Search results for "Drug effect"

showing 10 items of 70 documents

Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin

2014

We here report the synthesis of a series of 12 hybrid molecules composed of a colchicine moiety and a pironetin analogue fragment. The two fragments are connected through an ester-amide spacer of variable length. The cytotoxic activities of these compounds and their interactions with tubulin have been investigated. Relations between the structure and activity are discussed. Since the spacer is not long enough to permit a simultaneous binding of the hybrid molecules to the colchicine and pironetin sites on tubulin, a further feature investigated was whether these molecules would interact with the latter through the pironetin end (irreversible covalent binding) or through the colchicine end (…

StereochemistryChemical structureCellsFluorescent Antibody TechniqueAntineoplastic AgentsLigandsMicrotubulespironetinStructure-Activity Relationshipchemistry.chemical_compoundChemical structureTubulinNeoplasmsDrug DiscoveryTumor Cells CulturedHumansColchicineMoietyMoleculeStructure–activity relationshipBinding siteCell ProliferationPharmacologyBinding SitesDrug effectsMolecular StructurebiologyToxicityCell growthMoleculesTubulinchemistryPyronesDrug Designbiology.proteinMolecular MedicineColchicineJournal of Medicinal Chemistry
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D2R striatopallidal neurons inhibit both locomotor and drug reward processes.

2009

The specific functions of dopamine D(2) receptor-positive (D(2)R) striatopallidal neurons remain poorly understood. Using a genetic mouse model, we found that ablation of D(2)R neurons in the entire striatum induced hyperlocomotion, whereas ablation in the ventral striatum increased amphetamine conditioned place preference. Thus D(2)R striatopallidal neurons limit both locomotion and, unexpectedly, drug reinforcement.

Time FactorsstriatumParkinson's diseaseStriatumNeurons -- drug effectsEnkephalins -- metabolism10263 Institute of Experimental ImmunologyMiceDopamine Uptake InhibitorsTyrosine 3-Monooxygenase -- geneticsCorpus Striatum -- cytologyDiphtheria ToxinGlutamate Decarboxylase -- metabolismstriatum; indirect opathway; A2A receptors; D2 receptors; locomotion; amphetamine addiction; Parkinson's diseaseNeuronsamphetamine addictionGlutamate DecarboxylaseGeneral NeuroscienceAmphetamine -- pharmacologyNeurodegeneration2800 General NeuroscienceEnkephalinsSciences bio-médicales et agricoleslocomotionmedicine.anatomical_structureA2A receptorsIntercellular Signaling Peptides and ProteinsReceptors Dopamine D2 -- metabolismPsychologyLocomotionmedicine.drugHeparin-binding EGF-like Growth FactorProtein BindingGlobus Pallidus -- cytologyReceptors Dopamine D2 -- deficiencyReinforcement ScheduleTyrosine 3-MonooxygenaseGlutamate Decarboxylase -- geneticsLocomotion -- geneticsIntercellular Signaling Peptides and Proteins -- genetics610 Medicine & healthMice TransgenicNerve Tissue ProteinsDiphtheria Toxin -- pharmacologyGlobus PallidusNeurons -- physiologyLocomotion -- drug effectsRewardDopamineDopamine receptor D2medicineNerve Tissue Proteins -- metabolismAnimalsGene Expression Regulation -- geneticsAmphetamineD2 receptorsReceptors Adenosine A2Receptors Dopamine D2indirect opathwayVentral striatumReceptors Adenosine A2 -- geneticsDopamine Uptake Inhibitors -- pharmacologymedicine.diseaseConditioned place preferenceCorpus StriatumMice Inbred C57BLGene Expression Regulation -- drug effectsAmphetaminenervous systemGene Expression RegulationProtein Binding -- drug effectsTyrosine 3-Monooxygenase -- metabolism570 Life sciences; biologyAutoradiographyConditioning OperantNeuronConditioning Operant -- physiologyNeuroscienceEnkephalins -- geneticsNature neuroscience
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Characterization and DNA-binding properties of GRF, a novel monomeric binding orphan receptor related to GCNF and betaFTZ-F1

