Search results for " Regulation"

showing 10 items of 3187 documents

Evaluation of the IKKβ Binding of Indicaxanthin by Induced-Fit Docking, Binding Pose Metadynamics, and Molecular Dynamics

2021

Background: Indicaxanthin, a betaxanthin belonging to the betalain class of compounds, has been recently demonstrated to exert significant antiproliferative effects inducing apoptosis of human melanoma cells through the inhibition of NF-κB as the predominant pathway. Specifically, Indicaxanthin inhibited IκBα degradation in A375 cells. In resting cells, NF-κB is arrested in the cytoplasm by binding to its inhibitor protein IκBα. Upon stimulation, IκBα is phosphorylated by the IKK complex, and degraded by the proteasome, liberating free NF-κB into the nucleus to initiate target gene transcription. Inhibition of the IKK complex leads to the arrest of the NF-κB pathway.Methods: To acquire deta…

PharmacologyMolecular modelChemistryAllosteric regulationIKKβMetadynamicsindicaxanthinInhibitor proteinRM1-950Settore CHIM/08 - Chimica Farmaceuticamolecular dynamicsIκBαchemistry.chemical_compoundanticancer activityProteasomeDocking (molecular)Settore BIO/10 - BiochimicaBiophysicsbinding pose metadynamicsPharmacology (medical)induced fit dockingTherapeutics. PharmacologyIndicaxanthinOriginal ResearchFrontiers in Pharmacology
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Transcriptional regulation and expression of CYP3A4 in hepatocytes.

2007

CYP3A4 is the most abundantly expressed drug-metabolizing P450 enzyme in human liver and contributes to the metabolism of a large number of drugs in use today. CYP3A4 is constitutively expressed in adult hepatocytes but it can also be transcriptionally induced by a variety of structurally diverse xenochemicals. CYP3A4 strongly contributes to the important variability in the therapeutic and toxic effects of drugs owing to the major role it plays in xenobiotic metabolism and the large intra- and inter-individual variability to which it is subjected. The functional examination of up to 13 kb of the CYP3A4 5'-flanking region has revealed that the regulation of this gene is a complex issue, with…

PharmacologyRegulation of gene expressionPregnane X receptorTranscription GeneticClinical BiochemistryDown-RegulationBiologyPharmacologyRegulatory Sequences Nucleic AcidGene Expression Regulation EnzymologicCell biologyDrug developmentNuclear receptorCytochrome P-450 Enzyme SystemLiverRegulatory sequenceTranscriptional regulationHepatocytesAnimalsCytochrome P-450 CYP3AHumansTranscription factorDrug metabolismCurrent drug metabolism
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PPARα/HNF4α Interplay on Diversified Responsive Elements. Relevance in the Regulation of Liver Peroxisomal Fatty Acid Catabolism

2012

In mammals, the liver is the major organ of fatty acid catabolism. This pathway is involved in both mitochondria and peroxisome. While mitochondria breaks down fatty acids with short, medium and long carbon chains, peroxisomes are involved in the catabolism of very long and branched chain fatty acids, which are degraded by three enzymes: acyl-CoA oxidase, multifunctional enzyme and thiolase enzyme. The active pathway results mainly from a tight transcriptional control of these gene-encoding enzymes. Two major nuclear receptors that are highly expressed in this organ are involved in this control, e.g. PPARα (peroxisome proliferator-activated receptor, α isoform) and HNF4α (hepatic nuclear fa…

Pharmacologychemistry.chemical_classificationFatty acid metabolismCatabolismThiolaseFatty AcidsClinical BiochemistryPeroxisome proliferator-activated receptorMetabolismPeroxisomeBiologyResponse Elementschemistry.chemical_compoundGene Expression RegulationHepatocyte Nuclear Factor 4LiverHepatocyte nuclear factor 4BiochemistrychemistryNuclear receptorPeroxisomesAnimalsHumansPPAR alphaCurrent Drug Metabolism
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Furosemide interactions with brain GABAA receptors

1997

1. The loop diuretic furosemide is known to antagonize the function of gamma-aminobutyric acid type A (GABAA) receptors. The purpose of the present study was to examine the direct interaction of furosemide with the GABAA receptors by autoradiography and ligand binding studies with native rat and human receptors and with recombinant receptors composed of rat subunits. 2. Autoradiography with [35S]-t-butylbicyclophosphorothionate ([35S]-TBPS) as a ligand indicated that furosemide (0.1-1 mM) reversed the 5 microM GABA-induced inhibition of binding only in the cerebellar granule cell layer of rat brain sections. In all other regions studied, notably also in the hippocampal and thalamic areas, f…

Pharmacologymedicine.medical_specialtyGABAA receptorChemistryAllosteric regulationFurosemidePharmacologyGABA receptor antagonistLigand (biochemistry)GABAA-rho receptorEndocrinologynervous systemInternal medicineConvulsantmedicineReceptormedicine.drugBritish Journal of Pharmacology
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Regulation of Phenotypic Switching and Heterogeneity in Photorhabdus luminescens Cell Populations.

