Search results for "ErbB Receptor"

showing 7 items of 167 documents

Cytotoxicity of the Urokinase-Plasminogen Activator Inhibitor Carbamimidothioic Acid (4-Boronophenyl) Methyl Ester Hydrobromide (BC-11) on Triple-Neg…

2015

BC-11 is an easily synthesized simple thiouronium-substituted phenylboronic acid, which has been shown to be cytotoxic on triple negative MDA-MB231 breast cancer cells by inducing a perturbation of cell cycle when administered at a concentration equal to its ED50 at 72 h (117 μM). Exposure of cells to BC-11, either pre-absorbed with a soluble preparation of the N-terminal fragment of urokinase-plasminogen activator (uPa), or in co-treatment with two different EGFR inhibitors, indicated that: (i) BC-11 acts via binding to the N-terminus of the enzyme where uPa- and EGF receptor-recognizing sites are present, thereby abrogating the growth-sustaining effect resulting from receptor binding

boronic acidPharmaceutical ScienceGene ExpressionApoptosisAnalytical ChemistryDrug DiscoveryCytotoxic T cellSettore BIO/06 - Anatomia Comparata E CitologiaCytotoxicityEGFR inhibitorschemistry.chemical_classificationCell CycleDrug SynergismCell cycleBoronic AcidsMitochondriaErbB ReceptorsBiochemistryChemistry (miscellaneous)Molecular MedicinecytotoxicityFemaleQD0241Antineoplastic AgentsArticlelcsh:QD241-441plasminogen activator inhibitorbreast cancerlcsh:Organic chemistryCell Line TumorHumansPhysical and Theoretical ChemistryMammary Glands HumanCell ProliferationQD0415Reactive oxygen speciesHydrobromideOrganic ChemistryEpithelial CellsBC-11Molecular biologyUrokinase-Type Plasminogen ActivatorPlasminogen InactivatorsEnzymechemistryApoptosisQuinazolinesMDA-MB231 cellsReactive Oxygen Speciesboronic acid; BC-11; plasminogen activator inhibitor; breast cancer; cytotoxicity; MDA-MB231 cellsMolecules
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The Status of EGFR Modulates the Effect of miRNA-200c on ZEB1 Expression and Cell Migration in Glioblastoma Cells

2020

Migration of glioblastoma cells into surrounding tissue is one of the main features that makes this tumor incurable. We evaluated whole-genome miRNA expression profiling associated with different EGFR amplification patterns in 30 cases of primary glioblastoma. From the 64 miRNAs that showed differential expression between tumors with a high level of EGFR amplification and tumors without EGFR amplification, 40% were related with cell migration, being miR-200c the most differentially expressed between these two groups. We investigated the effect of miR-200c on ZEB1 expression and cell migration in an in vitro transfection model with a miR-200c mimic, a miR-200c inhibitor and siRNA targeting E…

cell migrationEGFR AmplificationApoptosisBiologyArticleCatalysismiR-200clcsh:ChemistryInorganic ChemistryDownregulation and upregulationCell MovementmicroRNABiomarkers TumorTumor Cells CulturedmedicineZEB1HumansGene silencingEGFR amplificationPhysical and Theoretical Chemistrylcsh:QH301-705.5Molecular BiologySpectroscopyCell ProliferationOrganic ChemistryglioblastomaGene AmplificationZinc Finger E-box-Binding Homeobox 1Cell migrationGeneral MedicineTransfectionPrognosismedicine.diseaseComputer Science ApplicationsErbB ReceptorsGene Expression Regulation NeoplasticMicroRNAslcsh:Biology (General)lcsh:QD1-999Cell cultureMutationCancer researchGlioblastomaInternational Journal of Molecular Sciences
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Design, Synthesis and Biological Evaluation of Novel Pyrazolo[1,2,4]triazolopyrimidine Derivatives as Potential Anticancer Agents

