Search results for "regulation"

showing 10 items of 4463 documents

Synthesis and antiproliferative activity of a natural like glycoconjugate polycyclic compound

2016

Abstract A natural like O -glycoconjugate polycyclic compound 4 was obtained by a multistep procedure starting from N -(3-methyl-1-(4-nitrophenyl)-1 H -pyrazol-5-yl)acetamide. The glycosyl derivative 4 showed antiproliferative activity against all the tumoral cell lines of the NCI panel in the range 0.47–5.43  μ M. Cytofluorimetric analysis performed on MDA-MB231, a very aggressive breast cancer cell line, which does not express estrogen, progesterone and HER-2/neu receptors, showed that 4 is able to induce prolonged cell cycle arrest at G2/M phase and morphological signs of differentiation. These events are correlated with down-regulation of both cyclin B1 and cdc2, the cyclins involved in…

0301 basic medicineCell cycle checkpointCell SurvivalReceptor ErbB-2StereochemistryGlycoconjugateAntineoplastic AgentsAntiproliferative activityChemistry Techniques Synthetic03 medical and health sciences0302 clinical medicineCyclin-dependent kinaseCell Line TumorDrug DiscoveryHumansPolycyclic CompoundsMDA-MB231Cyclin B1Cell ProliferationCyclinPharmacologychemistry.chemical_classificationBiological ProductsCyclin-dependent kinase 1G2/M phase arrestp21WAF1 inhibitorbiologyChemistryKinaseDrug Discovery3003 Pharmaceutical ScienceO-glycoconjugate polycyclic compoundOrganic ChemistryGeneral MedicineMolecular biologyG2 Phase Cell Cycle CheckpointsGene Expression Regulation Neoplastic030104 developmental biologyCell culturePyrazolo[34-b]pyrazolo[3′4′:23]azepino[45-f]azocineDrug Design030220 oncology & carcinogenesisbiology.proteinM Phase Cell Cycle CheckpointsReceptors ProgesteroneGlycoconjugatesEuropean Journal of Medicinal Chemistry
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Conversion of Nonproliferating Astrocytes into Neurogenic Neural Stem Cells: Control by FGF2 and Interferon-gamma

2016

Abstract Conversion of astrocytes to neurons, via de-differentiation to neural stem cells (NSC), may be a new approach to treat neurodegenerative diseases and brain injuries. The signaling factors affecting such a cell conversion are poorly understood, and they are hard to identify in complex disease models or conventional cell cultures. To address this question, we developed a serum-free, strictly controlled culture system of pure and homogeneous “astrocytes generated from murine embryonic stem cells (ESC).” These stem cell derived astrocytes (mAGES), as well as standard primary astrocytes resumed proliferation upon addition of FGF. The signaling of FGF receptor tyrosine kinase converted G…

0301 basic medicineCell signalingNeurogenesisBiologyInterferon-gammaMice03 medical and health sciences0302 clinical medicineNeural Stem CellsNeurosphereddc:570medicineAnimalsCell ProliferationEpidermal Growth FactorMultipotent Stem CellsCell CycleNeurogenesisMouse Embryonic Stem CellsCell BiologyAnatomyCell DedifferentiationEmbryonic stem cellNeural stem cellCell biologyNeuroepithelial cell030104 developmental biologymedicine.anatomical_structureGene Expression RegulationAstrocytesMolecular MedicineFibroblast Growth Factor 2Stem cell030217 neurology & neurosurgerySignal TransductionDevelopmental BiologyAstrocyte
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EphrinB2 repression through ZEB2 mediates tumour invasion and anti-angiogenic resistance.

