Search results for " ALPHA"

showing 10 items of 1610 documents

A Molecular Dynamics-Shared Pharmacophore Approach to Boost Early-Enrichment Virtual Screening: A Case Study on Peroxisome Proliferator-Activated Rec…

2016

Molecular dynamics (MD) simulations can be used, prior to virtual screening, to add flexibility to proteins and study them in a dynamic way. Furthermore, the use of multiple crystal structures of the same protein containing different co-crystallized ligands can help elucidate the role of the ligand on a protein's active conformation, and then explore the most common interactions between small molecules and the receptor. In this work, we evaluated the contribution of the combined use of MD on crystal structures containing the same protein but different ligands to examine the crucial ligand-protein interactions within the complexes. The study was carried out on peroxisome proliferator-activat…

Virtual screening0301 basic medicinePeroxisome proliferator-activated receptorComputational biologyMolecular Dynamics SimulationCrystallography X-RayLigandsPPARα01 natural sciencesBiochemistryDrug design03 medical and health sciencesMolecular dynamics0103 physical sciencesDrug DiscoveryHumansPPAR alphaGeneral Pharmacology Toxicology and PharmaceuticsPharmacologychemistry.chemical_classificationVirtual screeningBinding Sites010304 chemical physicsLigandOrganic ChemistryDynamic pharmacophoreSmall moleculeProtein Structure TertiaryMolecular Docking Simulation030104 developmental biologyROC CurvechemistryDocking (molecular)Area Under CurvePharmacology Toxicology and Pharmaceutics (all)Molecular dockingMolecular MedicinePeroxisome proliferator-activated receptor alphaPharmacophoreProtein BindingChemMedChem
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Hypoxia Positively Regulates the Expression of pH-Sensing G-Protein–Coupled Receptor OGR1 (GPR68)

2016

Background & Aims: A novel family of proton-sensing G-proteinâcoupled receptors, including ovarian cancer G-proteinâcoupled receptor 1 (OGR1) (GPR68) has been identified to play a role in pH homeostasis. Hypoxia is known to change tissue pH as a result of anaerobic glucose metabolism through the stabilization of hypoxia-inducible factor-1α. We investigated how hypoxia regulates the expression of OGR1 in the intestinal mucosa and associated cells. Methods: OGR1 expression in murine tumors, human colonic tissue, and myeloid cells was determined by quantitative reverse-transcription polymerase chain reaction. The influence of hypoxia on OGR1 expression was studied in monocytes/macrophages and…

WT wild type0301 basic medicineMM6 MonoMac 6HV healthy volunteerSPARC secreted protein acidic and rich in cysteineNF-κB nuclear factor-κBInflammationBiologyIEC intestinal epithelial cell03 medical and health sciencesIntestinal mucosaTDAG8Ovarian Cancer G-Protein–Coupled ReceptormedicineOGR1 ovarian cancer G-protein–coupled receptor 1 (GPR68)IFN interferonlcsh:RC799-869ReceptorOriginal ResearchTh T-helperInflammationTNF tumor necrosis factorIBD inflammatory bowel diseaseHepatologyRT-qPCR quantitative reverse-transcription polymerase chain reactionAICAR 5-aminoimidazole-4-carboxamide-1-β-4-ribofuranosideTDAG8 T-cell death-associated gene 8 (GPR65)Inflammatory Bowel DiseaseGRP65GastroenterologyHypoxia (medical)Molecular biologyGPR G-protein–coupled receptormRNA messenger RNAIL interleukinChIP chromatin immunoprecipitationHIF hypoxia-inducible factorUC ulcerative colitis030104 developmental biologyHypoxia-inducible factorsCancer researchCD Crohn's diseaselcsh:Diseases of the digestive system. GastroenterologyTumor necrosis factor alphaFCS fetal calf serummedicine.symptomChromatin immunoprecipitationHomeostasisCellular and Molecular Gastroenterology and Hepatology
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Anti-inflammatory Function of High-Density Lipoproteins via Autophagy of IκB Kinase