2021

Three novel pyrazolo-[4,3-e][1,2,4]triazolopyrimidine derivatives (1, 2, and 3) were designed, synthesized, and evaluated for their in vitro biological activity. All three compounds exhibited different levels of cytotoxicity against cervical and breast cancer cell lines. However, compound 1 showed the best antiproliferative activity against all tested tumor cell lines, including HCC1937 and HeLa cells, which express high levels of wild-type epidermal growth factor receptor (EGFR). Western blot analyses demonstrated that compound 1 inhibited the activation of EGFR, protein kinase B (Akt), and extracellular signal-regulated kinase (Erk)1/2 in breast and cervical cancer cells at concentrations…

cervical cancercrystal X-ray analysisPharmaceutical ScienceAntineoplastic AgentsArticleAnalytical ChemistryHeLa03 medical and health sciencesbreast cancerQD241-4410302 clinical medicineDrug DiscoveryHumansEpidermal growth factor receptorPhysical and Theoretical Chemistrypyrazolo[124]triazolopyrimidineCytotoxicityProtein Kinase InhibitorsProtein kinase BCell Proliferation030304 developmental biologyMitogen-Activated Protein Kinase 1pyrazolo[124]triazolopyrimidine; EGF-receptor inhibitor; breast cancer; cervical cancer; molecular docking; crystal X-ray analysis0303 health sciencesBinding SitesMitogen-Activated Protein Kinase 3biologyChemistryKinaseOrganic ChemistryBiological activitymolecular dockingTriazolesbiology.organism_classificationMolecular biologyIn vitroErbB ReceptorsMolecular Docking SimulationPyrimidinesChemistry (miscellaneous)Docking (molecular)030220 oncology & carcinogenesisbiology.proteinMolecular MedicineProto-Oncogene Proteins c-aktEGF-receptor inhibitorHeLa CellsProtein BindingMolecules
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MiR-33a Controls hMSCS Osteoblast Commitment Modulating the Yap/Taz Expression Through EGFR Signaling Regulation

2019

Mesenchymal stromal cells (hMSCs) display a pleiotropic function in bone regeneration. The signaling involved in osteoblast commitment is still not completely understood, and that determines the failure of current therapies being used. In our recent studies, we identified two miRNAs as regulators of hMSCs osteoblast differentiation driving hypoxia signaling and cytoskeletal reorganization. Other signalings involved in this process are epithelial to mesenchymal transition (EMT) and epidermal growth factor receptor (EGFR) signalings through the regulation of Yes-associated protein (YAP)/PDZ-binding motif (TAZ) expression. In the current study, we investigated the role of miR-33a family as a (…

epithelial mesenchymal transitionregenerative medicinePDZ DomainsCell CommunicationArticlemicroRNAmedicineHumansEpidermal growth factor receptorEpithelial–mesenchymal transitionBone regenerationCells CulturedEGFR inhibitorsAdaptor Proteins Signal TransducingOsteoblastsmicroRNAbiologyMesenchymal stem cellComputational BiologyOsteoblastMesenchymal Stem CellsYAP-Signaling ProteinsGeneral MedicinePhenotypeCell biologymicroRNAsErbB Receptorsmedicine.anatomical_structureTranscriptional Coactivator with PDZ-Binding Motif Proteinsmesenchymal stromal cellbiology.proteinTrans-Activatorsmesenchymal stromal cellsEGFR signalingSignal TransductionTranscription FactorsCells
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Amphiregulin activates human hepatic stellate cells and is upregulated in non alcoholic steatohepatitis

2015

AbstractAmphiregulin (AR) involvement in liver fibrogenesis and hepatic stellate cells (HSC) regulation is under study. Non-alcoholic fatty liver disease (NAFLD) and its more severe form non-alcoholic steatohepatitis (NASH) may progress to cirrhosis and hepatocellular cancer (HCC). Our aim was to investigate ex vivo the effect of AR on human primary HSC (hHSC) and verify in vivo the relevance of AR in NAFLD fibrogenesis. hHSC isolated from healthy liver segments were analyzed for expression of AR and its activator, TNF-α converting enzyme (TACE). AR induction of hHSC proliferation and matrix production was estimated in the presence of antagonists. AR involvement in fibrogenesis was also ass…

