Search results for "MICE"

showing 10 items of 6027 documents

Visualization of RNA-Quadruplexes in Live Cells

2015

Visualization of DNA and RNA quadruplex formation in human cells was demonstrated recently with different quadruplex-specific antibodies. Despite the significant interest in these immunodetection approaches, dynamic detection of quadruplex in live cells remains elusive. Here, we report on NaphthoTASQ (N-TASQ), a next-generation quadruplex ligand that acts as a multiphoton turn-on fluorescent probe. Single-step incubation of human and mouse cells with N-TASQ enables the direct detection of RNA-quadruplexes in untreated cells (no fixation, permeabilization or mounting steps), thus offering a unique, unbiased visualization of quadruplexes in live cells.

Static ElectricityMelanoma ExperimentalLigands010402 general chemistryG-quadruplex01 natural sciencesBiochemistryCatalysisMice03 medical and health scienceschemistry.chemical_compoundColloid and Surface ChemistryBiomimeticsCationsCell Line TumorFluorescence Resonance Energy TransferAnimalsHumans[CHIM]Chemical Sciences[SDV.BBM]Life Sciences [q-bio]/Biochemistry Molecular Biologyheterocyclic compoundsComputingMilieux_MISCELLANEOUSChelating AgentsFluorescent Dyes030304 developmental biologyPhotons[SDV.GEN]Life Sciences [q-bio]/Genetics0303 health sciencesbiologyChemistryRNADNAGeneral ChemistryFluorescenceMolecular biology3. Good health0104 chemical sciencesCell biologyVisualizationG-QuadruplexesFörster resonance energy transferMicroscopy FluorescenceCell cultureMCF-7 Cellsbiology.proteinRNAAntibodyDNAJournal of the American Chemical Society
researchProduct

Dilute and semi dilute solutions of block copolymers in water, near-critical and super-critical CO2: a small angle scattering study of the monomer–ag…

2002

Abstract Small angle neutron (SANS) and X-ray (SAXS) Scattering measurements on aggregate formation of block copolymers in water and in near-critical and supercritical CO2 are reported here. Time Resolved SAXS (TR-SAXS) has also been performed in the supercritical region. Experiments have been carried out for a series of different thermodynamic conditions, changing the solvent density by profiling the pressure at constant temperature. A sharp transition between monomers dissolved as random coils and micelles characterized by a solvo-philic shell and a solvo-phobic core occurs when the solvent density reaches the critical micellization value. This is easily shown in the case of scCO2.

Statistics and ProbabilityMaterials scienceSmall-angle X-ray scatteringScatteringAstrophysics::High Energy Astrophysical PhenomenaThermodynamicsCondensed Matter PhysicsMicelleSupercritical fluidCondensed Matter::Soft Condensed MatterCore (optical fiber)chemistry.chemical_compoundMonomerNuclear magnetic resonancechemistryCopolymerSmall-angle scatteringPhysica A: Statistical Mechanics and its Applications
researchProduct

On a set of data for the membrane potential in a neuron

2006

We consider a set of data where the membrane potential in a pyramidal neuron is measured almost continuously in time, under varying experimental conditions. We use nonparametric estimates for the diffusion coefficient and the drift in view to contribute to the discussion which type of diffusion process is suitable to model the membrane potential in a neuron (more exactly: in a particular type of neuron under particular experimental conditions).

Statistics and ProbabilityModels NeurologicalNeural ConductionAction PotentialsTetrodotoxinType (model theory)Statistics NonparametricGeneral Biochemistry Genetics and Molecular BiologyMembrane PotentialsSet (abstract data type)MiceStatisticsAnimalsDiffusion (business)MathematicsCerebral CortexNeuronsMembrane potentialStochastic ProcessesQuantitative Biology::Neurons and CognitionGeneral Immunology and MicrobiologyStochastic processPyramidal CellsApplied MathematicsNonparametric statisticsGeneral MedicineElectrophysiologyElectrophysiologynervous systemDiffusion processModeling and SimulationPotassiumGeneral Agricultural and Biological SciencesBiological systemAlgorithmsMathematical Biosciences
researchProduct

Acylated oleanane-type saponins from Ganophyllum giganteum

2014

Abstract Five oleanane-type saponins , 3- O -β- D -glucuronopyranosylzanhic acid 28- O -β- D -xylopyranosyl-(1→3)-[α- L -rhamnopyranosyl-(1→2)]-(4- O -acetyl)-β- D -fucopyranosyl ester ( 1 ), 3- O -β- D -glucopyranosylzanhic acid 28- O -β- D -xylopyranosyl-(1→3)-[α- L -rhamnopyranosyl-(1→2)]-(4- O -acetyl)-β- D -fucopyranosyl ester ( 2 ), zanhic acid 28- O -β- D -xylopyranosyl-(1→3)-[α- L -rhamnopyranosyl-(1→2)]-(4- O -acetyl)-β- D -fucopyranosyl ester ( 3 ), zanhic acid 28- O -α- L -rhamnopyranosyl-(1→2)-4- O -[(3′-hydroxy-2′-methyl-butyroyloxy)-3-hydroxy-2-methyl-butyroyloxy]-β- D -fucopyranosyl ester ( 4 ), medicagenic acid 28- O -α- L -rhamnopyranosyl-(1→2)-4- O -[(3′-hydroxy-2′-methyl-…