2016

Diffuse invasion of the surrounding brain parenchyma is a major obstacle in the treatment of gliomas with various therapeutics, including anti-angiogenic agents. Here we identify the epi-/genetic and microenvironmental downregulation of ephrinB2 as a crucial step that promotes tumour invasion by abrogation of repulsive signals. We demonstrate that ephrinB2 is downregulated in human gliomas as a consequence of promoter hypermethylation and gene deletion. Consistently, genetic deletion of ephrinB2 in a murine high-grade glioma model increases invasion. Importantly, ephrinB2 gene silencing is complemented by a hypoxia-induced transcriptional repression. Mechanistically, hypoxia-inducible facto…

0301 basic medicineCell signalingScienceGeneral Physics and AstronomyRepressorDown-RegulationAngiogenesis InhibitorsEphrin-B2BiologyGeneral Biochemistry Genetics and Molecular BiologyArticleNeovascularization03 medical and health sciencesDownregulation and upregulationddc:570GliomamedicineGene silencingAnimalsHumansNeoplasm InvasivenessPsychological repressionZinc Finger E-box Binding Homeobox 2Regulation of gene expressionMice KnockoutMultidisciplinaryNeovascularization PathologicQGeneral ChemistryGliomamedicine.diseaseHypoxia-Inducible Factor 1 alpha SubunitXenograft Model Antitumor AssaysCell HypoxiaCell biologyUp-RegulationBevacizumabGene Expression Regulation NeoplasticMice Inbred C57BL030104 developmental biologyDrug Resistance Neoplasmmedicine.symptomNature communications
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Anti-Oxidant, Anti-Inflammatory and Anti-Angiogenic Properties of Resveratrol in Ocular Diseases

2016

International audience; Resveratrol (3,4,5 trihydroxy-trans-stilbene) is one of the best known phytophenols with pleiotropic properties. It is a phytoalexin produced by vine and it leads to the stimulation of natural plant defenses but also exhibits many beneficial effects in animals and humans by acting on a wide range of organs and tissues. These include the prevention of cardiovascular diseases, anti-cancer potential, neuroprotective effects, homeostasia maintenance, aging delay and a decrease in inflammation. Age-related macular degeneration (AMD) is one of the main causes of deterioration of vision in adults in developed countries This review deals with resveratrol and ophthalmology by…

0301 basic medicineCell typeAntioxidantEye Diseasesmedicine.drug_classmedicine.medical_treatmentAnti-Inflammatory AgentsDrug Evaluation PreclinicalPharmaceutical ScienceAngiogenesis InhibitorsInflammationReviewPharmacologyBiologyResveratrolresveratrolNeuroprotectionAntioxidantsAnti-inflammatoryAnalytical Chemistrylcsh:QD241-44103 medical and health scienceschemistry.chemical_compoundImmune systemlcsh:Organic chemistry[ CHIM.ORGA ] Chemical Sciences/Organic chemistryStilbenesDrug DiscoverymedicineAnimalsHumansPhysical and Theoretical Chemistrychemistry.chemical_classificationPhytoalexinOrganic ChemistryeyesDisease Models Animal030104 developmental biologyGene Expression RegulationchemistryBiochemistryChemistry (miscellaneous)inflammation[ SDV.MHEP.OS ] Life Sciences [q-bio]/Human health and pathology/Sensory OrgansMolecular Medicinemedicine.symptom
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The Drosophila Hox gene Ultrabithorax acts both in muscles and motoneurons to orchestrate formation of specific neuromuscular connections

2016

Hox genes are known to specify motoneuron pools in the developing vertebrate spinal cord and to control motoneuronal targeting in several species. However, the mechanisms controlling axial diversification of muscle innervation patterns are still largely unknown. We present data showing that the Drosophila Hox gene Ultrabithorax (Ubx) acts in the late embryo to establish target specificity of ventrally projecting RP motoneurons. In abdominal segments A2 to A7, RP motoneurons innervate the ventrolateral muscles VL1-4, with VL1 and VL2 being innervated in a Wnt4-dependent manner. In Ubx mutants, these motoneurons fail to make correct contacts with muscle VL1, a phenotype partially resembling t…