2015

Background & Aims: Plasma levels of high-density lipoprotein (HDL) cholesterol are frequently found decreased in patients with inflammatory bowel disease (IBD). Therefore, and because HDL exerts anti-inflammatory activities, we investigated whether HDL and its major protein component apolipoprotein A-I (apoA-I) modulate mucosal inflammatory responses in vitro and in vivo. Methods: The human intestinal epithelial cell line T84 was used as the in vitro model for measuring the effects of HDL on the expression and secretion of tumor necrosis factor (TNF), interleukin-8 (IL-8), and intracellular adhesion molecule (ICAM). Nuclear factor-κB (NF-κB)-responsive promoter activity was studied by …

WT wild typeApolipoprotein BEMSA electrophoretic mobility shift assayMPO myeloperoxidaseIκB kinaseDSS dextran sodium sulphatemTOR the mammalian target of rapamycinRT-PCR real-time polymerase chain reactionNF-κBchemistry.chemical_compound540 ChemistryApoA-I apolipoprotein A-I10038 Institute of Clinical ChemistryOriginal ResearchTNF tumor necrosis factorbiologyIBD inflammatory bowel diseaseChemistryGastroenterologyMyeloperoxidase10076 Center for Integrative Human PhysiologyMEICS murine endoscopic index of colitis severityTumor necrosis factor alphalipids (amino acids peptides and proteins)3-MA 3-methyl adenineNF-κB nuclear factor κBHDL high-density lipoproteinLC3II light chain 3 IIPBS phosphate-buffered salinep-IKK phosphorylated IκB kinase610 Medicine & healthICAM intracellular adhesion molecule246-Trinitrobenzenesulfonic acidTg transgenicmedicineAutophagyCD Crohn’s disease2715 GastroenterologyColitislcsh:RC799-869KO knockoutHepatologyApolipoprotein A-IAutophagyInflammatory Bowel DiseaseTNBS 246-trinitrobenzenesulfonic acidmedicine.diseaseMolecular biologyIL interleukinsiRNA small interfering RNAPI-3 phosphatidylinositol-3Immunologybiology.protein2721 Hepatologylcsh:Diseases of the digestive system. GastroenterologyPFA paraformaldehydeLipoproteinDAPI 4′6-diamidino-2-phenylindoleCMGH Cellular and Molecular Gastroenterology and Hepatology
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Mosaic activating mutations in GNA11 and GNAQ are associated with phakomatosis pigmentovascularis and extensive dermal melanocytosis

2016

Common birthmarks can be an indicator of underlying genetic disease but are often overlooked. Mongolian blue spots (dermal melanocytosis) are usually localized and transient, but they can be extensive, permanent, and associated with extracutaneous abnormalities. Co-occurrence with vascular birthmarks defines a subtype of phakomatosis pigmentovascularis, a group of syndromes associated with neurovascular, ophthalmological, overgrowth, and malignant complications. Here, we discover that extensive dermal melanocytosis and phakomatosis pigmentovascularis are associated with activating mutations in GNA11 and GNAQ, genes that encode Gα subunits of heterotrimeric G proteins. The mutations were det…

WT wild typeDNA Mutational AnalysisMolecular Sequence Datapostzygotic mutationsMutation MissenseSWS Sturge-Weber syndromeDermatologycesioflammeagermlineBiochemistrySkin DiseasesAnimals Genetically Modifiedg-proteinDNA deoxyribonucleic acidMongolian Spotoculodermal melanocytosis[ SDV.MHEP ] Life Sciences [q-bio]/Human health and pathologyGeneticsAnimalsHumansddc:610Phosphorylationchoroidal melanomaMolecular BiologyAllelesZebrafishdiseaseBase SequenceNeurocutaneous Syndromessturge-weberInfantCell Biologymongolian spotPPV phakomatosis pigmentovascularisGTP-Binding Protein alpha SubunitsHEK293 CellsPhenotypeMutationGTP-Binding Protein alpha Subunits Gq-G11Original Articleuveal melanoma[SDV.MHEP]Life Sciences [q-bio]/Human health and pathologySignal Transduction
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Somatic Symptoms among Children and Adolescents in Poland: A Confirmatory Factor Analytic Study of the Children Somatization Inventory.

