Search results for "SOX"

showing 10 items of 240 documents

Coupling between agonist and chloride ionophore sites of the GABA(A) receptor: agonist/antagonist efficacy of 4-PIOL.

2000

Eight gamma-aminobutyric acid (GABA) mimetics were tested on their ability to differentiate native GABA(A) receptor subtypes present in various rat brain regions. In rat brain cryostat sections, little regional variations by the agonistic actions of muscimol, thiomuscimol, 4,5,6,7-tetrahydroisoazolo(5,4-c)pyridin-3-ol, piperidine-4-sulphonic acid, taurine and beta-alanine on [35S]t-butylbicyclophosphorothionate ([35S]TBPS) binding to GABA(A) receptor channels were found. They were very similar to those found for GABA itself and indicated no direct correlation with single subunit distributions for any of these compounds. Only the low-efficacy GABA mimetic 5-(4-piperidyl)isoxazol-3-ol (4-PIOL…

AgonistMalemedicine.medical_specialtyAgonist-antagonistmedicine.drug_classBiologyLigandsPartial agonistGABAA-rho receptorCell Linechemistry.chemical_compoundPiperidinesInternal medicinemedicineAnimalsHumansRats WistarReceptorGABA AgonistsPharmacologyIonophoresGABAA receptorBrainIsoxazolesBridged Bicyclo Compounds HeterocyclicReceptors GABA-ARatsEndocrinologyMuscimolchemistryThiomuscimolEuropean journal of pharmacology
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Aldosterone synthase activity in the Y-1 adrenal cell line.

1995

The Y-1 adrenal cell line was shown to produce 20 alpha-dihydroaldosterone from deoxycorticosterone. This compound was identified by GC-MS by comparison with the previously synthesized reference compound. Two other 18-hydroxylated metabolites were identified as 11 beta,18-dihydroxy-20 alpha-dihydroprogesterone from endogenous cholesterol and 18-hydroxy-20 alpha-dihydro-11-dehydrocorticosterone from DOC. The conditions necessary for the synthesis of these compounds are culturing in 20% serum-supplemented medium and repeated incubations with the substrate. The production of 11 beta-hydroxylated steroids and that of 18-oxygenated steroids is stimulated differently by ACTH and angiotensin II su…

Aldosterone synthasemedicine.medical_specialtymedicine.drug_classEndocrinology Diabetes and MetabolismClinical BiochemistryBiochemistryGas Chromatography-Mass SpectrometryCell LineMiceEndocrinologyAdrenocorticotropic HormoneCytochrome P-450 Enzyme SystemInternal medicineMineralocorticoidsmedicineAnimalsCytochrome P-450 CYP11B2RNA MessengerDesoxycorticosteroneMolecular BiologyGlucocorticoidschemistry.chemical_classificationbiologyAdrenal cortexAngiotensin IICytochrome P450Cell BiologyAngiotensin IIEnzymeEndocrinologymedicine.anatomical_structurechemistryBiochemistryCell cultureMineralocorticoidbiology.proteinAdrenal CortexMolecular MedicineSteroid 11-beta-HydroxylaseGlucocorticoidmedicine.drugThe Journal of steroid biochemistry and molecular biology
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Synthesis and antimicrobial activity of new 3-(1-R-3(5)-methyl-4-nitroso-1H-5(3)-pyrazolyl)-5-methylisoxazoles.

2000

A number of new 3-(1-R-3(5)-methyl-4-nitroso-1H-5(3)-pyrazolyl)-5-methylisoxazoles 6a-g (7b-f) were synthesized and tested for antibacterial and antifungal activity. Some of these compounds displayed antifungal activity at non-cytotoxic concentrations. Derivative 6c was 9 times more potent in vitro than miconazole and 20 times more selective against C. neoformans. 6c was also 8- and 125-fold more potent than amphotericin B and fluconazole, respectively. None of the compounds was active against bacteria. Preliminary structure-activity relationship (SAR) studies showed that the NO group at position 4 of the pyrazole ring is essential for the activity. Lipophilicity of the pyrazole moiety, N-a…

Antifungal AgentsStereochemistryClinical BiochemistryPharmaceutical ScienceMicrobial Sensitivity TestsPyrazoleGram-Positive BacteriaBiochemistryChemical synthesischemistry.chemical_compoundStructure-Activity RelationshipAnti-Infective AgentsDrug DiscoveryGram-Negative BacteriamedicineMoietyHumansCytotoxicityMolecular BiologyChemistryOrganic ChemistryFungiNitrosoIsoxazolesAntimicrobialAnti-Bacterial AgentsLipophilicityCryptococcus neoformansHIV-1Molecular MedicineMiconazolemedicine.drugBioorganicmedicinal chemistry
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Anaplastic Thyroid Carcinoma: A ceRNA Analysis Pointed to a Crosstalk between SOX2, TP53, and microRNA Biogenesis.