StereochemistryAcylationMolecular ConformationPlant ScienceHorticulturePlant RootsBiochemistryMiceStructure-Activity Relationshipchemistry.chemical_compoundSapindaceaeCell Line TumorAnimalsHumansOrganic chemistryMoietyOleanolic AcidMolecular BiologyOleananeCell ProliferationInflammationBiological ProductsDose-Response Relationship DrugChemistryHydrolysisAnti-Inflammatory Agents Non-SteroidalGeneral MedicineSaponinsAntineoplastic Agents PhytogenicMedicagenic acidDoratoxyleaeDrug Screening Assays AntitumorPhytochemistry
researchProduct

Synthesis and biological evaluation of 2- and 3-aminobenzo[b]thiophene derivatives as antimitotic agents and inhibitors of tubulin polymerization.

2007

Two new series of inhibitors of tubulin polymerization based on the 2-amino-3-(3,4,5-trimethoxybenzoyl)benzo[b]thiophene molecular skeleton and its 3-amino positional isomer were synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization, and cell cycle effects. Although many more 3-amino derivatives have been synthesized so far, the most promising compound in this series was 2-amino-6-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]thiophene, which inhibits cancer cell growth at subnanomolar concentrations and interacts strongly with tubulin by binding to the colchicine site.

StereochemistryAntimitotic Agents/chemistry Antimitotic Agents/pharmacologymacromolecular substancesThiophenesAntimitotic AgentsChemical synthesischemistry.chemical_compoundMiceRadioligand AssayStructure-Activity RelationshipTubulinCell Line TumorDrug DiscoveryThiopheneStructure–activity relationshipAnimalsHumansCytotoxicityCell ProliferationBinding SitesbiologyBicyclic moleculeChemistryTubulin ModulatorsCell CycleTubulin ModulatorsTubulinbiology.proteinMolecular MedicineAntimitotic AgentDrug Screening Assays AntitumorColchicineProtein BindingJournal of medicinal chemistry
researchProduct

N-Heterocyclic choline analogues based on 1,2,3,4-tetrahydro(iso)quinoline scaffold with anticancer and anti-infective dual action

2016

Pharmacological effects of biologically active “small molecules” can be improved by their targeted modification, which affects drug delivery and interaction with tumor cells and microorganisms. We aimed to evaluate anticancer and antimicrobial activity of lipid-like choline derivatives modified via simultaneous introduction of tetrahydro(iso)quinoline based pharmacophore system at nitrogen atom and long chain alkyl substituent at oxygen atom. Target compounds were synthesized under phase-transfer catalysis conditions followed by quaternization, and evaluated for cytotoxicity and NO-generation ability on HT-1080 and MG-22A tumor cell lines and NIH 3T3 normal mouse fibroblasts, and screened f…

StereochemistryAntineoplastic AgentsMicrobial Sensitivity TestsGram-Positive Bacteriamedicine.disease_cause01 natural sciencesDNA gyraseCholineInhibitory Concentration 50Mice03 medical and health scienceschemistry.chemical_compoundDrug Delivery Systems0302 clinical medicineAnti-Infective AgentsCell Line TumorNeoplasmsGram-Negative BacteriamedicineAnimalsHumansCytotoxicityEscherichia coliPharmacologybiology010405 organic chemistryQuinolineFungiBiological activityGeneral MedicineAntimicrobialbiology.organism_classificationProteus mirabilis0104 chemical scienceschemistry030220 oncology & carcinogenesisNIH 3T3 CellsQuinolinesAntibacterial activityPharmacological Reports
researchProduct

Comparing the Antileishmanial Activity of Gold(I) and Gold(III) Compounds in L. amazonensis and L. braziliensis in Vitro

2020

Abstract Abstract: A series of mononuclear coordination or organometallic AuI/AuIII complexes (1–9) have been comparatively studied in vitro for their antileishmanial activity against promastigotes and amastigotes, the clinically relevant parasite form, of Leishmania amazonensis and Leishmania braziliensis. One of the cationic AuI bis‐N‐heterocyclic carbenes (3) has low EC50 values (ca. 4 μM) in promastigotes cells and no toxicity in host macrophages. Together with two other AuIII complexes (6 and 7), the compound is also extremely effective in intracellular amastigotes from L. amazonensis. Initial mechanistic studies include an evaluation of the gold complexes′ effect on L. amazonensis’ pl…

