Search results for "PGE"

showing 10 items of 40 documents

2,3-Dihydrobenzofuran privileged structures as new bioinspired lead compounds for the design of mPGES-1 inhibitors

2016

International audience; 2,3-Dihydrobenzofurans are proposed as privileged structures and used as chemical platform to design small compound libraries. By combining molecular docking calculations and experimental verification of biochemical interference, we selected some potential inhibitors of microsomal prostaglandin E2 synthase (mPGES)-1. Starting from low affinity natural product 1, by our combined approach we identified the compounds 19 and 20 with biological activity in the low micromolar range. Our data suggest that the 2,3-dihydrobenzofuran derivatives might be suitable bioinspired lead compounds for development of new generation mPGES-1 inhibitors with increased affinity.

0301 basic medicine300323-Dihydrobenzofuran privileged structure; Cancer; Inflammation; Molecular docking; mPGES-1 inhibitors; Biochemistry; Clinical Biochemistry; Molecular Biology; Molecular Medicine; Organic Chemistry; Drug Discovery3003 Pharmaceutical Science; 3003Amino Acid MotifsClinical BiochemistryGene ExpressionPharmaceutical Science01 natural sciencesClinical biochemistryBiochemistry[ CHIM ] Chemical SciencesProtein Structure Secondary[ SDV.CAN ] Life Sciences [q-bio]/Cancerchemistry.chemical_compoundLow affinityDrug DiscoveryEnzyme Inhibitors23-Dihydrobenzofuran privileged structure; Molecular docking; mPGES-1 inhibitors; Cancer; InflammationProstaglandin-E SynthasesCancerAnti-Inflammatory Agents Non-SteroidalBiological activityProto-Oncogene Proteins c-metIntramolecular OxidoreductasesMolecular Docking SimulationMolecular dockingMolecular Medicinelipids (amino acids peptides and proteins)Cell SurvivalStereochemistryMolecular Sequence Data2Antineoplastic Agents[SDV.CAN]Life Sciences [q-bio]/Cancer3-Dihydrobenzofuran privileged structureInhibitory Concentration 50Structure-Activity Relationship03 medical and health sciencesCell Line TumorMicrosomesHumans[CHIM]Chemical SciencesMolecular BiologyBenzofuransInflammationNatural product010405 organic chemistryDrug Discovery3003 Pharmaceutical ScienceOrganic ChemistryEpithelial CellsmPGES-1 inhibitorsCombinatorial chemistryCombined approach0104 chemical sciences030104 developmental biologychemistryDrug DesignDrug Screening Assays Antitumor
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Involvement of interleukin-1 type 1 receptors in lipopolysaccharide-induced sickness responses

2017

Sickness responses to lipopolysaccharide (LPS) were examined in mice with deletion of the interleukin (IL)-1 type 1 receptor (IL-1R1). IL-1R1 knockout (1(0) mice displayed intact anorexia and HPA-axis activation to intraperitoneally injected LPS (anorexia: 10 or 120 mu g/kg; HPA-axis: 120 mu g/kg), but showed attenuated but not extinguished fever (120 g/kg). Brain PGE2 synthesis was attenuated, but Cox-2 induction remained intact. Neither the tumor necrosis factor-alpha (TNF alpha) inhibitor etanercept nor the IL -6 receptor antibody tocilizumab abolished the LPS induced fever in IL -1R1 KO mice. Deletion of IL -1R1 specifically in brain endothelial cells attenuated the LPS induced fever, b…

0301 basic medicineLipopolysaccharidesMalemedicine.medical_specialtyLipopolysaccharideFeverCell- och molekylärbiologiImmunologyHypothalamusAnorexiaEtanerceptInterleukin-1 type 1 receptor; Lipopolysaccharide; Fever; Anorexia; ACTH; Corticosterone; Endothelial cells; THF alpha; Interleukin-6; PGE(2)03 medical and health sciencesBehavioral Neurosciencechemistry.chemical_compoundEating0302 clinical medicineAdrenocorticotropic HormoneCorticosteroneInternal medicinemedicineJournal ArticleAnimalsInterleukin 6ReceptorIllness BehaviorInflammationMice KnockoutReceptors Interleukin-1 Type IbiologyEndocrine and Autonomic Systemsbusiness.industryInterleukinBrainEndothelial CellsAnorexia030104 developmental biologyEndocrinologychemistrybiology.proteinTumor necrosis factor alphaFemalemedicine.symptomInflammation MediatorsbusinessCorticosterone030217 neurology & neurosurgeryCell and Molecular Biologymedicine.drug
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Genome-wide diversity and runs of homozygosity in the “Braque Français, type Pyrénées” dog breed