1999

0014-2956 (Print) Comparative Study Journal Article Research Support, Non-U.S. Gov't; A PCR approach has been used to isolate, from Bombyx mori, a cDNA encoding a novel orphan receptor (GRF) that is most closely related to Bombyx betaFTZ-F1 and to the vertebrate germ cell nuclear factor. The major GRF mRNA is detected in most tissues as an 8-kb transcript whose amount follows the circulating ecdysteroid concentration with a delay. The expression pattern of GRF is similar to that of the Bombyx homologue of the Drosophila early-late gene DHR3, and precedes that of betaFTZ-F1 in all stages and tissues examined. The GRF protein is thus likely to be required in many tissues, but in a temporally …

Transcription GeneticReceptors Cytoplasmic and NuclearFushi Tarazu Transcription FactorsSequence HomologyGenes InsectDevelopmental/drug effectsSteroidogenic Factor 1BiochemistryBombyx/*chemistry/growth & developmentDNA/*metabolismNuclear Receptor Subfamily 6 Group A Member 1ReceptorsCloning MolecularReceptorRegulation of gene expressionOrphan receptorbiologyGene Expression Regulation DevelopmentalDNA-Binding ProteinsEcdysterone/pharmacologyAmino AcidEcdysteroneInsect Proteins/genetics/*isolation & purification/metabolismInsect ProteinsRecombinant Fusion Proteins/metabolismTranscriptionProtein StructureRecombinant Fusion ProteinsGerm cell nuclear factorMolecular Sequence DataGeneticComplementary DNAAnimalsAmino Acid SequenceBinding siteBombyxHomeodomain ProteinsBinding Sitespurification/metabolismSequence Homology Amino AcidBase SequencefungiMolecularCytoplasmic and Nuclear/chemistryDNABombyxbiology.organism_classificationMolecular biologyProtein Structure TertiaryTranscription Factors/chemistry/genetics/*isolation &Nuclear receptorGene Expression RegulationGenesDNA-Binding Proteins/chemistry/genetics/*isolation &InsectSequence AlignmentTertiaryTranscription FactorsCloning
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Extrahepatic Morbidity and Mortality of Chronic Hepatitis C

2015

Chronic hepatitis C virus (HCV) infection is associated with several extra-hepatic manifestations. Patients with HCV may develop mixed cryoglobulinemia and its sequelae, ranging from cutaneous and visceral vasculitis to glomerulonephritis and B cell non-Hodgkin’s lymphoma. HCV-infected patients have increased rates of insulin resistance, diabetes and atherosclerosis, which may lead to increased cardiovascular morbidity and mortality. Neurologic manifestations of HCV infection include fatigue and cognitive impairment. The mechanisms causing the extra-hepatic effects of HCV infection are likely multifactorial and may include endocrine effects, HCV replication in extra-hepatic cells, or a heig…

VasculitisLymphomaGlomerulonephritis/epidemiology/virologyLymphoma/epidemiology/virologyHepatitis C virusAlpha interferonHepacivirusddc:616.07Cryoglobulinemia/epidemiology/virologymedicine.disease_causeAntiviral AgentsAntiviral Agents/administration & dosage/pharmacology/therapeutic useHepacivirus/drug effects/pathogenicityLiver diseasechemistry.chemical_compoundGlomerulonephritisDiabetes mellitusRibavirinmedicineHumansGlucose Metabolism Disorders/epidemiology/virologyInterferon alfaGlucose Metabolism Disordersddc:616Hepatologybusiness.industryHepatitis C Chronic/drug therapy/epidemiology/immunology/mortality/virologyRibavirinVasculitis/epidemiology/virologyGastroenterologyInterferon-alphavirus diseasesHepatitis C Chronicmedicine.diseaseCryoglobulinemiadigestive system diseasesCryoglobulinemiachemistryRibavirin/pharmacology/therapeutic useHCVImmunologyMorbiditybusinessVasculitisInterferon-alpha/pharmacology/therapeutic usemedicine.drugGastroenterology
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Effect of intravitreal injection of Indocyanine Green, Triamcinolone Acetonide and Trypan Blue on the electroretinographic response of rats

