Search results for "Specific activity"

showing 10 items of 35 documents

Effect of a dominant-negative form of ADAM10 in a mouse model of Alzheimer's disease.

2009

The alpha-secretase cleaves in the non-amyloidogenic pathway the amyloid-beta protein precursor (AbetaPP) within the region of the amyloid-beta peptides to prevent their formation and aggregation in the brain. Members of the ADAM family (a disintegrin and metalloprotease) are the main candidates for physiologically relevant alpha-secretases. We recently demonstrated that overexpression of ADAM10 in mice transgenic for human AbetaPP (ADAM10 x APP[V717I]) alleviated functional deficits related to Alzheimer's disease. To further demonstrate that this is due to the specific activity of alpha-secretase, we characterized mice overexpressing an inactive form of ADAM10 (ADAM10[E384A]; ADAM10-dn). T…

ADAM10Morris water navigation taskGlutamic AcidStimulationMice TransgenicADAM10 ProteinAmyloid beta-Protein PrecursorMiceIn vivoAlzheimer DiseaseDisintegrinReaction TimeAnimalsHumansIsoleucineProtein precursorMaze LearningSwimmingMetalloproteinaseAlaninebiologyBehavior AnimalChemistryGeneral NeuroscienceAge FactorsMembrane ProteinsValineGeneral MedicineCell biologyMice Inbred C57BLPsychiatry and Mental healthClinical PsychologyADAM ProteinsDisease Models Animalbiology.proteinSpecific activityGeriatrics and GerontologyAmyloid Precursor Protein SecretasesJournal of Alzheimer's disease : JAD
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Dibutyryl cyclic AMP and adrenaline increase contractile force and 45Ca uptake in mammalian cardiac muscle

1973

The effects of dibutyryl cyclic AMP (DB-AMP; 10−3M) and adrenaline (2.2×10−6 M) on contractile force, 45Ca uptake, and total myocardial Ca concentration were investigated in electrically driven left auricles isolated from rat hearts. The experiments were performed at an extracellular Ca concentration of 0.45 mM and at low frequency of stimulation (15 beats/min). 45Ca exposure was 5 min. Under the conditions used, both drugs increased contractile force and enhanced 45Ca uptake (expressed as relative specific activity) by about 30% (DB-AMP) and 40% (adrenaline), respectively. Thus, the results provide evidence that the effects of adrenaline on 45Ca uptake in mammalian cardiac muscle can be mi…

Calcium Isotopesmedicine.medical_specialtyContraction (grammar)Epinephrinechemistry.chemical_elementStimulationIn Vitro TechniquesCalciumInternal medicineCyclic AMPmedicineExtracellularAnimalsCa uptakeCardiac OutputPharmacologyMyocardiumCardiac muscleHeartGeneral MedicineDibutyryl Cyclic AMPRatsEndocrinologymedicine.anatomical_structurechemistryCalciumFemaleSpecific activityNaunyn-Schmiedeberg's Archives of Pharmacology
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Labeling and preliminary in vivo assessment of niobium-labeled radioactive species: A proof-of-concept study.

2016

Abstract The application of radionuclide-labeled biomolecules such as monoclonal antibodies or antibody fragments for imaging purposes is called immunoscintigraphy . More specifically, when the nuclides used are positron emitters, such as zirconium-89, the technique is referred to as immuno-PET . Currently, there is an urgent need for radionuclides with a half-life which correlates well with the biological kinetics of the biomolecules under question and which can be attached to the proteins by robust labeling chemistry. 90 Nb is a promising candidate for in vivo immuno-PET , due its half-life of 14.6h and low β + energy of E mean =0.35MeV per decay. 95 Nb on the other hand, is a convenient …

Cancer ResearchPathologymedicine.medical_specialtyBiodistributionmedicine.drug_classMetaboliteNiobiumDeferoxamineMonoclonal antibody030218 nuclear medicine & medical imagingImmunoscintigraphy03 medical and health scienceschemistry.chemical_compoundMice0302 clinical medicineChloridesDrug StabilityIn vivomedicineAnimalsRadiology Nuclear Medicine and imagingTissue DistributionRadioisotopesOxalatesChemistryIn vitroBevacizumab030220 oncology & carcinogenesisIsotope LabelingPositron-Emission TomographyBiophysicsMolecular MedicineSpecific activityFemaleEx vivoHalf-LifeNuclear medicine and biology
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Glycogen phosphorylase in fish muscle: demonstration of three interconvertible forms

