Search results for "Rapamycin"

showing 10 items of 44 documents

The landscape of epilepsy-related GATOR1 variants

2019

Purpose:\ud \ud To define the phenotypic and mutational spectrum of epilepsies related to DEPDC5, NPRL2 and NPRL3 genes encoding the GATOR1 complex, a negative regulator of the mTORC1 pathway.\ud \ud Methods:\ud \ud We analyzed clinical and genetic data of 73 novel probands (familial and sporadic) with epilepsy-related variants in GATOR1-encoding genes and proposed new guidelines for clinical interpretation of GATOR1 variants.\ud \ud Results:\ud \ud The GATOR1 seizure phenotype consisted mostly in focal seizures (e.g., hypermotor or frontal lobe seizures in 50%), with a mean age at onset of 4.4 years, often sleep-related and drug-resistant (54%), and associated with focal cortical dysplasia…

Male0301 basic medicineProbandDEPDC5SUDEP030105 genetics & heredityBioinformaticsLoss of Function Mutation/geneticsEpilepsyINDEL MutationLoss of Function MutationmTORC1 pathwayGenetics(clinical)ChildGenetics (clinical)Multiprotein Complexes/geneticsBrugada SyndromeDNA Copy Number VariationBrugada syndromeINDEL Mutation/geneticsGTPase-Activating ProteinsNPRL3SeizureDEPDC5PhenotypePedigree3. Good healthBrugada Syndrome/geneticsChild PreschoolFemaleHumanSignal TransductionDNA Copy Number VariationsAdolescentSeizures/complicationsMechanistic Target of Rapamycin Complex 1/geneticsDNA Copy Number Variations/geneticsMechanistic Target of Rapamycin Complex 1Tumor Suppressor Proteins/geneticsArticleFocal cortical dysplasia03 medical and health sciencesSeizuresGTPase-Activating Proteins/geneticsmedicineHumansGenetic Predisposition to DiseaseDEPDC5; Focal cortical dysplasia; Genetic focal epilepsy; mTORC1 pathway; SUDEPGenetic focal epilepsyEpilepsy/complicationsRepressor Proteins/geneticsEpilepsybusiness.industryGTPase-Activating ProteinTumor Suppressor ProteinsInfant NewbornCorrectionInfantRepressor ProteinCortical dysplasiamedicine.diseaseddc:616.8Repressor Proteins030104 developmental biologyFrontal lobe seizures[SDV.GEN.GH]Life Sciences [q-bio]/Genetics/Human geneticsMultiprotein ComplexesMultiprotein ComplexeSignal Transduction/geneticsHuman medicinebusiness
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The K63 deubiquitinase CYLD modulates autism-like behaviors and hippocampal plasticity by regulating autophagy and mTOR signaling.

2021

Nondegradative ubiquitin chains attached to specific targets via Lysine 63 (K63) residues have emerged to play a fundamental role in synaptic function. The K63-specific deubiquitinase CYLD has been widely studied in immune cells and lately also in neurons. To better understand if CYLD plays a role in brain and synapse homeostasis, we analyzed the behavioral profile of CYLD-deficient mice. We found that the loss of CYLD results in major autism-like phenotypes including impaired social communication, increased repetitive behavior, and cognitive dysfunction. Furthermore, the absence of CYLD leads to a reduction in hippocampal network excitability, long-term potentiation, and pyramidal neuron s…

MaleAutism Spectrum DisorderNerve Tissue ProteinsHippocampal formationHippocampusDeubiquitinating enzymeSynapseMiceUbiquitinAutophagyAnimalsAutistic DisorderMechanistic target of rapamycinPI3K/AKT/mTOR pathwayNeuronsMultidisciplinarybiologyUbiquitinLysineTOR Serine-Threonine KinasesAutophagyMicrofilament ProteinsUbiquitinationLong-term potentiationBiological SciencesDeubiquitinating Enzyme CYLDMice Inbred C57BLSynapsesbiology.proteinFemaleNeuroscienceSignal TransductionProceedings of the National Academy of Sciences of the United States of America
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Sirolimus Use in Liver Transplant Recipients With Hepatocellular Carcinoma: A Randomized, Multicenter, Open-Label Phase 3 Trial