2007

International audience; Purpose:: Indocyanine Green (ICG) and Tripan Blue (TB) are commonly used in macular surgery by making easier the internal limiting membrane (ILM) removing. However, the innocuousness of these dyes is not actually established notably for ICG. Then, several authors proposed the use of triamcinolone acetonide (TA) as an alternative to the use of intraoperative dyes for visualizing the ILM. The purpose of this study was to evaluate the effects of intravitreal injection of ICG, TB and TA on the rat electroretinogram (ERG). Methods:: Three groups of 12-week-old Sprague Dawley rats (n=6) received intravitreal injection in one eye of 0.1mL of either ICG 0.5mg/mL, TB 3mg/mL o…

[SDV] Life Sciences [q-bio]retinagenetic structures[SPI.GPROC] Engineering Sciences [physics]/Chemical and Process Engineeringdrug effects[SDV]Life Sciences [q-bio][SDV.IDA]Life Sciences [q-bio]/Food engineering[SPI.GPROC]Engineering Sciences [physics]/Chemical and Process Engineeringsense organs[SDV.IDA] Life Sciences [q-bio]/Food engineeringelectroretinography: non-clinicaleye diseasesdrug toxicity
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Developmental profiles of epidermal mRNAs during the pupal-adult molt of Tenebrio molitor and isolation of a cDNA clone encoding an adult cuticular p…

1992

0012-1606 (Print) Journal Article; Changes in translatable mRNAs from the wing epidermis of the Coleoptera Tenebrio molitor have been investigated during metamorphosis by analysis of in vitro translated products. Striking differences between the patterns obtained from mRNAs extracted during pupal and adult cuticle secretion indicated that a drastic change in gene expression occurs during the pupal-adult transition. In addition to these stage-specific modifications, the mRNA patterns changed within each cuticular synthesis program (pupal or adult), especially at ecdysis. After tritiated leucine incorporation, some of the major radiolabeled cuticular proteins showed similar changes suggesting…

animal structuresPupa/drug effects/metabolismBiological/*geneticsBiologyMolting cycleWingDNA/*isolation & purificationJuvenile Hormones/*pharmacologyMessenger/*metabolismComplementary DNAGene expressionProtein biosynthesisWings AnimalAnimalsNorthern blotRNA MessengerTenebrioTenebrio/drug effects/*genetics/growth & developmentMolecular BiologyProteins/*geneticsDevelopmental profileMetamorphosisfungiMetamorphosis BiologicalPupaEpidermis/growth & developmentProteinsCell BiologyDNAMolecular biologyJuvenile HormonesEcdysisProtein BiosynthesisJuvenile hormoneInsect ProteinsRNAEpidermisDevelopmental Biology
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Diclofenac effects in sea urchin gametes and fertilization

2017

The drugs, agents for diseases therapy and prevention, are ubiquitous environmental pollutants. We analyzed a specific anti-inflammatory, diclofenac, present in soil and water. The study focused on Arbacia lixula (Linnaeus, 1758) and Paracentrotus lividus (Lamarck, 1816) reproductive success. In A. lixula we identified the drug qualitative and quantitative fertilization effects, and if they affect the functional male and female gametes capacity; in P. lividus we analyzed the drug effects and the male and female gametes quantitative integrity. Through the High Liquid Chromatografy we quantitatively evaluated the real diclofenac contribution on A. lixula embryos and on A. lixula and P. lividu…

diclofenacfertilizationspermatozoadrug effecteggSettore BIO/06 - Anatomia Comparata E Citologiasea urchin
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The NG2 Proteoglycan Protects Oligodendrocyte Precursor Cells against Oxidative Stress via Interaction with OMI/HtrA2.