0301 basic medicineCell typeEmbryo Nonmammaliananimal structuresNeuromuscular JunctionGenes InsectMuscle DevelopmentNeuromuscular junctionAnimals Genetically ModifiedHox genes03 medical and health sciencesWNT4MorphogenesismedicineAnimalsDrosophila ProteinsHox geneWnt Signaling PathwayMolecular BiologyTranscription factorUltrabithoraxHomeodomain ProteinsMotor NeuronsGeneticsbiologyMusclesmusculoskeletal neural and ocular physiologyfungiGenes HomeoboxGene Expression Regulation Developmentalbiology.organism_classificationMuscle innervationSegmental patterningCell biologyMotoneuronsDrosophila melanogaster030104 developmental biologymedicine.anatomical_structurenervous system209embryonic structuresDrosophilaWnt signalling pathwayDrosophila melanogasterDrosophila ProteinTranscription FactorsResearch ArticleDevelopmental BiologyDevelopment
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Deregulated miRNAs in bone health: Epigenetic roles in osteoporosis.

2019

MicroRNA (miRNA) has shown to enhance or inhibit cell proliferation, differentiation and activity of different cell types in bone tissue. The discovery of miRNA actions and their targets has helped to identify them as novel regulations actors in bone. Various studies have shown that miRNA deregulation mediates the progression of bone-related pathologies, such as osteoporosis. The present review intends to give an exhaustive overview of miRNAs with experimentally validated targets involved in bone homeostasis and highlight their possible role in osteoporosis development. Moreover, the review analyzes miRNAs identified in clinical trials and involved in osteoporosis.

0301 basic medicineCell typeHistologyPhysiologyEndocrinology Diabetes and MetabolismOsteoporosis030209 endocrinology & metabolismBiologyBone tissueBioinformaticsBone healthBone and BonesEpigenesis Genetic03 medical and health sciences0302 clinical medicineOsteoclastSettore BIO/13 - Biologia ApplicatamicroRNAmedicineAnimalsHumansEpigeneticsmiRNA Bone Bone diseaseOsteoblastsOsteoblastCell Differentiationmedicine.diseaseMicroRNAs030104 developmental biologymedicine.anatomical_structureGene Expression RegulationOsteoporosisBone
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Epithelium‐specific MyD88 signaling, but not DCs or macrophages, control acute intestinal infection with Clostridium difficile

2019

Infection with Clostridium difficile is one of the major causes of health care acquired diarrhea and colitis. Signaling though MyD88 downstream of TLRs is critical for initiating the early protective host response in mouse models of C. difficile infection (CDI). In the intestine, MyD88 is expressed in various tissues and cell types, such as the intestinal epithelium and mononuclear phagocytes (MNP), including DC or macrophages. Using a genetic gain-of-function system, we demonstrate here that restricting functional MyD88 signaling to the intestinal epithelium, but also to MNPs is sufficient to protect mice during acute CDI by upregulation of the intestinal barrier function and recruitment o…

0301 basic medicineCell typeImmunologyBiologyMice03 medical and health sciences0302 clinical medicineDownregulation and upregulationmedicineAnimalsImmunology and AllergyIntestinal MucosaColitisEnterocolitis PseudomembranousBarrier functionClostridioides difficileMacrophagesDendritic CellsClostridium difficilemedicine.diseaseIntestinal epitheliumPhenotypeEpitheliumDisease Models Animal030104 developmental biologymedicine.anatomical_structureHost-Pathogen InteractionsMyeloid Differentiation Factor 88ImmunologySignal Transduction030215 immunologyEuropean Journal of Immunology
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Spleen tyrosine kinase (SYK) is a potential target for the treatment of cutaneous lupus erythematosus patients

2016

Spleen tyrosine kinase (SYK) is a protein kinase involved in cell proliferation and the regulation of inflammatory pathways. Due to the increasing evidence that kinase inhibitors have potential as specific anti-inflammatory drugs, we have investigated the potential for SYK inhibition as a therapeutic target in autoimmune diseases, particularly cutaneous lupus erythematosus (CLE). Skin samples of patients with different CLE subtypes and appropriate controls were analysed for the expression of SYK and SYK-associated pro-inflammatory mediators via gene expression analysis and immunohistochemistry. The functional role of SYK in keratinocytes was investigated in vitro, using LE-typical pro-infla…