2019

Phenotypic heterogeneity in bacterial cell populations allows genetically identical organisms to different behavior under similar environmental conditions. The Gram-negative bacterium Photorhabdus luminescens is an excellent organism to study phenotypic heterogeneity since their life cycle involves a symbiotic interaction with soil nematodes as well as a pathogenic association with insect larvae. Phenotypic heterogeneity is highly distinct in P. luminescens. The bacteria exist in two phenotypic forms that differ in various morphologic and phenotypic traits and are therefore distinguished as primary (1°) and secondary (2°) cells. The 1 cells are bioluminescent, pigmented, produce several sec…

Phenotypic switchingBacterial Physiological Phenomena03 medical and health sciences0302 clinical medicineSymbiosisBacterial ProteinsStructural BiologyPhotorhabdus luminescensSymbiosisMolecular BiologyOrganism030304 developmental biologyGenetics0303 health sciencesLife Cycle StagesbiologyGenetic heterogeneityPigmentationQuorum SensingPhenotypic traitGene Expression Regulation Bacterialbiology.organism_classificationPhenotypeNematodePhenotypeBiological Variation PopulationPhotorhabdus030217 neurology & neurosurgeryJournal of molecular biology
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Pho85 and PI(4,5)P(2) regulate different lipid metabolic pathways in response to cold

2019

Lipid homeostasis allows cells to adjust membrane biophysical properties in response to changes in environmental conditions. In the yeast Saccharomyces cerevisiae, a downward shift in temperature from an optimal reduces membrane fluidity, which triggers a lipid remodeling of the plasma membrane. How changes in membrane fluidity are perceived, and how the abundance and composition of different lipid classes is properly balanced, remain largely unknown. Here, we show that the levels of phosphatidylinositol 4,5-bisphosphate [PI(4,5)P2], the most abundant plasma membrane phosphoinositide, drop rapidly in response to a downward shift in temperature. This change triggers a signaling cascade trans…

Phosphatidylinositol 45-DiphosphateSaccharomyces cerevisiae ProteinsMembrane FluiditySphingoid basesAcclimatizationOrm2PhospholipidSaccharomyces cerevisiaePhosphoinositideTriacylglycerideSphingolipidArticle03 medical and health scienceschemistry.chemical_compoundGlycogen Synthase Kinase 3Gene Expression Regulation FungalMembrane fluidityLow temperatureInositolPhosphatidylinositolProtein kinase AMolecular Biology1-IP7030304 developmental biology0303 health sciencesChemistry030302 biochemistry & molecular biologyCell MembraneCell BiologyLipid MetabolismSphingolipidCyclin-Dependent KinasesCell biologyTORC2-Pkh1-Ypk1 signaling moduleCold TemperatureCytosolMetabolic pathwayPhospholipidMetabolic Networks and PathwaysSignal Transduction
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Differential gene expression in p53-mediated G(1) arrest of human fibroblasts after gamma-irradiation or N-phosphoacetyl-L-aspartate treatment.

2000

In human fibroblasts, N:-phosphoacetyl-L-aspartate (PALA) and gamma-radiation induce reversible and irreversible p53-mediated G(1) cell cycle arrest, respectively. By coupling the premature chromosome condensation technique to fluorescence in situ hybridization, we found no evidence of DNA damage after PALA treatment. We used representational difference analysis (cDNA-RDA) to study changes in gene expression after PALA treatment and gamma-radiation in normal human fibroblasts. The mammary-derived growth inhibitor (MDGI) gene was expressed in PALA-treated cells. Ectopic MDGI expression arrested PALA-treated but not irradiated RKO cells. Expression of an antisense RNA against MDGI resulted in…

Phosphonoacetic AcidCancer ResearchTumor suppressor geneIn situ hybridizationBiologyFatty Acid-Binding ProteinsCell LineGene expressionHumansGeneIn Situ Hybridization FluorescenceMetaphaseSkinExpressed Sequence TagsExpressed sequence tagAspartic AcidCell CycleG1 PhaseChromosome MappingG0 phaseGeneral MedicineCell cycleFibroblastsMolecular biologyGrowth InhibitorsGene Expression RegulationGamma RaysKaryotypingRepresentational difference analysisTumor Suppressor Protein p53Carrier ProteinsCell Adhesion MoleculesFatty Acid Binding Protein 3Chromosomes Human Pair 7Carcinogenesis
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AAV-Mediated Clarin-1 Expression in the Mouse Retina: Implications for USH3A Gene Therapy