2013

The aim of the present study was to examine the factor structure and psychometric properties of the short version of the Children’s Somatization Inventory (CSI-24) in Poland. The CSI-24 is a self-report questionnaire designed to assess somatic symptoms in children and adolescents. A total of 733 children and adolescents, aged 12 to 17 years, participated in this research. The participants for this study were recruited from urban and suburban schools of Opole province in South Western Poland. In addition to the CSI-24, all participants completed the Spence Children’s Anxiety Scale (SCAS) and the Strength and Difficulties Questionnaire (SDQ). The bifactor model that included the three domain-…

Weaknessmedicine.medical_specialtylcsh:Public aspects of medicinePublic Health Environmental and Occupational HealthDiscriminant validityConstruct validitylcsh:RA1-1270Factor structuremedicine.diseaseCronbach's alphaanxiety disorderschildren and adolescentsmedicinePublic HealthChildren’s Somatization Inventorysomatic symptomsPolandLow correlationmedicine.symptomPsychologyPsychiatrySomatizationAnxiety scaleOriginal ResearchFrontiers in public health
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Hydration and dehydration kinetics of xylazine hydrochloride

2009

From the experiments where mixture of xylazine hydrochloride hydrate H and anhydrous X were held at constant conditions, the stable form of xylazine hydrochloride can be found out. To determine equilibrium relative humidity, the unstable form of xylazine hydrochloride was inserted in thermostated humidity chamber and its weight was recorded by weighing the sample outside the chamber. The kinetic model and the rate constant for each condition were determined. The rate constants give information regarding the speed of the process at every experimentally used relative humidity. Thus using the data in coordinates k – p for each temperature it is possible to determine the water vapor pressure of…

XylazineStereochemistryChemistry PharmaceuticalVapour pressure of waterEnthalpyAnalytical chemistryPharmaceutical ScienceXylazineReaction rate constantDrug StabilitymedicineRelative humidityDesiccationChemistryTemperaturefood and beveragesHumidityHumidityGeneral MedicinehumanitiesKineticsAnhydrousThermodynamicsCrystallizationHydrateAdrenergic alpha-Agonistsmedicine.drugPharmaceutical Development and Technology
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The relative stability of xylazine hydrochloride polymorphous forms

2009

All four known xylazine hydrochloride polymorphous forms were obtained and their relative stabilities were compared directly at three different temperatures. At higher temperatures, it is possible to determine the relative stability of all forms directly by measuring the changes in the composition of the mixtures of two polymorphous forms using powder x-ray diffraction methods. At lower temperatures, a solvent was added to the mixture and the changes in composition were determined. Polymorph transition temperatures were determined directly. To predict the transition temperature which was not found using the direct method, the polymorph melting data and determined transition temperatures wer…

XylazineVapor PressureVapor pressureStereochemistryChemistryTransition temperatureVapour pressure of waterTemperatureAnalytical chemistryWaterPharmaceutical ScienceGeneral Medicinelaw.inventionSolventDrug StabilityX-Ray DiffractionPolymorphism (materials science)lawX-ray crystallographySolventsAnhydrousTransition TemperatureCrystallizationCrystallizationAdrenergic alpha-AgonistsPharmaceutical Development and Technology
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Ambiguous Role of Interleukin-12 in Yersinia enterocolitica Infection in Susceptible and Resistant Mouse Strains

1998

ABSTRACT Endogenous interleukin-12 (IL-12) mediates protection against Yersinia enterocolitica in C57BL/6 mice by triggering gamma interferon (IFN-γ) production in NK and CD4 + T cells. Administration of exogenous IL-12 confers protection against yersiniae in Yersinia -susceptible BALB/c mice but exacerbates yersiniosis in resistant C57BL/6 mice. Therefore, we wanted to dissect the different mechanisms exerted by IL-12 during Yersinia infections by using different models of Yersinia -resistant and -susceptible mice, including resistant C57BL/6 mice, susceptible BALB/c mice, intermediate-susceptible wild-type 129/Sv mice, 129/Sv IFN-γ-receptor-deficient (IFN-γR −/− ) mice and C57BL/6 tumor n…

Yersinia Infectionsmedicine.medical_treatmentImmunologyCD8-Positive T-LymphocytesYersiniaMicrobiologyMicrobiologyProinflammatory cytokineInterferon-gammaMiceTransforming Growth Factor betamedicineAnimalsInterferon gammaYersinia enterocoliticaReceptors InterferonYersinia enterocoliticaMice KnockoutHost Response and InflammationMice Inbred BALB CbiologyTumor Necrosis Factor-alphaYersiniosisbiology.organism_classificationmedicine.diseaseInterleukin-12Killer Cells NaturalMice Inbred C57BLInfectious DiseasesCytokineImmunologyInterleukin 12FemaleParasitologyTumor necrosis factor alphamedicine.drugInfection and Immunity
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Differential inclusions involving normal cones of nonregular sets in Hilbert spaces