medicine.medical_specialtyBiopsyGene ExpressionADAM17 ProteinBiologyAmphiregulinSeverity of Illness Indexp38 Mitogen-Activated Protein Kinasesdigestive systemArticleMicePhosphatidylinositol 3-Kinases03 medical and health sciences0302 clinical medicineDownregulation and upregulationAmphiregulinGrowth factor receptorNon-alcoholic Fatty Liver DiseaseInternal medicineHepatic Stellate CellsmedicineAnimalsHumansProtein Kinase CPI3K/AKT/mTOR pathwayCell Proliferation030304 developmental biology0303 health sciencesMultidisciplinaryFatty livernutritional and metabolic diseasesmedicine.diseaseFibrosisActinsdigestive system diseases3. Good healthEnzyme ActivationErbB ReceptorsADAM ProteinsDisease Models AnimalEndocrinologyHepatic stellate cellCancer research030211 gastroenterology & hepatologyTumor necrosis factor alphaCollagenSteatohepatitisSignal TransductionScientific Reports
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Expression of differentiation antigens and growth-related genes in normal kidney, autosomal dominant polycystic kidney disease, and renal cell carcin…

1992

Cellular differentiation and mRNA levels of genes involved in kidney growth were investigated in normal kidney cells, cyst-lining epithelial cells of polycystic kidney disease, and renal carcinoma cells (RCC). All cells comparatively studied exhibited an antigenic phenotype of proximal tubular cells as shown by the expression of a panel of brush border membrane enzymes and kidney-associated cell surface antigens. The epithelial developmental antigen Exo-1 was expressed in 50% to 80% of cyst-lining epithelia in polycystic kidney tissue and in 20% to 30% of polycystic kidney cells cultured in vitro. Normal kidney cells and RCC were negative under identical culture conditions. The expression o…

medicine.medical_specialtyTGF alphaCellular differentiationAutosomal dominant polycystic kidney diseaseGene ExpressionBiologyKidneyEpitheliumProto-Oncogene Proteins c-mycGrowth factor receptorEpidermal growth factorInternal medicinemedicinePolycystic kidney diseaseHumansRNA MessengerGrowth SubstancesCarcinoma Renal CellCells CulturedKidneyurogenital systemAntibodies MonoclonalTransforming Growth Factor alphamedicine.diseasePolycystic Kidney Autosomal DominantAntigens DifferentiationImmunohistochemistryKidney NeoplasmsErbB ReceptorsEndocrinologymedicine.anatomical_structureGenesNephrologyAntigens SurfaceCancer researchTransforming growth factorAmerican journal of kidney diseases : the official journal of the National Kidney Foundation
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Mtlinteracts with members of Egfr signaling and cell adhesion genes in the Drosophila eye

2011

Mtl is a member of the Rho family of small GTPases in Drosophila. It was shown that Mtl is involved in planar cell polarity (PCP) establishment, together with other members of the same family like Cdc42, Rac1, Rac2 and RhoA. However, while Rac1, Rac2 and RhoA function downstream of Dsh in Fz/PCP signaling and upstream of a JNK cassette, Mtl and Cdc42 do not. To determine the functional context of Mtl during PCP establishment in the Drosophila eye, we performed a loss-of-function screen to search for dominant modifiers of a sev>Mtl rough eye phenotype. In addition, genetic interaction assays with candidate genes were also carried out. Our results show that Mtl interacts genetically with memb…

rho GTP-Binding ProteinsGeneticsOmmatidial rotationRHOAbiologyCytoskeleton organizationCell PolarityCDC42Cell biologyErbB ReceptorsPhenotypeInsect ScienceCell polarityCell Adhesionbiology.proteinAnimalsDrosophila ProteinsImmunoglobulin superfamilyDrosophilaCompound Eye ArthropodReceptors Invertebrate PeptideCell adhesionpsychological phenomena and processesDrosophila ProteinSignal TransductionFly
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