2016

International audience; BACKGROUND:We investigated whether sirolimus-based immunosuppression improves outcomes in liver transplantation (LTx) candidates with hepatocellular carcinoma (HCC).METHODS:In a prospective-randomized open-label international trial, 525 LTx recipients with HCC initially receiving mammalian target of rapamycin inhibitor-free immunosuppression were randomized 4 to 6 weeks after transplantation into a group on mammalian target of rapamycin inhibitor-free immunosuppression (group A: 264 patients) or a group incorporating sirolimus (group B: 261). The primary endpoint was recurrence-free survival (RFS); intention-to-treat (ITT) analysis was conducted after 8 years. Overal…

MaleTime FactorsIntention to Treat Analysimedicine.medical_treatmentMedizinPROGRESSIONKaplan-Meier EstimateLiver transplantationGastroenterologyImmunosuppressive Agent0302 clinical medicineEVEROLIMUSRENAL-CELL CARCINOMARisk FactorsMedicine and Health SciencesClinical endpointAge FactorSirolimuProspective StudiesIMMUNOSUPPRESSIONTOR Serine-Threonine KinaseTOR Serine-Threonine KinasesHazard ratioLiver NeoplasmsAge FactorsImmunosuppressionMiddle AgedCANCER3. Good healthIntention to Treat AnalysisEuropeRAPAMYCIN INHIBITORSTreatment OutcomeTARGETLocalLiver Neoplasm030220 oncology & carcinogenesisCombinationDisease ProgressionSURVIVAL[SDV.IMM]Life Sciences [q-bio]/Immunology030211 gastroenterology & hepatologyDrug Therapy CombinationFemaleImmunosuppressive Agentsmedicine.drugHumanAdultmedicine.medical_specialtyCanadaCarcinoma HepatocellularTime Factor[SDV.MHEP.CHI]Life Sciences [q-bio]/Human health and pathology/SurgeryRisk AssessmentDisease-Free Survival03 medical and health sciencesYoung AdultDrug TherapyInternal medicinemedicineHumansAdult; Age Factors; Aged; Australia; Canada; Carcinoma Hepatocellular; Disease Progression; Disease-Free Survival; Drug Therapy Combination; Europe; Female; Humans; Immunosuppressive Agents; Intention to Treat Analysis; Kaplan-Meier Estimate; Liver Neoplasms; Male; Middle Aged; Neoplasm Recurrence Local; Prospective Studies; Risk Assessment; Risk Factors; Sirolimus; TOR Serine-Threonine Kinases; Time Factors; Treatment Outcome; Young Adult; Liver Transplantation; TransplantationRECURRENCEMETAANALYSISAgedSirolimusTransplantationEverolimusIntention-to-treat analysisbusiness.industryRisk FactorCarcinomaAustraliaHepatocellular3126 Surgery anesthesiology intensive care radiologySurgeryLiver TransplantationTransplantationProspective StudieNeoplasm RecurrenceSirolimusNeoplasm Recurrence Localbusiness
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Sirolimus exposure and the occurrence of cytomegalovirus DNAemia after allogeneic hematopoietic stem cell transplantation

2018

Sirolimus appears to protect against cytomegalovirus (CMV) in organ transplant recipients. The effect of this drug in allogeneic hematopoietic stem cell transplantation recipients remains unexplored. By means of multivariate continuous-time Markov model analyses, we identified 3 independent covariates that significantly impacted the risk of CMV DNAemia: recipient/donor CMV serostatus, tacrolimus exposure, and sirolimus exposure. CMV-seropositive recipients with CMV-seronegative donors had a significantly higher probability of having detectable CMV DNAemia. Increasing the tacrolimus trough concentration from 0 to 16 ng/mL increased the probability of patients having detectable CMV DNAemia by…

Malebasic (laboratory) research/science0301 basic medicinemedicine.medical_treatmentCytomegalovirusHematopoietic stem cell transplantationGastroenterologyOrgan transplantation0302 clinical medicineRisk FactorsImmunology and AllergyPharmacology (medical)Whole bloodIncidenceHematopoietic Stem Cell Transplantationvirus diseasesMiddle AgedPrognosissurgical procedures operativeCytomegalovirus Infectionscytomegalovirus (CMV) [infection and infectious agents-viral]Femaleantiviral [antibiotic]pharmacokinetics/pharmacodynamicsImmunosuppressive Agentsmedicine.drugAdultmedicine.medical_specialtyinfectious diseasesirolimus [immunosuppressant-mechanistic target of rapamycin]clinical research/practicetacrolimus [immunosuppressant-calcineurin inhibitor]03 medical and health sciencesInternal medicinemedicineHumansTransplantation HomologousTrough ConcentrationViremiabone marrow/hematopoietic stem cell transplantationAgedSirolimusTransplantationbusiness.industryTransplant RecipientsTacrolimus030104 developmental biologySpainRelative riskSirolimusDNA ViralpharmacologybusinessSerostatusFollow-Up Studies030215 immunology
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Muscle protein synthesis, mTORC1/MAPK/Hippo signaling, and capillary density are altered by blocking of myostatin and activins

