Search results for "Fluorescence anisotropy"

showing 6 items of 16 documents

Molecular topology applied to the discovery of 1-benzyl-2-(3-fluorophenyl)-4-hydroxy-3-(3-phenylpropanoyl)-2H-pyrrole-5-one as a non-ligand-binding-p…

2014

We report the discovery of 1-benzyl-2-(3- fluorophenyl)-4-hydroxy-3-(3-phenylpropanoyl)-2H-pyrrole- 5-one as a novel non-ligand binding pocket (non-LBP) antagonist of the androgen receptor (AR) through the application of molecular topology techniques. This compound, validated through time-resolved fluorescence resonance energy transfer and fluorescence polarization biological assays, provides the basis for lead optimization and structure−activity relationship analysis of a new series of non-LBP AR antagonists. Induced-fit docking and molecular dynamics studies have been performed to establish a consistent hypothesis for the interaction of the new active molecule on the AR surface. Refereed/…

StereochemistryGeneral Chemical EngineeringMolecular ConformationLibrary and Information SciencesMolecular Dynamics Simulationmolecular topologySmall Molecule LibrariesMolecular dynamicschemistry.chemical_compoundStructure-Activity RelationshipUser-Computer Interfaceexperimental validationDrug DiscoveryFluorescence Resonance Energy TransferMoleculeHumansPyrrolesPyrroleBinding SitesChemistryAntagonistAndrogen AntagonistsGeneral Chemistryvirtual screeningComputer Science ApplicationsHigh-Throughput Screening AssaysAndrogen receptorMolecular Docking SimulationFörster resonance energy transferDocking (molecular)Receptors AndrogenThermodynamicsFluorescence anisotropyProtein Binding
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Membrane fluidity of stressed cells of Oenococcus oeni

2000

International audience; The determination of membrane fluidity in whole cells of Oenococcus oeni was achieved by membrane probe 1,6-diphenyl-1,3,5-hexatriene fluorescence anisotropy measurements. The results demonstrated instantaneous fluidity variations with cells directly stressed during the measure. Heat (42°C) or acid (pH 3.2) shocks decreased the anisotropy values (fluidising effects), whereas an ethanol shock (10% ethanol, v/v) increased the membrane rigidity. The velocities of fluidity variation with non-adapted or adapted cells (incubation in inhibitory growth conditions) were compared. The adaptation of the cells to acid conditions had no effect on the membrane fluidity variation a…

Thermal shockStress toleranceMicrobiologychemistry.chemical_compoundMembrane fluiditymedicine[SPI.GPROC]Engineering Sciences [physics]/Chemical and Process EngineeringMembrane fluidityIncubationOenococcus oeniEthanolbiologyEthanolGeneral MedicineHydrogen-Ion Concentrationbiology.organism_classificationAdaptation PhysiologicalGram-Positive CocciMembranechemistryBiochemistryShock (circulatory)Biophysicsmedicine.symptomOenococcus oeniFluorescence labellingFluorescence anisotropyLeuconostocFood Science
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Cholesterol Modulates the Interaction of β-Amyloid Peptide with Lipid Bilayers

2009

The interaction of an amphiphilic, 40-amino acid beta-amyloid (Abeta) peptide with liposomal membranes as a function of sterol mole fraction (X(sterol)) was studied based on the fluorescence anisotropy of a site-specific membrane sterol probe, dehydroergosterol (DHE), and fluorescence resonance energy transfer (FRET) from the native Tyr-10 residue of Abeta to DHE. Without Abeta, peaks or kinks in the DHE anisotropy versus X(sterol) plot were detected at X(sterol) approximately 0.25, 0.33, and 0.53. Monomeric Abeta preserved these peaks/kinks, but oligomeric Abeta suppressed them and created a new DHE anisotropy peak at X(sterol) approximately 0.38. The above critical X(sterol) values coinci…