2018

Objective Braque Français, type Pyrénées is a French hunting-dog breed whose origin is traced back to old pointing gun-dogs used to assist hunters in finding and retrieving game. This breed is popular in France, but seldom seen elsewhere. Despite the ancient background, the literature on its genetic characterization is surprisingly scarce. A recent study looked into the demography and inbreeding using pedigree records, but there is yet no report on the use of molecular markers in this breed. The aim of this work was to genotype a population of Braque Français, type Pyrénées dogs with the high-density SNP array to study the genomic diversity of the breed. Results The average observed (\docum…

0301 basic medicineMalelcsh:MedicineRuns of HomozygosityGenetic diversitySettore AGR/17 - Zootecnica Generale E Miglioramento Geneticotype PyrénéesSNPGenetic diversityMolecular markersInbreedingRuns of homozygosityHeterozygosityEffective population sizeDogInbreedingDogBraque Français type PyrénéesSNPGenetic diversityMolecular markersInbreedingRuns of homozygosityHeterozygositylcsh:QH301-705.5education.field_of_studyHeterozygosityGenomeHomozygote04 agricultural and veterinary sciencesGeneral Medicinetype PyrénéesBraque Français type PyrénéesBreedResearch NoteFemaleFranceInbreedingSNP arrayGenetic MarkersHeterozygotePopulationSNPBiologyRuns of homozygosityPolymorphism Single NucleotideGeneral Biochemistry Genetics and Molecular Biology03 medical and health sciencesDogsAnimalsGenetic variabilityeducationlcsh:Science (General)Genetic diversityDogBraque Françaislcsh:R0402 animal and dairy sciencebraque françaisMolecular markersGenetic Variation040201 dairy & animal science030104 developmental biologylcsh:Biology (General)Evolutionary biologyDog Braque Français type Pyrénées SNP Genetic diversity Molecular markers Inbreeding Runs of homozygosity Heterozygositylcsh:Q1-390BMC Research Notes
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The role of extracellular calcium in bone metastasis

2016

AbstractThis review summarizes the role of extracellular calcium, as found present in the bone tissue, in the process of bone metastasis.

0301 basic medicinelcsh:Diseases of the musculoskeletal systemIGF insulin-like growth factorPGE-2 prostaglandin E-2Bone tissueFibroblast growth factorM-CSF macrophage colony-stimulating factorPDGF platelet-derived growth factorBone remodelingSK3 small conductance calcium-activated potassium channel 30302 clinical medicineERK extracellular signal-regulated kinaseTGFβ transforming growth factor betaBMP's bone morphogenetic proteinsbiologyAKT AKT8 virus oncogene cellular homologBone metastasislcsh:Neoplasms. Tumors. Oncology. Including cancer and carcinogenshumanitiescAMP cyclic adenosine monophosphatemedicine.anatomical_structureOncologyRANKL030220 oncology & carcinogenesisIon channelsCaSR calcium-sensing receptorPTHrP parathyroid hormone-related proteinPlatelet-derived growth factor receptorResearch PaperTRP transient receptor potentialmedicine.medical_specialtychemistry.chemical_elementCalciumRANKL receptor activator of NF-κB ligandlcsh:RC254-28203 medical and health sciencesPLC phospholipase CInternal medicinemedicineExtracellularCaSRET-1 endothelin-1PTEN phosphatase and tensin homolog deleted on chromosome 10business.industryBone metastasismedicine.diseaseFGF fibroblast growth factor030104 developmental biologyEndocrinologyPSA prostate specific antigenchemistryCOPD chronic obstructive pulmonary diseasebiology.proteinCancer researchJNK jun N-terminal kinasePKA protein kinase ARANK receptor activator of NF-κBCalciumlcsh:RC925-935businessMAPK mitogen-activated protein kinaseJournal of Bone Oncology
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Response of AGATA segmented HPGe detectors to gamma rays up to 15.1MeV

