 293T cells, NGFRAP1 requires p75 to induce apoptosis. (inhibitorkits.com)
Extracellular signal1
  • Trametinib is a reversible inhibitor of mitogen-activated extracellular signal regulated kinase 1 (MEK1) and MEK2 activation, and of MEK1 and MEK2 kinase activity. (medscape.com)
Selective inhibitors3
  • The present invention relates to cell permeable, stable conjugates comprising a cell-permeability enhancement moiety and a peptide or peptidomimetic, as selective inhibitors of protein kinases, to pharmaceutical compositions containing them, as well as to processes for the preparation and use of such complex molecules. (justia.com)
  • Novel selective inhibitors of nuclear export (SINE) have achieved outstanding preclinical results and are currently in Phase I trials. (massgeneral.org)
  • Put forward the invention of selective inhibitors against various isoenzymes is beneficial to reduce the burden of inclusive deleterious effects of drug for normal physiological process. (pi3k-inhibitors.com)
Receptor6
  • Chemerin is an adipocytokine involved in the recruitment of immune cells [ 11 ] and serves as a bridge between various immune cells from the initial stage of inflammatory diseases through the development process [ 12 ], and its receptor CMKLR1 (also named ChemR23 in humans) is a specific functional member of the G protein receptor family. (biomedcentral.com)
  • Since PKB activation is PI′-3-kinase dependent, the persistent activation of certain protein tyrosine kinases, such as IGF−1 receptor, EGF receptor, PDGF receptor, pp60c-Src, and the like, leads to the persistent activation of PKB which is indeed encountered in many tumors. (justia.com)
  • At 24 h post-operatively, we assessed the serum levels of creatinine and urea nitrogen, expression levels of peroxisome proliferator-activated receptor gamma (PPAR-γ) and NF-κB-related (p-IKK-β and IκB-α) proteins, and mRNA expression levels of the inflammatory cytokines, including TNF-α and MCP-1, in the renal tissue of various study groups. (frontiersin.org)
  • In macrophages, necroptosis can be induced by co-treatment with Toll-like receptor (TLR) ligands (lipopolysaccharide [LPS] for TLR4 and polyinosinic-polycytidylic acid [poly I:C] for TLR3) and a cell-permeable pan-caspase inhibitor zVAD. (molcells.org)
  • Our data further support the involvement of autocrine IFNs action in reactive oxygen species (ROS)-dependent necroptosis, LPS/zVAD-elicited ROS production was inhibited by necrostatin-1, neutralizing antibody of IFN receptor (IFNR) and JAK inhibitor AZD1480. (molcells.org)
  • All IFNαs and IFNβ bind to the same receptor and as a result, the cytoplasmic kinases JAK1 and TYK2 become activated and phosphorylate the STAT1 and STAT2 molecules. (cdc.gov)
Small molecule2
  • Here, we have determined the growth-inhibitory and proapototic mechanisms of 2 small molecule inhibitors of FLT3, AG1295 or PKC412, in hematopoietic progenitor cells, human leukemic cell lines, and primary AML cells expressing FLT3-ITD. (ashpublications.org)
  • These observations have prompted the development of small-molecule Bcl-2 inhibitors (refs. (aacrjournals.org)
Induction5
  • The stilbene promoted p53-dependent apoptosis, whereas EGF opposed induction of apoptosis by resveratrol via a PKC-α-mediated mechanism. (tmu.edu.tw)
  • Apoptosis induction seems to be mediated either by stimulation of BAX and FAS antigen expression, or by repression of Bcl-2 expression. (lsbio.com)
  • Collectively, these findings suggest down-regulation of Mcl-1 by either CDK inhibitors or genetic approaches dramatically potentiate ABT-737 lethality through cooperative interactions at two distinct levels: unleashing of Bak from both Bcl-xL and Mcl-1 and simultaneous induction of Bak activation and Bax translocation. (aacrjournals.org)
  • HA14-1) that disable Bcl-2, resulting in induction of apoptosis in leukemia cell lines ( 8 ). (aacrjournals.org)
  • Combinatorial effect of QUE and resveratrol has been found to be antiproliferative via suppression of oncogenic microRNA-27a and induction of zinc finger protein ZBTB10 against HT-29 colon cancer (Del Follo-Martinez et al. (pi3k-inhibitors.com)
Activation and apoptosis1