2012

Loss of muscle mass and function occurs in various diseases. Myostatin blocking can attenuate muscle loss, but downstream signaling is not well known. Therefore, to elucidate associated signaling pathways, we used the soluble activin receptor IIb (sActRIIB-Fc) to block myostatin and activins in mice. Within 2 wk, the treatment rapidly increased muscle size as expected but decreased capillary density per area. sActRIIB-Fc increased muscle protein synthesis 1–2 days after the treatment correlating with enhanced mTORC1 signaling (phosphorylated rpS6 and S6K1, r = 0.8). Concurrently, increased REDD1 and eIF2Bε protein contents and phosphorylation of 4E-BP1 and AMPK was observed. In contrast, pr…

Malemedicine.medical_specialtyPhysiologyEndocrinology Diabetes and MetabolismMuscle ProteinsCell CountP70-S6 Kinase 1MyostatinMechanistic Target of Rapamycin Complex 1Protein Serine-Threonine KinasesBiologyMice03 medical and health sciences0302 clinical medicinePhysiology (medical)Internal medicinemedicineAnimalsHippo Signaling PathwayExtracellular Signal-Regulated MAP KinasesMuscle Skeletalta315030304 developmental biology0303 health sciencesHippo signaling pathwayMyogenesisTOR Serine-Threonine KinasesSkeletal muscleActivin receptorMyostatinActivinsCapillariesMice Inbred C57BLmedicine.anatomical_structureEndocrinologyHippo signalingMultiprotein ComplexesProtein Biosynthesisbiology.proteinIntercellular Signaling Peptides and ProteinsPhosphorylation030217 neurology & neurosurgerySignal TransductionAmerican Journal of Physiology-Endocrinology and Metabolism
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Mitochondrial dynamics in type 2 diabetes: Pathophysiological implications

2017

Mitochondria play a key role in maintaining cellular metabolic homeostasis. These organelles have a high plasticity and are involved in dynamic processes such as mitochondrial fusion and fission, mitophagy and mitochondrial biogenesis. Type 2 diabetes is characterised by mitochondrial dysfunction, high production of reactive oxygen species (ROS) and low levels of ATP. Mitochondrial fusion is modulated by different proteins, including mitofusin-1 (MFN1), mitofusin-2 (MFN2) and optic atrophy (OPA-1), while fission is controlled by mitochondrial fission 1 (FIS1), dynamin-related protein 1 (DRP1) and mitochondrial fission factor (MFF). PARKIN and (PTEN)-induced putative kinase 1 (PINK1) partici…

MiD51 mitochondrial dynamics proteins of 51 kDaΔΨm mitochondrial membrane potential0301 basic medicineMitochondrial fission factorClinical BiochemistryMitochondrial DegradationMFN2Review ArticleTXNIP thioredoxin interacting proteinMitochondrial DynamicsBiochemistryAdenosine TriphosphateGRP78 78 kDa glucose-regulated proteinMFF mitochondrial fission factorMFN2 mitofusin 2TRX2 thioredoxin 2Redox biologylcsh:QH301-705.5NF-κB nuclear factor kappa Blcsh:R5-920MitophagyType 2 diabetesDRP1 dynamin-related protein 1FIS1 fission protein 1BNIP3 BCL2/adenovirus E1B 19 kDa interacting protein 3MitochondriaOPA1 optic atrophy 1SIRT1/3 sirtuin 1/3Biochemistrymitochondrial fusionTGF-β1 transforming growth factor-β1Mitochondrial fissionOMM outer mitochondrial membranelcsh:Medicine (General)MiD49 mitochondrial dynamics proteins of 49Nox 4 NADPH oxidase-4IMM inner mitochondrial membraneFIS1ATF6 activating transcription factor 6PINK1mTOR mammalian target of rapamycinCHOP C/EBP homologous proteinBiologymdivi-1 mitochondrial division inhibitor-1Mitochondrial Proteins03 medical and health sciencesROS reactive oxygen speciessXBP1 spliced X-box binding protein 1UCP-1 uncoupling protein-1MFN1 mitofusin 1SOD superoxide dismutaseLC3 1 A/1B-light chain 3HumansPINK1 (PTEN)-induced putative kinase 1S3 15-OxospiramilactoneOrganic ChemistrymtDNA mitochondrial DNAAMPK AMP-activated protein kinase030104 developmental biologyDiabetes Mellitus Type 2Mitochondrial biogenesislcsh:Biology (General)Oxidative stressp38 MAPK p38 mitogen-activated protein kinasep62/SQSTM1 ubiquitin and sequestosome-1Reactive Oxygen SpeciesRedox Biology
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Yeast Translation Elongation Factor eIF5A Expression Is Regulated by Nutrient Availability through Different Signalling Pathways