1990

White skeletal muscle of crucian carp contains a single isoenzyme of glycogen phosphorylase, which was purified approximately 300-fold to a specific activity of approximately 13 mumol.min-1.mg protein-1 (assayed in the direction of glycogen breakdown at 25 degrees C). Tissue extracts of crucian muscle produced three distinct peaks of phosphorylase activity when separated on DEAE-Sephacel. Peaks 1 and 3 were identified, in terms of kinetic properties and by interconversion experiments, as phosphorylase b and a, respectively. Peak 2 was shown to be a phospho-dephospho hybrid. The three interconvertible forms of phosphorylase were purified and shown to be dimeric molecules at 20 degrees C. At …

CarpsPhosphorylasesPhysiologyPhysical ExertionAnesthesia GeneralIsozymeChromatography AffinityGlycogen phosphorylasemedicineAnimalsPhosphorylase aPhosphorylase bPhosphorylationGel electrophoresischemistry.chemical_classificationbiologyChemistryMusclesSkeletal muscleCell BiologyChromatography Ion Exchangebiology.organism_classificationIsoenzymesKineticsmedicine.anatomical_structureEnzymeBiochemistryCrucian carpPhosphorylationSpecific activityAmerican Journal of Physiology-Cell Physiology
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Phosphatidylinositol specific phospholipase C of plant stems : membrane associated activity concentrated in plasma membranes.

1987

A phosphatidylinositol-specific phospholipase C of plant stems (EC 3.1.4.10) assayed at pH 6.6 and at 30 degrees C cleaved phosphatidylinositol such that more than 85% of the product was inositol-1-phosphate. Other phospholipids were cleaved 5 to 10% or less under these conditions. The phospholipase had both a soluble and a membrane-associated form. The soluble activity accounted for approximately 85 to 90% of the activity and 15% was associated with membranes. The membrane-associated activity was most concentrated in the plasma membranes of hypocotyl segments of both soybean (Glycine max) and bushbean (Phaseolus vulgaris). The plasma membrane location was verified by analysis of highly pur…

ChromatographyCalmodulinbiologyPhospholipase CPhysiologychemistry.chemical_elementPlant ScienceCalciumPhospholipasechemistry.chemical_compoundMembranechemistryBiochemistryDevelopment and Growth RegulationGlycineGeneticsbiology.proteinSpecific activityPhosphatidylinositolPlant physiology
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Fusarium proliferatum: induction and intracellular location of a lipoxygenase

1998

The fungus Fusarium proliferatum was grown in a soya oil- and glucose-supplemented medium. Induction of lipoxygenase activity (13-fold) in an extract of Fusarium biomass has been observed at day four on soya oil culture medium. A band at 232 kDa was detected using a specific lipoxygenase stain combined with native PAGE. The method of fungal homogenate obtained has been checked via subcellular marker enzymes activities: succinate dehydrogenase (SDH) for mitochondrial fraction and NADH-cytochrome C reductase (NADH-cyt. C) for the microsomal fraction. Protoplasts production and disintegration followed by subcellular fractionation using differential centrifugation was the best method to recover…

Differential centrifugationFusariumSuccinate dehydrogenasefood and beveragesFusarium proliferatumBioengineeringBiologyReductasebiology.organism_classificationApplied Microbiology and BiotechnologyBiochemistryLipoxygenaseBiochemistrybiology.proteinSpecific activityCell fractionationBiotechnologyEnzyme and Microbial Technology
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Specificity of mouse liver cytosolic epoxide hydrolase for K-region epoxides derived from polycyclic aromatic hydrocarbons

1980

Mouse liver cytosol epoxide hydrolase, known to be very active for certain alkene oxides, had a specific activity which was 2.1-, 11- and 160-fold lower than that of the microsomal epoxide hydrolase for the arene oxides 7-methylbenz[a]anthracene 5,6-oxide, benz[a]anthracene 5,6-oxide and phenanthrene 9,10-oxide, respectively. For benzo[a]pyrene 4,5-oxide no activity (less than 10 pmol product/mg protein/min) of cytoplasmic epoxide hydrolase was detectable. The specific activity of cytoplasmic epoxide hydrolase was much lower for all K-region epoxides investigated, compared to trans-stilbene oxide used as a positive control and for which a new assay is described. It is concluded from these r…