  • Ectopic Mcl-1 expression attenuates Bak activation and apoptosis by ABT-737 + roscovitine, whereas cells overexpressing Bcl-2 or Bcl-xL remain fully sensitive. (aacrjournals.org)
Apoptotic2
  • Paraptosis does not demonstrate nuclear fragmentation, formation of apoptotic bodies, or definitive demonstration of chromatin condensation - all seen in apoptosis. (wikipedia.org)
  • PKB is an anti-apoptotic protein kinase whose activity is strongly elevated in human malignancies. (justia.com)
Degradation4
  • After the degradation of damaged proteins and lipids, amino acids and fatty acids are released into the cytoplasm and recycled for new biosynthesis of cellular components or energy production [ 4 ]. (hindawi.com)
  • In contrast to the influx of amino acids, the degradation of proteins is also the important intracellular mechanism for releasing free amino acids both under steady-state conditions and during cellular stresses. (spandidos-publications.com)
  • Here, we report that the ER-associated protein degradation (ERAD) inhibitor eeyarestatin sensitized MTC cells to the TKIs, sunitinib and vandetanib, thereby leading to synergistic upregulation of ATF4 expression, accumulation of reactive oxygen species, and subsequent cell death. (figshare.com)
  • which facilitates the proteasomal degradation of FBXL20 by another F-box protein, FBXO31. (iahrgrenoble2016.org)
Cyclin9
  • We describe here the meriolins, a new family of inhibitors of cyclin-dependent kinases (CDK). (rcsb.org)
  • The structures of pCDK2/cyclin A/variolin B and pCDK2/cyclin A/meriolin 3 complexes reveal that the two inhibitors bind within the ATP binding site of the kinase, but in different orientations. (rcsb.org)
  • We observed downregulated expression of BUB1B, Aurora Kinases A and B, cyclin-dependent kinases (CDKs) 4 and 6, and polo-like kinase 1 (PLK1) in NSP-B treated cells, which was further corroborated by Western blot analysis. (bvsalud.org)
  • Mechanistically, benzofuran derivatives enhanced the cyclin-dependent kinase inhibitor p21Cip/WAF1 expression at both mRNA and protein levels and this occurs transcriptionally in an Sp1-dependent manner. (unical.it)
  • Right chromosome segregation is closely controlled by mitotic kinases such as cyclin dependent NIMA related kinase 2, Pololike kinase, kinase 1 and Aurora kinases. (survivinpathway.com)
  • Here, we show that Mcl-1 down-regulation by the cyclin-dependent kinase (CDK) inhibitor roscovitine or Mcl-1-shRNA dramatically increases ABT-737 lethality in human leukemia cells. (aacrjournals.org)
  • The N-terminal region of the protein binds CDC2 to form a complex showing reduced H1 histone kinase activity, indicating a role as a negative regulator of CDC2/cyclin A. In addition, the C-terminal kinase domain binds to its own N-terminal region, suggesting potential negative regulation through interference with complex formation via intramolecular binding. (cancerindex.org)
  • The cyclin-dependent kinase (CDK) inhibitors p21 and p16 inhibit the activity of CDKs, such as CDK4. (medscape.com)
  • The p16INK4A protein is a cell-cycle inhibitor that acts by inhibiting activated cyclin D:CDK4/6 complexes, which play a crucial role in the control of the cell cycle by phosphorylating Rb protein. (medscape.com)
Antitumor2
  • Regorafenib is an inhibitor of multiple protein kinases which exerts antitumor and antimetastatic activities in metastatic colorectal cancer (CRC). (oncotarget.com)
  • Proliferative Effects - In a screen for naturally occurring angiogenic inhibitors, we have identified an extract from the roots of Glycyrrhiza glabra, which has potent antiangiogenic and antitumor activity. (theinterstellarplan.com)
Leukemic1
  • Exposure of leukemic cells to the commercial AMPK inhibitor compound C resulted in massive apoptosis only in cells with MLL gene rearrangements. (usuhs.edu)
Anticancer4
  • Protein kinases represent promising anticancer drug targets. (rcsb.org)
  • These findings are discussed in relation to the anticancer properties of SK1 inhibitors. (strath.ac.uk)
  • Therefore, we hypothesized the improved anticancer efficacy of QUE in combination with isoenzyme inhibitors-rottlerin (ROT-PKCδ inhibitor), G0 6983 (PKCα inhibitor), and PI-103 (p110α-class I PI3K inhibitor) in MCF-7 and RAW 264.7 cells. (pi3k-inhibitors.com)