2020

Translation elongation factor eIF5A binds to ribosomes to promote peptide bonds between problematic amino acids for the reaction like prolines. eIF5A is highly conserved and essential in eukaryotes, which usually contain two similar but differentially expressed paralogue genes. The human eIF5A-1 isoform is abundant and implicated in some cancer types

MitochondrionBiotecnologialcsh:ChemistryPeptide Initiation FactorsGene Expression Regulation Fungalmitochondrial respirationGene expressionExpressió genèticaHap1Protein Isoformshemelcsh:QH301-705.5SpectroscopyChemistryRNA-Binding ProteinsTranslation (biology)Iron DeficienciesGeneral MedicineTORAerobiosisUp-RegulationComputer Science ApplicationsCell biologySnf1EIF5ASignal TransductionGene isoformSaccharomyces cerevisiae ProteinsIronCitric Acid CycleDown-RegulationSaccharomyces cerevisiaeMechanistic Target of Rapamycin Complex 1Models BiologicalArticleCatalysisInorganic ChemistryeIF5APhysical and Theoretical ChemistryMolecular BiologyTranscription factorGeneLysineOrganic ChemistryNutrientsMetabolismCarbonMetabolic Flux AnalysisGlucoselcsh:Biology (General)lcsh:QD1-999Fermentationgene expressionInternational Journal of Molecular Sciences
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A prospective randomised, open-labeled, trial comparing sirolimus-containing versus mTOR-inhibitor-free immunosuppression in patients undergoing live…

2010

Abstract Background The potential anti-cancer effects of mammalian target of rapamycin (mTOR) inhibitors are being intensively studied. To date, however, few randomised clinical trials (RCT) have been performed to demonstrate anti-neoplastic effects in the pure oncology setting, and at present, no oncology endpoint-directed RCT has been reported in the high-malignancy risk population of immunosuppressed transplant recipients. Interestingly, since mTOR inhibitors have both immunosuppressive and anti-cancer effects, they have the potential to simultaneously protect against immunologic graft loss and tumour development. Therefore, we designed a prospective RCT to determine if the mTOR inhibito…

OncologyCancer ResearchTime Factorsmedicine.medical_treatmentMedizinIntracellular Signaling Peptides and Proteins - antagonists & inhibitors metabolismKaplan-Meier Estimate312 Clinical medicineProtein-Serine-Threonine KinaseLiver transplantationTHERAPYStudy ProtocolImmunosuppressive Agentendothelial growth-factor renal-cell carcinoma tumor progression rapamycin cancer cyclosporine efficacy therapy target model0302 clinical medicineRENAL-CELL CARCINOMARisk FactorsRecurrenceSurgical oncologyMedicine and Health SciencesLiver Neoplasms - drug therapy enzymology mortality surgerySirolimuProspective StudiesTUMOR PROGRESSIONTransplantation Homologoueducation.field_of_studyliver transplantationTOR Serine-Threonine KinasesLiver NeoplasmsIntracellular Signaling Peptides and ProteinsImmunosuppressionhepatocellular carcinomalcsh:Neoplasms. Tumors. Oncology. Including cancer and carcinogensCANCER3. Good healthEuropeMulticenter StudyTreatment OutcomeTARGETsirolimusOncologyLiver Neoplasm030220 oncology & carcinogenesisHepatocellular carcinomaRandomized Controlled TrialmTORCarcinoma Hepatocellular - drug therapy enzymology mortality surgery030211 gastroenterology & hepatologyImmunosuppressive AgentsRCTHumanmedicine.drugCanadamedicine.medical_specialtyCarcinoma HepatocellularTime FactoreducationPopulationLiver Transplantation - adverse effects mortalityProtein Serine-Threonine Kinaseslcsh:RC254-282Disease-Free Survival03 medical and health sciencesInternal medicineGeneticsmedicineTransplantation HomologousHumansComparative StudyRapamycinddc:610educationProtein-Serine-Threonine Kinases - antagonists & inhibitors metabolismKaplan-Meiers Estimatebusiness.industryRisk FactorAustraliaImmunosuppressive Agents - therapeutic useSirolimus - therapeutic useEFFICACYHumans; Liver Transplantation; Hepatocellular Carcinoma; Randomized Controlled Trial; RCT; Multicenter Study; Comparative Study; Rapamycin; mTOR; Sirolimusmedicine.diseaseSurgeryMODELTransplantationClinical trialProspective StudieIntracellular Signaling Peptides and ProteinSirolimusENDOTHELIAL GROWTH-FACTORCYCLOSPORINERAPAMYCINbusiness
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Deregulation of the EGFR/PI3K/PTEN/Akt/mTORC1 pathway in breast cancer: possibilities for therapeutic intervention