2014

It has been suggested that cancer stem cells (CSC) may play a central role in oncogenesis, especially in undifferentiated tumours. Anaplastic thyroid carcinoma (ATC) has characteristics suggestive of a tumour enriched in CSC. Previous studies suggested that the stem cell factorSOX2has a preeminent hierarchical role in determining the characteristics of stem cells in SW1736 ATC cell line. In detail, silencing SOX2 in SW1736 is able to suppress the expression of the stem markers analysed, strongly sensitizing the line to treatment with chemotherapeutic agents. Therefore, in order to further investigate the role of SOX2 in ATC, a competing endogenous RNA (ceRNA) analysis was conducted in order…

Article SubjectEndocrinology Diabetes and MetabolismSOX2Stem cell factorAnaplastic Thyroid carcinomaBiologyBioinformaticsmedicine.disease_causelcsh:Diseases of the endocrine glands. Clinical endocrinologySettore MED/13 - EndocrinologiaEndocrinologySOX2Cancer stem cellmicroRNAmedicineGene silencinglcsh:RC648-665microRNAEndocrine and Autonomic SystemsCompeting endogenous RNAceRNACancer researchStem cellCarcinogenesisResearch ArticleInternational journal of endocrinology
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Pharmacological blockade of the fatty acid amide hydrolase (FAAH) alters neural proliferation, apoptosis and gliosis in the rat hippocampus, hypothal…

2015

Endocannabinoids participate in the control of neurogenesis, neural cell death and gliosis. The pharmacological effect of the fatty acid amide hydrolase (FAAH) inhibitor URB597, which limits the endocannabinoid degradation, was investigated in the present study. Cell proliferation (phospho-H3(+) or BrdU(+) cells) of the main adult neurogenic zones as well as apoptosis (cleaved caspase-3(+)), astroglia (GFAP(+)), and microglia (Iba1(+) cells) were analyzed in the hippocampus, hypothalamus and striatum of rats intraperitoneally treated with URB597 (0.3 mg/kg/day) at one dose/4-days resting or 5 doses (1 dose/day). Repeated URB597 treatment increased the plasma levels of the N-acylethanolamine…