2015

The NG2 proteoglycan is characteristically expressed by oligodendrocyte progenitor cells (OPC) and also by aggressive brain tumours highly resistant to chemo- and radiation therapy. Oligodendrocyte-lineage cells are particularly sensitive to stress resulting in cell death in white matter after hypoxic or ischemic insults of premature infants and destruction of OPC in some types of Multiple Sclerosis lesions. Here we show that the NG2 proteoglycan binds OMI/HtrA2, a mitochondrial serine protease which is released from damaged mitochondria into the cytosol in response to stress. In the cytosol, OMI/HtrA2 initiates apoptosis by proteolytic degradation of anti-apoptotic factors. OPC in which NG…

lcsh:MedicineApoptosisdrug effects [Cytosol]HTRA2 protein humangenetics [RNA Small Interfering]genetics [Serine Endopeptidases]genetics [Glioblastoma]570 Life sciencespathology [Glioblastoma]MiceCytosolCerebellumpathology [Cerebellum]RNA Small Interferinglcsh:Sciencemetabolism [Antigens]Mice Knockoutchondroitin sulfate proteoglycan 4metabolism [Proteoglycans]Brain NeoplasmsSerine Endopeptidasesdrug effects [Mitochondria]metabolism [Cerebellum]High-Temperature Requirement A Serine Peptidase 2Mitochondriametabolism [Brain Neoplasms]Gene Expression Regulation Neoplasticpharmacology [Antibodies Neutralizing]genetics [Mitochondrial Proteins]Proteoglycans570 BiowissenschaftenResearch ArticleProtein BindingSignal Transductionpathology [Brain Neoplasms]Primary Cell Culturedrug effects [Cerebellum]drug effects [Apoptosis]metabolism [Mitochondrial Proteins]Mitochondrial Proteinsantagonists & inhibitors [Proteoglycans]pharmacology [Hydrogen Peroxide]genetics [Antigens]Cell Line Tumormetabolism [Serine Endopeptidases]AnimalsHumansddc:610metabolism [RNA Small Interfering]Antigenslcsh:RHtra2 protein mouseHydrogen Peroxidemetabolism [Mitochondria]Antibodies Neutralizinggenetics [Proteoglycans]genetics [Brain Neoplasms]Mice Inbred C57BLOxidative Stressnervous systemlcsh:Qmetabolism [Cytosol]Glioblastomametabolism [Glioblastoma]
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Double copies of blaKPC-3::Tn4401a on an IncX3 plasmid in Klebsiella pneumoniae successful clone ST512 from Italy

2015

ABSTRACT A carbapenem-resistant sequence type 512 (ST512) Klebsiella pneumoniae carbapenemase 3 (KPC-3)-producing K. pneumoniae strain showing a novel variant plasmid content was isolated in Palermo, Italy, in 2014. ST512 is a worldwide successful clone associated with the spread of bla KPC genes located on the IncFIIk pKpQIL plasmid. In our ST512 strain, the bla KPC-3 gene was unusually located on an IncX3 plasmid, whose complete sequence was determined. Two copies of bla KPC-3 ::Tn 4401a caused by intramolecular transposition events were detected in the plasmid.