2013

WOS: 000314826000009

AGATA; Gamma-ray spectroscopy; Gamma-ray tracking; HPGe detectors; Pulse-shape and gamma-ray tracking algorithms; Semiconductor detector performance and simulationsNuclear and High Energy PhysicsPulse-shape and gamma-ray tracking algorithmsAstrophysics::High Energy Astrophysical PhenomenaFOS: Physical sciencesSemiconductor detector performance and simulationsTracking (particle physics)01 natural sciencesNuclear physicsGamma-ray tracking0103 physical sciencesGamma spectroscopyddc:530Gamma-ray spectroscopyNuclear Experiment (nucl-ex)010306 general physicsNuclear ExperimentInstrumentationNuclear ExperimentDetectors de radiacióPhysicsSpectrometer010308 nuclear & particles physicsDetectorHPGe detectorsGamma ray81V35Semiconductor detectorAGATAFísica nuclearHpge detectorAGATA
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Récit d’un « tremplin ». Des bacheliers professionnels en classe préparatoire

2021

International audience; Rares sont les bacheliers professionnels à déjouer les statistiques en s’orientant vers une classe préparatoire aux grandes écoles. L’audace des bacheliers professionnels, peu préparés aux exigences académiques des cursus longs et engagés dans une voie où ils sont traditionnellement moins attendus, interpelle. Comment ces jeunes justifient-ils ce parcours improbable ? Les propos des bacheliers professionnels rencontrés sont révélateurs à la fois de la représentation qu’ils se font de leur orientation, de la place qu’ils « rêvent » dans la société à venir et aussi du niveau de confiance dans leurs « capacités » à y parvenir. Dans un cadre stimulant, l'horizon des écol…

Baccalauréat professionnelOrientation scolaire[SHS.EDU]Humanities and Social Sciences/EducationCPGE[SHS.EDU] Humanities and Social Sciences/EducationBachelier
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Efficience de l'enseignement supérieur dans la production des élites

2004

International audience

Ecole d'ingénieur[SHS.EDU]Humanities and Social Sciences/EducationCPGEIngénieurEfficience[SHS.EDU] Humanities and Social Sciences/EducationEfficacité interneFranceEfficacité externeComputingMilieux_MISCELLANEOUSEnseignement supérieur
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Studio di modelli equivalenti per la simulazione con il codice PENELOPE della risposta in efficienza di un rivelatore HPGe

2017

La simulazione della risposta di un rivelatore HPGe con l’impiego di codici Monte Carlo è una tecnica ormai diffusamente impiegata e particolarmente utile per la valutazione di efficienze quando non sono disponibili standards di calibrazione con stessa forma e composizione del campione in esame. Il risultato della simulazione dipende dalla conoscenza più o meno dettagliata delle caratteristiche del rivelatore, atte a definire un “modello” dello stesso. Per evidenziare anche quelle parti non definite nella certificazione del costruttore, solitamente si effettua una radiografia del rivelatore fatta eccezione per i casi in cui non è realizzabile pena lo smontaggio della struttura di schermatur…

Efficienza Monte Carlo Rivelatori HPGeSettore ING-IND/20 - Misure E Strumentazione Nucleari
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Evaluation des compétences des anciens élèves des classes préparatoires scientifiques par leurs performances scolaires et professionnelles

2004

International audience

Enseignement scientifiqueCompétence professionnelle[SHS.EDU]Humanities and Social Sciences/EducationCPGE[SHS.EDU] Humanities and Social Sciences/EducationÉtudiantÉvaluation des compétencesFrancePerformance scolaireComputingMilieux_MISCELLANEOUSEnseignement supérieurFilière sciences
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Equivalent detector models for the simulation of efficiency response of an HPGe detector with PENELOPE code

2019

Monte Carlo simulation of response of an HPGe detector is a widely used technique to evaluate counting efficiencies. It is particularly useful when calibration standards with the same shape and composition of the sample under examination are not available. The result of the simulation depends on the more or less detailed knowledge of the characteristics of the detector, able to define a "model" of the same detector. To highlight parts not well defined in the manufacturer's certification, a detector X-ray analysis is usually performed, except in cases when it is not possible to dismantle the shielding structure with the loss of previous calibration data. In this work, in absence of some data…

Gamma-ray spectrometry Monte Carlo HPGe detectors efficiency modelingSettore ING-IND/20 - Misure E Strumentazione Nucleari
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