AstrocitosNeurobiologia del desenvolupamentAmidohidrolasasCannabinoid receptorCarbamatos:Chemicals and Drugs::Amino Acids Peptides and Proteins::Proteins::Intracellular Signaling Peptides and Proteins::Apoptosis Regulatory Proteins::Caspases [Medical Subject Headings]:Phenomena and Processes::Cell Physiological Phenomena::Cell Physiological Processes::Cell Differentiation::Neurogenesis [Medical Subject Headings]medicine.medical_treatment:Chemicals and Drugs::Carbohydrates::Monosaccharides::Hexoses::Glucose [Medical Subject Headings]Apoptosis:Phenomena and Processes::Physiological Phenomena::Body Constitution::Body Weights and Measures::Body Size::Body Weight [Medical Subject Headings]chemistry.chemical_compound:Chemicals and Drugs::Amino Acids Peptides and Proteins::Proteins::Membrane Proteins::Receptors Cell Surface::Receptors G-Protein-Coupled::Receptors Cannabinoid::Receptor Cannabinoid CB1 [Medical Subject Headings]0302 clinical medicine:Chemicals and Drugs::Organic Chemicals::Carboxylic Acids::Acids Acyclic::Carbamates [Medical Subject Headings]Fatty acid amide hydrolaseReceptor cannabinoide CB1:Organisms::Eukaryota::Animals [Medical Subject Headings]FAAHGliosishealth care economics and organizations:Chemicals and Drugs::Nucleic Acids Nucleotides and Nucleosides::Nucleosides::Deoxyribonucleosides::Deoxyuridine::Bromodeoxyuridine [Medical Subject Headings]:Chemicals and Drugs::Lipids::Glycerides::Triglycerides [Medical Subject Headings]Original Research0303 health sciencesNeurogenesisBenzamidas:Chemicals and Drugs::Polycyclic Compounds::Steroids::Cholestanes::Cholestenes::Cholesterol [Medical Subject Headings]Endocannabinoid systemEtanolaminas3. Good healthEndocannabinoides:Chemicals and Drugs::Lipids::Fatty Acids::Fatty Acids Unsaturated::Fatty Acids Monounsaturated::Oleic Acids [Medical Subject Headings]CannabinoidesMicroglíalipids (amino acids peptides and proteins)medicine.symptomColesterol:Chemicals and Drugs::Organic Chemicals::Hydrocarbons::Terpenes::Cannabinoids [Medical Subject Headings]:Chemicals and Drugs::Lipids::Fatty Acids::Palmitic Acids [Medical Subject Headings]psychological phenomena and processesProliferación celularmedicine.medical_specialtyCerebroNeurogenesiseducationBiologyBromodesoxiuridina:Anatomy::Nervous System::Neuroglia::Microglia [Medical Subject Headings]Triglicéridoslcsh:RC321-571Ácidos oléicosRatas03 medical and health sciencesCellular and Molecular NeuroscienceInternal medicineHipocampomedicineCaspasa 3:Anatomy::Nervous System::Central Nervous System::Brain::Limbic System::Hippocampus [Medical Subject Headings]:Phenomena and Processes::Cell Physiological Phenomena::Cell Physiological Processes::Cell Growth Processes::Cell Proliferation [Medical Subject Headings]lcsh:Neurosciences. Biological psychiatry. Neuropsychiatry030304 developmental biologyPalmitoylethanolamide:Chemicals and Drugs::Chemical Actions and Uses::Pharmacologic Actions::Molecular Mechanisms of Pharmacological Action::Neurotransmitter Agents::Endocannabinoids [Medical Subject Headings]:Chemicals and Drugs::Enzymes and Coenzymes::Enzymes::Hydrolases::Amidohydrolases [Medical Subject Headings]Cannabinoids:Anatomy::Cells::Neuroglia::Astrocytes [Medical Subject Headings]Peso corporalEnergy metabolism:Anatomy::Nervous System::Central Nervous System::Brain [Medical Subject Headings]:Anatomy::Nervous System::Central Nervous System::Brain::Limbic System::Hypothalamus [Medical Subject Headings]URB597:Phenomena and Processes::Cell Physiological Phenomena::Cell Physiological Processes::Cell Death [Medical Subject Headings]:Diseases::Pathological Conditions Signs and Symptoms::Pathologic Processes::Gliosis [Medical Subject Headings]:Chemicals and Drugs::Organic Chemicals::Amines::Amino Alcohols::Ethanolamines [Medical Subject Headings]Muerte celular:Phenomena and Processes::Cell Physiological Phenomena::Cell Physiological Processes::Cell Death::Apoptosis [Medical Subject Headings]:Organisms::Eukaryota::Animals::Chordata::Vertebrates::Mammals::Rodentia::Muridae::Murinae::Rats [Medical Subject Headings]EndocrinologyURB597chemistryGliosisnervous systemGlucosaCannabinoidEnergy Metabolism:Chemicals and Drugs::Organic Chemicals::Amides::Benzamides [Medical Subject Headings]HipotálamoÁcidos palmíticos030217 neurology & neurosurgeryNeuroscienceFrontiers in Cellular Neuroscience
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Synthesis and in vitro antimicrobial activities of new (cyano-NNO-azoxy) pyrazole derivatives

2011

The antibacterial and antifungal activity of a series of products, in which the 1,5-dimethyl-4-(cyano- NNO-azoxy)pyrazol-3-yl and 1,3-dimethyl-4-(cyano-NNO-azoxy)pyrazol-5-yl moieties were linked to pyridine, pyrazole, isoxazole, thiophene and the furan ring, were examined. No molecule displayed activity against the Gram-negative bacteria tested. Conversely, some compounds displayed activity against two Staphylococcus aureus strains, including the methicillin resistant strain. All compounds displayed interesting antifungal activity, the most active compound of the series being the thiophene derivative 7a. This compound’s activity against Candida krusei and Candida glabrata (MIC = 0.25 and 0…