  • Clinically it is mainly used for high levels of estrogen in breast cancer patients, which combines with androgen and other anticancer drugs (such as doxorubicin, etc., enhancing the effectiveness and showing good effect in postmenopausal patients with advanced breast cancer. (lookchem.com)
MRNA2
  • Within the same prostate cancer cell line model, a whole new HDAC inhibitor, H6CAHA, sup pressed the expression of BRCA1 mRNA, and when used in Inhibitors,Modulators,Libraries mixture with g radiation, prevented the development of tumor xenografts. (pkc-inhibitors.com)
  • In contrast to earlier reviews through which MDK gene and protein expression was established to become higher in late stage cancer, we observed a drop in the ranges of MDK mRNA in CRPC versus RAD. (inhibitorkits.com)
Gene6
  • Like apoptosis and other types of programmed cell death, the cell is involved in causing its own death, and gene expression is required. (wikipedia.org)
  • This gene encodes a member of the aldo/keto reductase superfamily, which consists of more than 40 known enzymes and proteins. (cancerindex.org)
  • What does this gene/protein do? (cancerindex.org)
  • [ 1 ] His prediction was subsequently supported by the cloning of the retinoblastoma tumor suppressor gene ( RB1 ) and by functional studies of the retinoblastoma protein, Rb. (medscape.com)
  • For example, the TP53 gene, located on chromosome 17, encodes a 53-kd nuclear protein that functions as a cell cycle checkpoint. (medscape.com)
  • The TP53 gene is also capable of stimulating apoptosis of cells containing damaged DNA. (medscape.com)
PI3K-AKT1
  • KEGG enrichment analysis showed that FO mainly regulates PI3K-AKT- and apoptosis-related signals, in which BBC3, DDIT3, NOXA, and CDKN1A on the surface serve as the novel targets of FO inducing HCC cell apoptosis. (hindawi.com)
Cellular5
  • Cellular proteins and organelles are engulfed into a double-membrane vesicle to form an autophagosome. (spandidos-publications.com)
  • The sensitizing properties of HDAC inhibitors to DNA damaging agents has been linked to aberrant dou ble strand break repair and cellular pressure signaling. (pkc-inhibitors.com)
  • Kask L., Hillarp A., Ramesh B., Dahlbäck B., and Blom A. M. (2002) Structural requirements for the intra-cellular subunit polymerization of the complement inhibitor C4b-binding protein. (lu.se)
  • Binding to dsRNA by these proteins may result in initiation of helicase activity, concomitant with a conformational change that leads to recruiting additional cellular factors, including the recently identified IPS-1/MAVS protein ( 5 , 6 ). (cdc.gov)
  • As a result, different cellular kinases, including the IRF3 kinases TBK1 and IKKε, become activated. (cdc.gov)
Cytoplasmic1
  • Similar to apoptosis, staining techniques can be used to identify paraptotic cells by highlighting the translocation of phosphatidylserine from the plasma membrane cytoplasmic (inner) leaflet to the cell surface or outer leaflet. (wikipedia.org)
Necrosis1
  • Paraptosis (from the Greek παρά para, "related to" and apoptosis) is a type of programmed cell death, morphologically distinct from apoptosis and necrosis. (wikipedia.org)
Abstract1
  • abstract = "Sphingosine kinase 1 (SK1) catalyzes the conversion of sphingosine to the bioactive lipid sphingosine 1-phosphate. (strath.ac.uk)
Proapoptotic3
Cells22
  • Prevents apoptosis and enhances the survival and cloning efficiency of dissociated hES cells without affecting their pluripotency. (sigmaaldrich.com)
  • Several inhibitors have been described, such as AG1295, CEP701, PKC412, and SU-11 248, with cytotoxic effects to cell lines and primary AML cells in vitro expressing mutant FLT3. (ashpublications.org)
  • While certain templates of programmed cell death have been known to rely on de novo protein synthesis, paraptotic cell death induced by IGFIR-IC in 293T cells is deterred by actinomycin D and cycloheximide, thus demonstrating a dependence on transcription and translation. (wikipedia.org)
  • Additionally, research found that caspase inhibitors (zVAD.fmk, p53, BAF), x-chromosome-linked inhibitor (xiap), and Bcl-xL( from the Bcl-2 family) did not prevent cell death in 293T cells when induced by IGFIR-IC. (wikipedia.org)