Time FactorsLipid BilayersMolecular Sequence DataBiophysicsPeptideFluorescence Polarization7. Clean energy03 medical and health scienceschemistry.chemical_compound0302 clinical medicineAlzheimer DiseaseErgosterolFluorescence Resonance Energy TransferAmino Acid SequenceLipid bilayer030304 developmental biologychemistry.chemical_classification0303 health sciencesLiposomeAmyloid beta-PeptidesChemistryCholesterolSterolPeptide FragmentsCrystallographyFörster resonance energy transferMembraneCholesterolCell BiophysicsTyrosinelipids (amino acids peptides and proteins)030217 neurology & neurosurgeryFluorescence anisotropyProtein BindingBiophysical Journal
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Use of the Transglutaminase Reaction To Study the Dissociation of Histone N-Terminal Tails from DNA in Nucleosome Core Particles

1997

We have recently shown that core histones are glutaminyl substrates for transglutaminase (TGase) and that when native nucleosome cores are incubated with monodansylcadaverine (DNC) as donor amine, this fluorescent probe is incorporated into Gln5 and Gln19 of H3 and in Gln22 of H2B [Ballestar et al. (1996) J. Biol. Chem. 271, 18817-18825]. In the present paper, we report that the cause by which Gln22 of H2B is modified in nucleosomes but not in the free histone is the interaction of the region containing that glutamine with DNA. We have used the specificity of the TGase reaction to study the changes induced by increasing ionic strength in the interaction between the histone N-terminal tails …

TransglutaminasesbiologyMovementOsmolar ConcentrationFluorescence PolarizationDNABiochemistryLinker DNAMolecular biologyNucleosomesHistoneschemistry.chemical_compoundHistoneModels ChemicalchemistryIonic strengthCadaverineChromatosomeBiophysicsbiology.proteinNucleosomeHistone octamerFluorescence anisotropyDNABiochemistry
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Ultrafast Dynamics of Dansylated POPAM Dendrimers and Energy Transfer in their Dye Complexes

2009

We have studied internal dynamics of dansylated poly(propyleneamine) dendrimers of different generations in solution and excitation energy transfer from dansyl chromophores to xanthene dyes that form van der Waals complexes with the dendrimers

XantheneChemistryDynamics (mechanics)Chromophoresymbols.namesakechemistry.chemical_compoundChemical physicsComputational chemistryDendrimersymbolsvan der Waals forceUltrashort pulseFluorescence anisotropyExcitation
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Micelles as containers for self-assembled nanodevices: a fluorescent sensor for lipophilicity

2008

Potentiometric titrations, fluorescence versus pH titrations, dynamic light scattering and fluorescence polarization anisotropy studies demonstrate that inside the nanodimensioned Triton X-100 micelles, 1-pyrenecarboxylic acid, PCOO-, forms an apical complex with the Zn2+ cation encircled by a lipophilic cyclen ligand and hugely increasing its fluorescence. The ability of the Zn2+-cyclen-PCOO- complex plus its micellar container to act as a fluorescent sensor to evaluate the lipophilicity of molecular species is demonstrated on the fatty acid series CH 3(CH2)xCOOH (x=0-16). At pH 7.4 a decrease in fluorescence is observed on the addition of fatty acids that is directly related to their chai…

chemistry.chemical_classification010405 organic chemistryChemistryStereochemistryInorganic chemistryFatty acidmicelles light scattering pH fluorescence010402 general chemistry01 natural sciencesFluorescenceMicelleAtomic and Molecular Physics and Optics3. Good health0104 chemical sciences[CHIM.THEO]Chemical Sciences/Theoretical and/or physical chemistrychemistry.chemical_compoundCyclenLipophilicity[ CHIM.THEO ] Chemical Sciences/Theoretical and/or physical chemistryTitrationPhysical and Theoretical ChemistryApical complexFluorescence anisotropyComputingMilieux_MISCELLANEOUS
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