transposonsequence analysispolymerase chain reactionDrug ResistanceGene DosageSettore MED/42 - Igiene Generale E Applicatabacterial proteinbeta-Lactamaseopen reading framecarbapenemasePlasmidminocyclineplasmid DNAmeropenemPharmacology (medical)geneticscolistincefpodoximeceftazidime610 Medicine & healthCarbapenemBacterialpolymyxin Btimentingene expression regulationbacteriumKlebsiella pneumoniae carbapenemase 3 producing Klebsiella pneumoniae3. Good healthantiinfective agentmicrobial sensitivity testKlebsiella pneumoniaeItalypriority journaltigecyclineMultipleclone (Java method)cefotaxime030106 microbiologyKlebsiella pneumoniae carbapenemase 3tobramycinMicrobial Sensitivity Testsgentamicinpiperacillin plus tazobactamchemistryGene dosageArticleMicrobiology03 medical and health sciencesComplete sequenceClone CellOpen Reading FramesertapenemBacterial Proteinsmultidrug resistanceextensively drug resistant bacteriumAnti-Bacterial AgentcefepimePharmacologylevofloxacinmicrobiologycefoxitinbiochemical phenomena metabolism and nutritionbacterial infections and mycosesVirologyAnti-Bacterial Agents; Bacterial Proteins; Carbapenems; Clone Cells; Drug Resistance Multiple Bacterial; Gene Dosage; Italy; Klebsiella Infections; Klebsiella pneumoniae; Microbial Sensitivity Tests; Open Reading Frames; Plasmids; beta-Lactamases; DNA Transposable Elements; Gene Expression Regulation Bacterial; Pharmacology (medical); Pharmacology; Infectious Diseasesantibiotic sensitivityClone CellsKlebsiella InfectionsceftriaxoneCarbapenemsbacterial genetics0301 basic medicinemolecular cloningSettore MED/07 - Microbiologia E Microbiologia ClinicaKlebsiella pneumoniaeTransposition (music)Drug Resistance Multiple Bacterialpolycyclic compoundsgenetic screeningcell clonecarbapenem derivativeKlebsiella infectionunclassified drugAnti-Bacterial AgentsInfectious Diseasesbacterial genePlasmidsenzymologydoripenemBiologyminimum inhibitory concentrationbeta-Lactamasesbeta lactamaseMechanisms of ResistanceciprofloxacinAmikacin; aztreonam; carbapenemase; cefepime; cefotaxime; cefoxitin; cefpodoxime; ceftazidime; ceftriaxone; ciprofloxacin; colistin; cotrimoxazole; doripenem; doxycycline; ertapenem; gentamicin; imipenem; Klebsiella pneumoniae carbapenemase 3; levofloxacin; meropenem; minocycline; piperacillin plus tazobactam; plasmid DNA; polymyxin B; tigecycline; timentin; tobramycin; unclassified drug; antiinfective agent; bacterial protein; beta lactamase; carbapenem derivative; transposon antibiotic sensitivity; Article; bacterial gene; bacterial genetics; bacterial strain; bacterium; bacterium detection; bacterium isolation; Escherichia coli; extensively drug resistant bacterium; gene dosage; genetic screening; Italy; Klebsiella pneumoniae; Klebsiella pneumoniae carbapenemase 3 producing Klebsiella pneumoniae; minimum inhibitory concentration; molecular cloning; nonhuman; polymerase chain reaction; priority journal; sequence analysis; cell clone; chemistry; drug effects; enzymology; gene expression regulation; genetics; isolation and purification; Klebsiella infection; Klebsiella pneumoniae; metabolism; microbial sensitivity test; microbiology; multidrug resistance; open reading frame; plasmid; transposon Anti-Bacterial Agents; Bacterial Proteins; beta-Lactamases; Carbapenems; Clone Cells; DNA Transposable Elements; Drug Resistance Multiple Bacterial; Gene Dosage; Gene Expression Regulation Bacterial; Italy; Klebsiella Infections; Klebsiella pneumoniae; Microbial Sensitivity Tests; Open Reading Frames; Plasmidsplasmidbacterium isolationEscherichia coliGeneAmikacinbacterium detectionnonhumandoxycyclineisolation and purificationGene Expression Regulation Bacterialbiology.organism_classificationbacterial straincotrimoxazoleOpen reading frameDNA Transposable Elementdrug effectsDNA Transposable Elementsmetabolismaztreonamimipenem
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SV40 transformed fibroblasts recognize the same 140 kD fibronectin chemotactic fragment as non-transformed cells

1985

SV40-virus-transformed human embryonal fibroblasts show an enhanced chemotactic response to the glycoprotein fibronectin. However, they recognize the same chemotactic active region as non-transformed fibroblasts. The result suggests that an enhancement of chemotaxis by fibroblasts which have been transformed with Simian Virus 40 is due not to the utilization of further chemotactic domains in the molecule, but to an increased sensitivity of the cells to the chemoattractant.

virusesSimian virus 40BiologyVirus*Cell Transformation Viral Cells Cultured Chemotaxis/*drug effects Embryo Fibroblasts/physiology Fibronectins/*pharmacology Human Peptide Fragments/pharmacology Polyomavirus macacae/*physiologyCellular and Molecular NeurosciencemedicineHumansFibroblastMolecular BiologyCells CulturedPharmacologychemistry.chemical_classificationChemotaxisChemotaxisEmbryoCell BiologyFibroblastsCell Transformation ViralEmbryo MammalianVirologyPeptide FragmentsCell biologyFibronectinsSv40 virusFibronectinmedicine.anatomical_structurechemistryCell culturebiology.proteinMolecular MedicineGlycoprotein
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