2014

// Nicole M. Davis 1 , Melissa Sokolosky 1 , Kristin Stadelman 1 , Stephen L. Abrams 1 , Massimo Libra 2 , Saverio Candido 2 , Ferdinando Nicoletti 2 , Jerry Polesel 3 , Roberta Maestro 4 , Antonino D’Assoro 5 , Lyudmyla Drobot 6 , Dariusz Rakus 7 , Agnieszka Gizak 7 , Piotr Laidler 8 , Joanna Dulinska-Litewka 8 , Joerg Basecke 9 , Sanja Mijatovic 10 , Danijela Maksimovic-Ivanic 10 , Giuseppe Montalto 11,12 , Melchiorre Cervello 12 , Timothy L. Fitzgerald 13 , Zoya N. Demidenko 14 , Alberto M. Martelli 15 , Lucio Cocco 15 , Linda S. Steelman 1 and James A. McCubrey 1 1 Department of Microbiology and Immunology, Brody School of Medicine at East Carolina University Greenville, NC 27858 USA 2 …

Oncologymedicine.medical_specialtytherapy resistanceClass I Phosphatidylinositol 3-Kinasesmedicine.medical_treatmentBreast NeoplasmsReviewBiologyMechanistic Target of Rapamycin Complex 1PI3KMetastasisTargeted therapyPhosphatidylinositol 3-KinasesBreast cancerTARGETED THERAPYInternal medicinemedicinePTENHumansTargeted Therapy Therapy Resistance Mutations PI3K mTOR rapamycinskin and connective tissue diseasesProtein kinase BneoplasmsPI3K/AKT/mTOR pathwayRoswell Park Cancer InstituterapamycinTOR Serine-Threonine KinasesMTORPTEN PhosphohydrolaseCancerTargeted TherapyTherapy Resistancemedicine.diseaseTargeted Therapy; Therapy Resistance; Mutations; PI3K; mTOR; rapamycin3. Good healthErbB ReceptorsGene Expression Regulation NeoplasticOncologyMultiprotein ComplexesCancer researchbiology.proteinFemaleReceptor Epidermal Growth FactormutationRAPAMYCINProto-Oncogene Proteins c-aktMutationsSignal Transduction
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Inhalable polymeric microparticles as pharmaceutical porous powder for drug administration

2022

In this work, the production of inhalable polymeric microparticles with modulable porosity is described. The starting polymeric material was the PHEA-g-RhB-g-PLA graft copolymer, which was suitably processed by spray drying (SD). Thanks to the addition of AB (weight percentage equal to 10 and 20 % with respect to the polymer) in the liquid feed, three biocompatible matrices were obtained with an increasing porosity in terms of pore volume (from 0.015 to 0.024 cc/g) and pore average diameter (from 1.942 to 3.060 nm), a decreasing tapped density values (from 0.75 to 0.50), and favorable aerosolization characteristics. These differences were high-lighted also by a significant increase in the r…

Porous microparticlesDrug CarriersPolymersSettore CHIM/09 - Farmaceutico Tecnologico ApplicativoAdministration InhalationPharmaceutical SciencePulmonary administrationRapamycinPowdersParticle SizePorosityαβ-Poly(N-2-hydroxyethyl)-Dl-ASPARTAMIDE (PHEA)
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