Epoxide HydrolasesMaleEpoxide hydrolase 2Cancer ResearchAnthracenePhenanthrenesSubstrate SpecificityMicechemistry.chemical_compoundCytosolLiverOncologychemistryBiochemistryEthers CyclicMicrosomal epoxide hydrolaseHydrolaseBenz(a)AnthracenesMicrosomes LiverMicrosomeAnimalsEpoxy CompoundsPyreneSpecific activityEpoxide hydrolaseCancer Letters
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Rat Cytosolic Epoxide Hydrolase

1986

Rat liver microsomal and cytosolic epoxide hydrolase may be distinguished through differences in substrate specificity: styrene 7,8-oxide is preferentially hydrolyzed by the microsomal form, while trans-stilbene oxide is the prefered substrate for cytosolic epoxide hydrolase. Large interindividual differences in the specific activity of SpragueDawley (outbred strain) liver cytosolic epoxide hydrolase were observed, varying from 2 to 77 pmol/min x mg protein. Interindividual variations were much lower for microsomal epoxide hydrolase. The specific activity of Fischer F-344 (inbred strain) liver cytosolic epoxide hydrolase varied only by a factor of 2. The specific activity of cytosolic epoxi…

Epoxide hydrolase 2chemistry.chemical_compoundClofibratechemistryTiadenolBiochemistryMicrosomal epoxide hydrolaseStyrene oxidemedicineMicrosomeSpecific activityEpoxide hydrolasemedicine.drug
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Total synthesis and evaluation of [18F]MHMZ.

2007

Radiochemical labeling of MDL 105725 using the secondary labeling precursor 2-[(18)F]fluoroethyltosylate ([(18)F]FETos) was carried out in yields of approximately 90% synthesizing [(18)F]MHMZ in a specific activity of approximately 50MBq/nmol with a starting activity of approximately 3GBq. Overall radiochemical yield including [(18)F]FETos synthon synthesis, [(18)F]fluoroalkylation and preparing the injectable [(18)F]MHMZ solution was 42% within a synthesis time of approximately 100 min. The novel compound showed excellent specific binding to the 5-HT(2A) receptor (K(i)=9.0 nM) in vitro and promising in vivo characteristics.

Fluorine RadioisotopesStereochemistryClinical BiochemistryPharmaceutical ScienceBiochemistryBinding CompetitiveRadioligand AssayPiperidinesIn vivoDrug DiscoveryAnimalsRadionuclide imagingReceptor Serotonin 5-HT2ARadionuclide ImagingMolecular BiologyChemistryOrganic ChemistrySynthonTotal synthesisBrainBiological activityRadioligand AssayRatsFluorobenzenesKineticsYield (chemistry)Isotope LabelingSerotonin 5-HT2 Receptor AntagonistsMolecular MedicineSpecific activityKetanserinSerotonin AntagonistsRadiopharmaceuticalsNuclear chemistryBioorganicmedicinal chemistry letters
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Stabilisation of mixed peptide/lipid complexes in selective antifungal hexapeptides

2004

AbstractThe design of antimicrobial peptides could have benefited from structural studies of known peptides having specific activity against targetmicrobes, but not toward other microorganisms. We have previously reported the identification of a series of peptides (PAF-series) activeagainst certain postharvest fungal phytopathogens, and devoid of toxicity towards E. coli and S. cerevisiae [Lo´pez-Garci´a et al. Appl.Environ. Microbiol. 68 (2002) 2453]. The peptides inhibited the conidia germination and hyphal growth. Here, we present a comparativestructural characterisation of selected PAF peptides obtained by single-amino-acid replacement, which differ in biological activity. Thepeptides w…

Hyphal growthCircular dichroismAntifungal AgentsProtein ConformationStereochemistryFungicideAntimicrobial peptidesBiophysicsPeptideMicrobial Sensitivity TestsBiochemistryMembrane LipidsmedicinePostharvestMicelleschemistry.chemical_classificationMembranesCircular DichroismBiological activityCell BiologyPlantsSpectrometry FluorescenceConformational analysisMembraneEnergy TransferMechanism of actionBiochemistrychemistryDrug DesignSpecific activitymedicine.symptomAntimicrobial peptidePeptide–lipid interactionOligopeptidesBiochimica et Biophysica Acta (BBA) - Biomembranes
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