Search results for "Phosphorylation"

showing 10 items of 975 documents

miR‐200c and phospho‐AKT as prognostic factors and mediators of osteosarcoma progression and lung metastasis

2016

Lung metastasis is the major cause of death in osteosarcoma patients. However, molecular mechanisms underlying this metastasis remain poorly understood. To identify key molecules related with pulmonary metastasis of pediatric osteosarcomas, we analyzed high-throughput miRNA expression in a cohort of 11 primary tumors and 15 lung metastases. Results were further validated with an independent cohort of 10 primary tumors and 6 metastases. In parallel, we performed immunohistochemical analysis of activated signaling pathways in 36 primary osteosarcomas. Only phospho-AKT associated with lower overall survival in primary tumors, supporting its role in osteosarcoma progression. CTNNB1 expression a…

0301 basic medicineOncologyMaleCancer ResearchmiR‐200cLung NeoplasmsCDH1MetastasisCohort Studies0302 clinical medicineCell MovementPhospho‐AKTPhosphorylationChildOsteosarcomabiologyGeneral MedicineArticlesCadherinsPrognosisPrimary tumorGene Expression Regulation Neoplasticmedicine.anatomical_structureLung metastasisOncology030220 oncology & carcinogenesisDisease ProgressionMolecular MedicineOsteosarcomaFemaleSignal Transductionmedicine.medical_specialtyAdolescentMesenchymal to epithelial transitionArticle03 medical and health sciencesYoung AdultAntigens CDInternal medicineCell Line TumormicroRNAGeneticsmedicineBiomarkers TumorHumansEpithelial–mesenchymal transitionCell ProliferationLungGene Expression ProfilingReproducibility of ResultsEpithelial CellsPediatric osteosarcomamedicine.diseaseSurvival AnalysisEnzyme ActivationMicroRNAs030104 developmental biologyTumor progressionbiology.proteinProto-Oncogene Proteins c-aktMolecular Oncology
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Innovative Therapeutic Strategies Targeting Colorectal Cancer Stem Cells

2017

Colorectal cancer is the fourth most common cause of cancer-related death. Although many advances in the treatment of this disease have been made, a large number of patients develop metastasis and resistance to current therapies. The current evidence indicates that cancer stem cells (CSCs) and epithelial-to-mesenchymal transition (EMT) have crucial roles in colorectal carcinogenesis and metastasis. It is also very important to understand the mechanisms that allow the survival of CSCs, such as metabolic reprogramming, which permits them to obtain specific properties or the activation of alternative signaling pathways in response to first-line therapies. In this review, we discuss the failure…

0301 basic medicineOncologymedicine.medical_specialtyColorectal cancerMetabolic reprogrammingDiseaseMultidrug resistanceTarget therapyMetastasis03 medical and health sciences0302 clinical medicineCancer stem cellInternal medicineMedicineOxidative phosphorylationHepatologybusiness.industryCancer stem cellEMTGastroenterologyColorectal carcinogenesismedicine.disease030104 developmental biologyOncology030220 oncology & carcinogenesisCancer cellStem cellbusinessCurrent Colorectal Cancer Reports
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αB-crystallin response to a pro-oxidant non-cytotoxic environment in murine cardiac cells: An "in vitro" and "in vivo" study.

2020

The αB-crystallin (HSPB5) protein is modulated in response to a wide variety of stressors generated by multiple physio-pathological conditions, sustained by reactive oxygen species (ROS) production. In cardiac muscle tissue, this protein regulates various cellular processes, such as protein degradation, apoptosis and the stabilization of cytoskeletal elements. In this work, we studied the role of HSPB5 expression, activation and localization in HL-1 murine cardiomyocytes exposed to pro-oxidant and non-cytotoxic H2O2 concentration, as well as in cardiac tissue isolated from mice following an acute, non-damaging endurance exercise. Our results demonstrated that HSPB5 is the most abundant HSP …

0301 basic medicineOxidative eustressOxidative phosphorylationProtein degradationBiochemistry03 medical and health sciencesMice0302 clinical medicineIn vivoPhysiology (medical)medicineAnimalsCardiac musclePhosphorylationchemistry.chemical_classificationReactive oxygen speciesHSPB5ChemistryCardiac musclealpha-Crystallin B ChainHydrogen PeroxidePro-oxidantEndurance exerciseHSPA1ACell biology030104 developmental biologymedicine.anatomical_structureProteolysisCardiac muscle tissueReactive Oxygen SpeciesOxidation-Reduction030217 neurology & neurosurgeryFree radical biologymedicine
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Free-energy studies reveal a possible mechanism for oxidation-dependent inhibition of MGL

2016

AbstractThe function of monoacylglycerol lipase (MGL), a key actor in the hydrolytic deactivation of the endocannabinoid 2-arachidonoyl-sn-glycerol (2AG), is tightly controlled by the cell’s redox state: oxidative signals such as hydrogen peroxide suppress MGL activity in a reversible manner through sulfenylation of the peroxidatic cysteines, C201 and C208. Here, using as a starting point the crystal structures of human MGL (hMGL), we present evidence from molecular dynamics and metadynamics simulations along with high-resolution mass spectrometry studies indicating that sulfenylation of C201 and C208 alters the conformational equilibrium of the membrane-associated lid domain of MGL to favo…