  • Enzastaurin enhances the antiangiogenic effects of radiation by radiosensitizing human endothelial cells in pancreatic cancer xenografts. (lclabs.com)
  • Enzastaurin, an inhibitor of PKCβ, enhances antiangiogenic effects and cytotoxicity of radiation against endothelial cells. (lclabs.com)
  • FOXM1 and BUB1B expression exhibited a dose-dependent reduction in NSP-B-treated CTCL cells.FOXM1 silencing decreased cell viability and increased apoptosis via BUB1B downregulation. (bvsalud.org)
  • Recent studies show that synthetic and dietary epigenetic inhibitors attenuate the abnormal epigenetic modifications in cancer cells and therefore have strong potential for cancer treatment. (bvsalud.org)
  • The present invention provides inhibitors of protein kinases comprising a molecule having at least a first moiety competent for penetration of the molecule into cells, and a second moiety for having a protein kinase inhibiting effect within the cells. (justia.com)
  • Also, PKB is overexpressed in 15% of ovarian cancers, 12% of pancreatic cancers and 3% of breast cancers, and was shown to produce a survival signal that protects cells from apoptosis thus contributing to resistance to chemotherapy. (justia.com)
  • This suggested that overexpression of Nrf-2 resulted in enhanced resistance of cancer cells to chemotherapeutic agents. (nih.gov)
  • We transfected cells with Rap1 targeting or scrambled siRNA and then done protein Retroperitoneal lymph node dissection transfection of the GST fused constitutively active type of Rac1. (survivinpathway.com)
  • Comparisons with the SK1 inhibitor, SKi or siRNA knockdown of SK1 indicated that (S)-FTY720 vinylphosphonate and FTY720 behave as typical SK1 inhibitors in preventing sphingosine 1-phosphate-stimulated rearrangement of actin in MCF-7 cells. (strath.ac.uk)
  • ChIP assays revealed that ATF4 occupancy at the KLF9 promoter was increased in MTC cells treated with eeyarestatin or vandetanib alone and was further enhanced in cells treated with both drugs, leading to increased KLF9 transcription. (figshare.com)
  • RNAi-mediated ablation of FBXL20 results in increased levels of PUMA as well as BAX, which further enhances the sensitivity of cancer cells to chemotherapeutic drugs. (iahrgrenoble2016.org)
  • We showed that high level expression of FBXL20 in cancer cells reduces therapeutic drug-induced apoptosis and promotes chemoresistance. (iahrgrenoble2016.org)
  • In addition, UMUC3 cells transfected having a constitutively active RalB(G23V) exhibited enhanced subcutaneous tumor growth, while those transfected with phospho-deficient RalB(G23V-S198A) were indistinguishable from control cells. (iahrgrenoble2016.org)
  • Knockdown of HDAC6 significantly improved BZ-induced apoptosis but only marginally sensitized cells to CQ. (ampkpathway.com)
  • To determine whether proteins aggregation correlated with the power of these realtors to stimulate apoptosis HCT8 and HT29 cells had been treated with BZ or the autophagic inhibitors (CQ and 3-MA) for 24 hrs with or without VOR. (ampkpathway.com)
  • This increment in cell deaths are positively correlated with enhanced morphological alteration observed in MCF-7 cells. (pi3k-inhibitors.com)
  • Bufalin not only inhibited the growth of colon cancer SW620 cells, but also induced apoptosis of SW620 cells. (biomedcentral.com)
  • Pertoft H. and Fries E. (1995) Inter-a-inhibitor is required for the formation of the hyaluronan-containing coat on fibroblasts and mesothelial cells. (lu.se)
Cell-permeable2
  • Y-27632A, CAS 331752-47-7, is a cell-permeable, reversible, inhibitor of Rho kinases (K i = 140 nM for p160ROCK). (sigmaaldrich.com)
  • A highly potent, cell-permeable, reversible, and selective inhibitor of Rho-associated protein kinases (K i = 140 nM for p160 ROCK ). (sigmaaldrich.com)
Autophagic1
  • Several studies have identified various forms of cell death, such as apoptosis, necroptosis, autophagic cell death, and pyroptosis. (molcells.org)
Survival1
  • Enhances survival & cloning efficiency of ESC without affecting their pluripotency. (sigmaaldrich.com)
Inhibitory2