2015

Usher syndrome type III (USH3A) is an autosomal recessive disorder caused by mutations in clarin-1 (CLRN1) gene, leading to progressive retinal degeneration and sensorineural deafness. Efforts to develop therapies for preventing photoreceptor cell loss are hampered by the lack of a retinal phenotype in the existing USH3 mouse models and by conflicting reports regarding the endogenous retinal localization of clarin-1, a transmembrane protein of unknown function. In this study, we used an AAV-based approach to express CLRN1 in the mouse retina in order to determine the pattern of its subcellular localization in different cell types. We found that all major classes of retinal cells express AAV…

Photoreceptors0301 basic medicineRetinal degenerationSensory ReceptorsPhysiologyUsher syndromeCell Membraneslcsh:MedicineSocial SciencesNervous SystemPhotoreceptor cellMicechemistry.chemical_compound0302 clinical medicineAnimal CellsMedicine and Health SciencesPsychologylcsh:ScienceNeuronsRegulation of gene expressionGeneticsMultidisciplinaryRetinal DegenerationAnimal ModelsDependovirusCell biologyElectrophysiologymedicine.anatomical_structureSensory PerceptionCellular TypesAnatomyCellular Structures and OrganellesUsher SyndromesResearch ArticleSignal TransductionCell typeImaging TechniquesOcular AnatomyNeurophysiologyOuter plexiform layerMouse ModelsBiologyResearch and Analysis MethodsRetina03 medical and health sciencesModel OrganismsOcular SystemFluorescence ImagingmedicineAnimalsHumansRetinalcsh:RMembrane ProteinsBiology and Life SciencesAfferent NeuronsRetinalGenetic TherapyCell Biologymedicine.diseaseDisease Models Animal030104 developmental biologyGene Expression RegulationchemistrySynapsesEyeslcsh:QHead030217 neurology & neurosurgeryNeurosciencePLOS ONE
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Functioning of DcuC as the C 4 -Dicarboxylate Carrier during Glucose Fermentation by Escherichia coli

1999

ABSTRACT The dcuC gene of Escherichia coli encodes an alternative C 4 -dicarboxylate carrier (DcuC) with low transport activity. The expression of dcuC was investigated. dcuC was expressed only under anaerobic conditions; nitrate and fumarate caused slight repression and stimulation of expression, respectively. Anaerobic induction depended mainly on the transcriptional regulator FNR. Fumarate stimulation was independent of the fumarate response regulator DcuR. The expression of dcuC was not significantly inhibited by glucose, assigning a role to DcuC during glucose fermentation. The inactivation of dcuC increased fumarate-succinate exchange and fumarate uptake by DcuA and DcuB, suggesting a…

Physiology and MetabolismMolecular Sequence DataMutantStimulationBiologymedicine.disease_causeMicrobiologyBacterial ProteinsFumaratesConsensus SequenceEscherichia colimedicineTranscriptional regulationDicarboxylic AcidsAnaerobiosisPromoter Regions GeneticMolecular BiologyEscherichia coliPsychological repressionDicarboxylic Acid TransportersBinding SitesBase SequenceEscherichia coli ProteinsSuccinatesGene Expression Regulation BacterialKineticsResponse regulatorGlucoseBiochemistryFermentationFermentationEffluxCarrier ProteinsRibosomesJournal of Bacteriology
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Regulation of aerobic and anaerobic D-malate metabolism of Escherichia coli by the LysR-type regulator DmlR (YeaT).

2010

ABSTRACT Escherichia coli K-12 is able to grow under aerobic conditions on d -malate using DctA for d -malate uptake and the d -malate dehydrogenase DmlA (formerly YeaU) for converting d -malate to pyruvate. Induction of dmlA encoding DmlA required an intact dmlR (formerly yeaT ) gene, which encodes DmlR, a LysR-type transcriptional regulator. Induction of dmlA by DmlR required the presence of d -malate or l - or meso -tartrate, but only d -malate supported aerobic growth. The regulator of general C 4 -dicarboxylate metabolism (DcuS-DcuR two-component system) had some effect on dmlA expression. The anaerobic l -tartrate regulator TtdR or the oxygen sensors ArcB-ArcA and FNR did not have a m…

Physiology and MetabolismRegulatorMalatesDehydrogenasemedicine.disease_causeMicrobiologyMalate dehydrogenaseMicrobiologyMalate DehydrogenasemedicineAnaerobiosisMolecular BiologyEscherichia coliTartratesChromatography High Pressure LiquidbiologyEscherichia coli K12Escherichia coli ProteinsMetabolismGene Expression Regulation Bacterialbiology.organism_classificationbeta-GalactosidaseAerobiosisBiochemistryMutationFermentationAnaerobic exerciseBacteriaJournal of bacteriology
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