2017

This thesis is dedicated to the study of differential inclusions involving normal cones of nonregular sets in Hilbert spaces. In particular, we are interested in the sweeping process and its variants. The sweeping process is a constrained differential inclusion involving normal cones which appears naturally in several applications such as elastoplasticity, electrical circuits, hysteresis, crowd motion, etc.This work is divided conceptually in three parts: Study of positively alpha-far sets, existence results for differential inclusions involving normal cones and characterizations of Lyapunov pairs for the sweeping process. In the first part (Chapter 2), we investigate the class of positivel…

[ MATH.MATH-OC ] Mathematics [math]/Optimization and Control [math.OC]cône normalMoreau-Yosida regularizationcono normalmétodo de tipo Galerkinfonction distanceGalerkin-like methodMSC: 34A60 49J52 34G25 49J53 34B10 93D30subdiferencial de Clarkeprocessus de rafleInclusión diferencialensembles positivement alpha-far'sweeping processfonctions de Lyapunovsous-différentiel de Clarkeprocesos de arrastrefunción distanciaLyapunov functionsconjuntos positivamente alpha-farFunciones de Lyapunovméthode de type Galerkinrégularisation de Moreau-YosidaDifferential inclusions[MATH.MATH-OC] Mathematics [math]/Optimization and Control [math.OC]Clarke subdifferentialregularización de Moreau-YosidaDistance functionInclusion différentielle[MATH.MATH-OC]Mathematics [math]/Optimization and Control [math.OC]Normal conepositively alpha-far sets
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In vivo and in vitro sensitivity of blastic plasmacytoid dendritic cell neoplasm to SL-401, an interleukin-3 receptor targeted biologic agent.

2015

International audience; Blastic plasmacytoid dendritic cell neoplasm is an aggressive malignancy derived from plasmacytoid dendritic cells. There is currently no accepted standard of care for treating this neoplasm, and therapeutic strategies have never been prospectively evaluated. Since blastic plasmacytoid dendritic cell neoplasm cells express high levels of interleukin-3 receptor α chain (IL3-Rα or CD123), antitumor effects of the interleukin-3 receptor-targeted drug SL-401 against blastic plasmacytoid dendritic cell neoplasm were evaluated in vitro and in vivo. The cytotoxicity of SL-401 was assessed in patient-derived blastic plasmacytoid dendritic cell neoplasm cell lines (CAL-1 and …

[SDV.MHEP.HEM] Life Sciences [q-bio]/Human health and pathology/HematologyMalePathology[SDV]Life Sciences [q-bio]ApoptosisMice SCIDMice0302 clinical medicineMice Inbred NODhemic and lymphatic diseasesTumor Cells CulturedMedicineCytotoxic T cellNeoplasm[ SDV.MHEP.HEM ] Life Sciences [q-bio]/Human health and pathology/HematologyCytotoxicityAged 80 and overmedicine.diagnostic_test[SDV.MHEP.HEM]Life Sciences [q-bio]/Human health and pathology/HematologyHematologyArticlesMiddle AgedFlow Cytometry3. Good health[SDV] Life Sciences [q-bio]030220 oncology & carcinogenesisHematologic NeoplasmsFemaleAdultmedicine.medical_specialtyRecombinant Fusion ProteinsBlotting WesternInterleukin-3 Receptor alpha Subunit[SDV.CAN]Life Sciences [q-bio]/Cancer[SDV.BC]Life Sciences [q-bio]/Cellular BiologyIn Vitro TechniquesFlow cytometry03 medical and health sciences[SDV.CAN] Life Sciences [q-bio]/CancerBiomarkers TumorAnimalsHumans[SDV.BC] Life Sciences [q-bio]/Cellular BiologyAgedCell ProliferationMyeloproliferative Disordersbusiness.industryCell growthDendritic Cellsmedicine.diseaseXenograft Model Antitumor Assaysstomatognathic diseasesCell cultureApoptosisCancer researchInterleukin-3 receptorbusiness030215 immunologyPlasmacytomaHaematologica
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