  • The inhibitory effect of HT7 on cocaine‐enhanced locomotion was blocked by optogenetic silencing of the mPFC‐LHb circuit. (researchgate.net)
  • Sjöberg A., Trouw L., McGrath F., Hack E. C. and Blom A. M. (2006) Regulation of complement activation by C-reactive protein: targeting of the inhibitory activity of C4b-binding protein. (lu.se)
Transcriptional2
  • However, only silencing of Bim, or its direct transcriptional activator FOXO3a, abrogated apoptosis efficiently. (ashpublications.org)
  • LincRNA-p21 participates in TP53-dependent transcriptional repression leading to apoptosis and seem to have to effect on cell-cycle regulation. (lsbio.com)
Prevents1
  • Prevents CDK7 kinase activity when associated to CAK complex in response to DNA damage, thus stopping cell cycle progression. (lsbio.com)
Selectivity2
  • A selectivity study done on 32 kinases showed that, compared with variolin B, meriolins display enhanced specificity toward CDKs, with marked potency on CDK2 and CDK9. (rcsb.org)
  • The complex molecules are preferably peptide conjugates having improved cell-permeability, serum stability and kinase selectivity compared to known protein kinase inhibitors. (justia.com)
Arrest2
Activity8
  • Does not affect the activity of p21-activated protein kinase (PAK) even at high concentrations (~100 µM). (sigmaaldrich.com)
  • We describe how these are activated, which are their target proteins, and how their proteolytic activity modulates platelet functions. (frontiersin.org)
  • Pharmaceutical compositions that include these protein kinase inhibitors, and methods of using such compositions for treatment of cancers and other diseases associated with protein kinase activity are also disclosed. (justia.com)
  • Isoform 2 enhances the transactivation activity of isoform 1 from some but not all TP53-inducible promoters. (lsbio.com)
  • A model is proposed in which (S)-FTY720 vinylphosphonate binding to and stabilization of the allosteric site might enhance the autoinhibitory effect on SK1 activity. (strath.ac.uk)
  • However, little is known about the mechanism regarding regorafenib affects SHP-1 tyrosine phosphatase activity and leads to apoptosis and tumor suppression in CRC. (oncotarget.com)
  • In addition, chronic diagnostic test for follow-up of patients cy and for biochemical determination inflammation associated with the infec- with H. pylori gastritis and were able of tissue COX-2 activity using COX tion leads to damage in proteins, the to predict the risk of development of Activity Assay Kit (Cayman Chemical production of reactive oxygen species stomach cancer. (who.int)
  • Preclinical and clinical activity of DZD1516, a full blood-brain barrier-penetrant, highly selective HER2 inhibitor. (medscape.com)
Tumour1
  • Finally treatment with the CQ/VOR combination significantly reduced tumour burden and induced apoptosis inside a colon cancer xenograft model. (ampkpathway.com)
Histone2
  • The effects of DNA methylation and the histone code are due, at least in part, to modification-specific recruitment of factors, such as heterochromatin-associated proteins (HP1) and methyl-binding domain proteins, which establish and maintain higher order of chromatin structure. (aacrjournals.org)
  • The histone deacetylase (HDAC) inhibitor vorinostat (VOR) obstructed BZ-induced aggresome formation but marketed CQ-mediated ubiquitinated proteins accumulation. (ampkpathway.com)
Cytotoxicity2
  • The knockdown of L-type amino acid transporter 1 (LAT-1) by siRNA also enhanced GEF-induced cytotoxicity. (spandidos-publications.com)
  • Interestingly, NSP-B also enhanced the cytotoxicity of bortezomib (BTZ), an existing MM treatment. (bvsalud.org)
STAT12
  • Although zVAD did not affect LPS- or poly I:C-induced activation of IKK, JNK, and p38, it enhanced IRF3 and STAT1 activation as well as type I interferon (IFN) expression. (molcells.org)
  • RHAMM regulates MMTV-PyMT-induced lung metastasis by connecting STING-dependent DNA damage sensing to interferon/STAT1 pro-apoptosis signaling. (medscape.com)
Antibody1
  • Anticytotoxic T-lymphocyte-associated protein 4 (CTLA-4) is a humanized antibody that overcomes CTLA-4-mediated T-cell suppression to enhance the immune response against tumors. (medscape.com)