0301 basic medicineOxidative phosphorylationMolecular Dynamics SimulationRedoxArticle03 medical and health scienceschemistry.chemical_compoundCatalytic DomainHumansCysteineHydrogen peroxideMultidisciplinary030102 biochemistry & molecular biologybiologyHydrogen bondMetadynamicsActive siteSubstrate (chemistry)Hydrogen BondingHydrogen PeroxideMonoacylglycerol LipasesMonoacylglycerol lipase030104 developmental biologyBiochemistrychemistrybiology.proteinBiophysicsThermodynamicsOxidation-ReductionProtein Processing Post-TranslationalProtein BindingScientific Reports
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Increased basal antioxidant levels in RCAN1 - deficient mice lowers oxidative injury after acute paraquat insult.

2020

RCAN1 is an inhibitor of the phosphatase calcineurin, which is involved in the regulation of oxidative stress and apoptosis, among other important cell processes. Here we have used RCAN1 deficient mice (RCAN1-/-) to elucidate its role after an acute oxidative insult such as paraquat injection. We have observed that RCAN1-/- mice show less oxidative damage than wildtype (WT) mice after treatment. Under basal conditions, RCAN1-/- animals express more calcineurin, heme oxygenase-1, Nrf2, and catalase compared to WT mice (controls). This may explain the less severe effect of paraquat treatment on RCAN1-/- mice compared to WT. We showed that oxidative stress is involved in the early stages of ap…

0301 basic medicineParaquatmedicine.medical_specialtyAntioxidantmedicine.medical_treatmentMuscle ProteinsOxidative phosphorylationmedicine.disease_causeBiochemistryAntioxidants03 medical and health scienceschemistry.chemical_compoundMiceParaquatInternal medicinemedicineAnimals030102 biochemistry & molecular biologybiologyCalcineurinGeneral MedicineGlutathioneCalcineurinDNA-Binding ProteinsOxidative Stress030104 developmental biologyEndocrinologychemistryCatalaseApoptosisbiology.proteinOxidative stressFree radical research
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(+)-Pentazocine reduces oxidative stress and apoptosis in microglia following hypoxia/reoxygenation injury

2016

Abstract Background Sigma-1 receptors (σ 1 R) are highly expressed in neurons as well as microglia and have been shown to modulate the inflammatory response in the central nervous system and thus may serve as possible target for neuroprotective strategies. The aim of the present study was to test the effect of (+)-pentazocine, a putative σ 1 R agonist, in an in vitro model of microglia activation. Methods Microglia (BV2 cells) was exposed (3 h) to 1% oxygen and reoxygenation was allowed for 24 h. Cells were treated with different concentrations (1, 10, 25 and 50 μM) of (+)-pentazocine in the presence or absence of NE-100 (1 μM), a well established σ 1 R antagonist. Cell viability and apopto…

0301 basic medicinePentazocineSigma receptorCell SurvivalmicrogliaApoptosisPharmacologyBiologymedicine.disease_causeNeuroprotection(+)-PentazocineCell LineMice03 medical and health scienceschemistry.chemical_compound0302 clinical medicinePentazocine; microglia; SIGMAmedicineAnimalsReceptors sigmaViability assayAnnexin A5PhosphorylationHypoxiaMembrane Potential MitochondrialMitogen-Activated Protein Kinase 1Mitogen-Activated Protein Kinase 3MicrogliaAnimalGeneral NeuroscienceApoptosiOxidative StreGlutathioneGlutathioneOxidative Stress030104 developmental biologymedicine.anatomical_structurePentazocineBiochemistrychemistryApoptosis030217 neurology & neurosurgeryIntracellularOxidative stressSIGMAmedicine.drug
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Estrogen Receptor Signaling and the PI3K/Akt Pathway Are Involved in Betulinic Acid-Induced eNOS Activation

2016

Betulinic acid (BA) is a naturally occurring pentacyclic triterpenoid with anti-inflammatory, antiviral and anti-cancer properties. Beneficial cardiovascular effects such as increased nitric oxide (NO) production through enhancement of endothelial NO synthase (eNOS) activity and upregulation of eNOS expression have been demonstrated for this compound. In the present study, immortalized human EA.hy 926 endothelial cells were incubated for up to 1 h with 1–100 µM BA and with the phosphatidylinositol-3-kinase (PI3K) inhibitors LY294002 and wortmannin, or the estrogen receptor (ER) antagonist ICI 182,780. Phosphorylation status of eNOS and total eNOS protein were analyzed by Western blotting us…