StereochemistryAntiprotozoal Agentsamastigotes01 natural sciencesBiochemistryMiceGold iiiParasitic Sensitivity TestsGold CompoundsDrug Discoverygold compoundsmedicineAnimalsGeneral Pharmacology Toxicology and PharmaceuticsAmastigoteleishmaniasisCells CulturedEC50LeishmaniaPharmacologyMice Inbred BALB CMolecular Structurebiology010405 organic chemistryChemistryCommunicationOrganic ChemistryLeishmaniasismedicine.diseasebiology.organism_classificationLeishmania braziliensisCommunicationsIn vitroddc:0104 chemical sciences010404 medicinal & biomolecular chemistryMolecular MedicinepromastigotesOrganogold CompoundsIntracellularChemMedChem
researchProduct

Interface charge density matching as driving force for new mesostructured oxovanadium phosphates with hexagonal structure, [CTA]xVOPO4·zH2O

1999

Hexagonal mesostructured mixed-valence oxovanadium phosphates [CTA]xVOPO4·zH2O, in short ICMUV-2, have been synthesized through a S+I- cooperative mechanism using cationic surfactant (cetyltrimethylammonium, CTAB) rodlike micelles as a template. On the lines of the hypothesis that the driving force leading to the formation of mesostructured solids is the charge density matching at the interface between the supramolecular−organic and supramolecular−inorganic moieties, the self-assembling process between CTA+ micelles and VOPO4q- planar anions can be thought of as consequence of the adequate adjustment of the metal mean oxidation state. X-ray powder diffraction and TEM techniques show that th…

StereochemistryChemistryGeneral Chemical EngineeringCharge densityGeneral ChemistryMicelleMetalCrystallographyOxidation statevisual_artX-ray crystallographyMaterials Chemistryvisual_art.visual_art_mediumMesoporous materialHydratePowder diffraction
researchProduct

Crystallization and preliminary X-ray studies of mouse centrin1.

2005

The expression, purification, crystallization and preliminary X-ray diffraction studies of mouse centrin1 are reported. Centrins belong to a family of Ca{sup 2+}-binding EF-hand proteins that play a fundamental role in centrosome duplication and the function of cilia. To shed light on the structure–function relationship of these proteins, mouse centrin1 has been crystallized. The mouse centrin1 has been expressed in Escherichia coli as a GST-centrin fusion protein containing a thrombin protease cleavage site between the fusion partners. Two constructs with different linking-sequence lengths were expressed and purified. Thrombin cleavage yielded functional centrin1 and N-terminally extended …

StereochemistryChromosomal Proteins Non-HistoneMolecular Sequence DataBiophysicsmacromolecular substancesCleavage (embryo)Crystallography X-RayBiochemistrylaw.inventionchemistry.chemical_compoundMiceStructure-Activity RelationshipThrombinStructural BiologylawGeneticsmedicineEscherichia coliAnimalsCentrosome duplicationAmino Acid SequenceCrystallizationDose-Response Relationship DrugCalcium-Binding ProteinsSpace groupCondensed Matter PhysicsFusion proteinRecombinant ProteinsCrystallographyenzymes and coenzymes (carbohydrates)KineticschemistryCrystallization CommunicationsX-ray crystallographybiological scienceshealth occupationsbacteriaCrystallizationEthylene glycolmedicine.drugActa crystallographica. Section F, Structural biology and crystallization communications
researchProduct

In vivo and in vitro anti-leishmanial activities of 4-nitro-N-pyrimidin- and N-pyrazin-2-ylbenzenesulfonamides, and N2-(4-nitrophenyl)-N1-propylglyci…

2009

A series of compounds containing the nitrobenzene and sulfonamido moieties were synthesized and their leishmanicidal effect was assessed in vitro against Leishmania infantum promastigotes. Among the compounds evaluated, the p-nitrobenzenesulfonamides 4Aa and 4Ba, and the p-nitroaniline 5 showed significant activity with a good selectivity index. In a Balb/c mice model of L. Infantum, administration of compounds 4Aa, 4Ba or 5 (5 mg/kg/day for 10 days, injected ip route) led to a clear-cut parasite burden reduction (ca. 99%). In an attempt to elucidate their mechanism of action, the DNA interaction of 4Aa and 5 was investigated by means of viscosity studies, thermal denaturation and nuclease …

StereochemistryClinical BiochemistryNitro compoundGlycinePharmaceutical ScienceBiochemistryChemical synthesisMiceIn vivoDrug DiscoverymedicineAnimalsMolecular BiologyLeishmaniasischemistry.chemical_classificationNucleaseMice Inbred BALB CSulfonamidesAniline CompoundsbiologyOrganic Chemistrybiology.organism_classificationTrypanocidal AgentsIn vitroPyrimidineschemistryMechanism of actionBiochemistrybiology.proteinNitroMolecular MedicineLeishmania infantummedicine.symptomBioorganicmedicinal chemistry
researchProduct