0301 basic medicineCell typeSykchemical and pharmacologic phenomenaDermatologyenvironment and public healthBiochemistry03 medical and health sciencesImmune systemDownregulation and upregulationLupus Erythematosus CutaneousmedicineHumansSyk KinasePhosphorylationMolecular BiologyCells CulturedInnate immune systemSystemic lupus erythematosusKinasebusiness.industryhemic and immune systemsmedicine.diseaseenzymes and coenzymes (carbohydrates)030104 developmental biologyCase-Control StudiesImmunologyCytokinesPhosphorylationbiological phenomena cell phenomena and immunitybusinessExperimental Dermatology
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A High Throughput Phenotypic Screening reveals compounds that counteract premature osteogenic differentiation of HGPS iPS-derived mesenchymal stem ce…

2016

AbstractHutchinson-Gilford progeria syndrome (HGPS) is a rare fatal genetic disorder that causes systemic accelerated aging in children. Thanks to the pluripotency and self-renewal properties of induced pluripotent stem cells (iPSC), HGPS iPSC-based modeling opens up the possibility of access to different relevant cell types for pharmacological approaches. In this study, 2800 small molecules were explored using high-throughput screening, looking for compounds that could potentially reduce the alkaline phosphatase activity of HGPS mesenchymal stem cells (MSCs) committed into osteogenic differentiation. Results revealed seven compounds that normalized the osteogenic differentiation process an…

0301 basic medicineCell typecongenital hereditary and neonatal diseases and abnormalitiesPhenotypic screeningInduced Pluripotent Stem CellsRetinoic acidTretinoinBiologyArticle03 medical and health scienceschemistry.chemical_compoundProgeriaOsteogenesis[SDV.BBM.GTP]Life Sciences [q-bio]/Biochemistry Molecular Biology/Genomics [q-bio.GN]medicineHumansInduced pluripotent stem cellChildIsotretinoinGeneticsProgeriaMultidisciplinaryintegumentary systemGuided Tissue RegenerationMesenchymal stem cellnutritional and metabolic diseasesAging PrematureCell DifferentiationMesenchymal Stem Cellsmedicine.diseaseProgerinAlkaline PhosphataseLamin Type A3. Good healthCell biologyHigh-Throughput Screening Assays030104 developmental biologychemistryGene Expression Regulation[ SDV.BBM.GTP ] Life Sciences [q-bio]/Biochemistry Molecular Biology/Genomics [q-bio.GN]Alkaline phosphataseScientific Reports
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The HDAC6 Inhibitor tubacin induces release of CD133+ extracellular vesicles from cancer cells

2017

Tumor-derived extracellular vesicles (EVs) are emerging as an important mode of intercellular communication, capable of transferring biologically active molecules that facilitate the malignant growth and metastatic process. CD133 (Prominin-1), a stem cell marker implicated in tumor initiation, differentiation and resistance to anti-cancer therapy, is reportedly associated with EVs in various types of cancer. However, little is known about the factors that regulate the release of these CD133+ EVs. Here, we report that the HDAC6 inhibitor tubacin promoted the extracellular release of CD133+ EVs from human FEMX-I metastatic melanoma and Caco-2 colorectal carcinoma cells, with a concomitant dow…

0301 basic medicineCellBiologyBiochemistry03 medical and health sciencesDownregulation and upregulationSettore BIO/13 - Biologia ApplicataExtracellularmedicineLIPIDMolecular BiologyCancerCD 133TubacinCell BiologyHDAC6MicrovesiclesCell biologyExosome030104 developmental biologymedicine.anatomical_structureTrichostatin ACancer cellCancer researchextracellular vesicleIntracellularDeacetylase activitymedicine.drug
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