0301 basic medicinePharmaceutical ScienceEstrogen receptorPI3KAnalytical ChemistryWortmanninchemistry.chemical_compound0302 clinical medicineEnosDrug DiscoveryLY294002PhosphorylationFulvestrantLungbiologyEstradiolendothelial cellsReceptors EstrogenChemistry (miscellaneous)030220 oncology & carcinogenesisMolecular MedicinePhosphorylationSignal transductionPentacyclic TriterpenesWortmanninSignal Transductionestrogen receptormedicine.medical_specialtyNitric Oxide Synthase Type IIIMorpholinesArticleCell Linelcsh:QD241-44103 medical and health sciencesbetulinic acidlcsh:Organic chemistryInternal medicinemedicineAnimalsHumansPhysical and Theoretical ChemistryProtein kinase BPI3K/AKT/mTOR pathwayendothelial nitric oxide synthaseAktOrganic ChemistryFibroblastsbiology.organism_classificationMolecular biologyTriterpenesbetulinic acid; endothelial nitric oxide synthase; endothelial cells; estrogen receptor; PI3K; AktRatsAndrostadienes030104 developmental biologyEndocrinologychemistryGene Expression RegulationChromonesPhosphatidylinositol 3-KinaseProto-Oncogene Proteins c-aktMolecules
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Agonist‐induced desensitisation of β 3 ‐adrenoceptors: Where, when, and how?

2019

β3 -Adrenoceptor agonists have proven useful in the treatment of overactive bladder syndrome, but it is not known whether their efficacy during chronic administration may be limited by receptor-induced desensitisation. Whereas the β2 -adrenoceptor has phosphorylation sites that are important for desensitisation, the β3 -adrenoceptor lacks these; therefore, it had been assumed that β3 -adrenoceptors are largely resistant to agonist-induced desensitisation. While all direct comparative studies demonstrate that β3 -adrenoceptors are less susceptible to desensitisation than β2 -adrenoceptors, desensitisation of β3 -adrenoceptors has been observed in many models and treatment settings. Chimeric …

0301 basic medicinePharmacologyAgonistMessenger RNAmedicine.medical_specialtyCell typePhosphorylation sitesAdrenergic receptormedicine.drug_classbusiness.industryChinese hamster ovary cellTransfection03 medical and health sciences030104 developmental biology0302 clinical medicineEndocrinologyInternal medicinemedicinebusinessReceptor030217 neurology & neurosurgeryBritish Journal of Pharmacology
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Silencing of C3G increases cardiomyocyte survival inhibition and apoptosis via regulation of p-ERK1/2 and Bax.

2018

Experimental studies have shown that overexpression of Rap guanine nucleotide exchange factor 1 (C3G) plays pro-survival and anti-apoptotic roles through molecule phosphorylated extracellular signal-regulated kinase1/2 (p-ERK1/2) in cardiomyocytes. However, it is still unclear if silencing of C3G may increase cell survival inhibition and apoptosis in cardiomyocytes, and whether C3G silence induced injuries are reduced by the overexpression of C3G through regulation of p-ERK1/2 and pro-apoptotic molecule Bax. In this study, the rat-derived H9C2 cardiomyocytes were infected with C3G small hairpin RNA interference recombinant lentiviruses, which silenced the endogenous C3G expression in the ca…

0301 basic medicinePhysiologyCell SurvivalEndogenyApoptosisCell LineSmall hairpin RNA03 medical and health sciences0302 clinical medicinePhysiology (medical)ExtracellularmedicineGene silencingAnimalsMyocytes CardiacGene SilencingGuanine Nucleotide-Releasing Factor 2Cell Proliferationbcl-2-Associated X ProteinPharmacologyMitogen-Activated Protein Kinase 1Mitogen-Activated Protein Kinase 3Cell growthChemistryHypoxia (medical)PhosphoproteinsCell biologyRats030104 developmental biologyApoptosis030220 oncology & carcinogenesisPhosphorylationmedicine.symptomClinical and experimental pharmacologyphysiology
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MYC and MCL1 Cooperatively Promote Chemotherapy-Resistant Breast Cancer Stem Cells via Regulation of Mitochondrial Oxidative Phosphorylation

2017

Summary Most patients with advanced triple-negative breast cancer (TNBC) develop drug resistance. MYC and MCL1 are frequently co-amplified in drug-resistant TNBC after neoadjuvant chemotherapy. Herein, we demonstrate that MYC and MCL1 cooperate in the maintenance of chemotherapy-resistant cancer stem cells (CSCs) in TNBC. MYC and MCL1 increased mitochondrial oxidative phosphorylation (mtOXPHOS) and the generation of reactive oxygen species (ROS), processes involved in maintenance of CSCs. A mutant of MCL1 that cannot localize in mitochondria reduced mtOXPHOS, ROS levels, and drug-resistant CSCs without affecting the anti-apoptotic function of MCL1. Increased levels of ROS, a by-product of a…

0301 basic medicinePhysiologyMice NudeTriple Negative Breast NeoplasmsOxidative phosphorylationTumor initiationMitochondrionBiologyOxidative PhosphorylationArticleProto-Oncogene Proteins c-myc03 medical and health sciencesCancer stem cellCell Line TumorAnimalsHumansMCL1Molecular BiologyTriple-negative breast cancerchemistry.chemical_classificationReactive oxygen speciesCell BiologyMitochondria030104 developmental biologychemistryDrug Resistance NeoplasmNeoplastic Stem CellsCancer researchMyeloid Cell Leukemia Sequence 1 ProteinFemaleStem cellReactive Oxygen SpeciesCell Metabolism
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