AzoxyStaphylococcus aureusAntifungal AgentsStereochemistryClinical BiochemistryPharmaceutical ScienceMicrobial Sensitivity TestsPyrazoleBiochemistryChemical synthesisAntifungal activity Pyrazole Azole sistance Cyano-NNO-azoxy Thiophenechemistry.chemical_compoundAnti-Infective AgentsThiopheneCandida kruseiNitrilesDrug DiscoveryThiopheneAntifungal activityIsoxazoleAntifungal activity; Pyrazole; Azole resistance; Cyano-NNO-azoxy; Thiophene.Molecular BiologyCandidaMolecular StructurebiologyCandida glabrataOrganic ChemistryBiological activitybiology.organism_classificationSettore CHIM/08 - Chimica FarmaceuticachemistryCyano-NNO-azoxyPyrazoleAzole resistancePyrazolesMolecular MedicineAzo Compounds
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A case of meningitis due to Achromobacter xylosoxidans denitrificans 60 years after a cranial trauma

2011

Import JabRef | WosArea Research and Experimental Medicine; International audience; Background: Achromobacter xylosoxidans (AX) is a non-fermentative aerobic Gram-negative bacillus. It is an opportunistic pathogen and the causative agent of various infections. We report an original case of late posttraumatic meningitis due to AX denitrificans. Case Report: An 83-year-old man was hospitalized for acute headache, nausea and vomiting. The emergency brain computer tomography (CT) scan did not reveal any anomaly. In his medical history, there was an auditory injury due to a cranial trauma incurred in a skiing accident 60 years earlier. Cytobiochemical analysis of the cerebrospinal fluid (CSF) re…

BACTEREMIAPOSTTRAUMATIC MENINGITIS[SCCO.NEUR] Cognitive science/NeuroscienceINFECTION[ SCCO.NEUR ] Cognitive science/NeuroscienceNEONATAL MENINGITISALCALIGENES-XYLOSOXIDANSRHINORRHEAPATIENT
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CCDC 1564495: Experimental Crystal Structure Determination

2017

Related Article: Fernando Rabasa-Alcañiz, Javier Torres, María Sánchez-Roselló, Tomás Tejero, Pedro Merino, Santos Fustero, Carlos del Pozo|2017|Adv.Synth.Catal.|359|3752|doi:10.1002/adsc.201700975

Benzyl [(3aR5S9bR)-7-fluoro-3-methyl-9b-(trifluoromethyl)-133a459bhexahydronaphtho[21-c]isoxazol-5-yl](hydroxy)carbamateSpace GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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4-(4-Fluorophenyl)-2-methyl-3-(1-oxy-4-pyridyl)isoxazol-5(2H)-one

2008

The crystal structure of the title compound, C15H11FN2O3, was determined as part of a study on the biological activity of isoxazolone derivatives as p38 mitogen-activated protein kinase (MAPK) inhibitors. The dihedral angles between rings are isoxazole/benzene = 55.0 (3)°, isoxazole/pyridine = 33.8 (2)° and benzene/pyridine = 58.1 (2)°.

Biological activityGeneral ChemistryCrystal structureDihedral angleCondensed Matter PhysicsBioinformaticsOrganic PapersMedicinal chemistrylcsh:Chemistrychemistry.chemical_compoundlcsh:QD1-999chemistryPyridineGeneral Materials ScienceIsoxazoleBenzeneProtein kinase AActa Crystallographica Section E Structure Reports Online
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3D bioprinting of tissue units with mesenchymal stem cells, retaining their proliferative and differentiating potential, in polyphosphate-containing …

2021

Abstract The three-dimensional (3D)-printing processes reach increasing recognition as important fabrication techniques to meet the growing demands in tissue engineering. However, it is imperative to fabricate 3D tissue units, which contain cells that have the property to be regeneratively active. In most bio-inks, a metabolic energy-providing component is missing. Here a formulation of a bio-ink is described, which is enriched with polyphosphate (polyP), a metabolic energy providing physiological polymer. The bio-ink composed of a scaffold (N,O-carboxymethyl chitosan), a hydrogel (alginate) and a cell adhesion matrix (gelatin) as well as polyP substantially increases the viability and the …

Biomedical EngineeringBioengineeringMatrix (biology)Biochemistrylaw.inventionBiomaterialsSOX2Tissue engineeringPolyphosphateslawCell adhesion3D bioprintingTissue EngineeringTissue ScaffoldsChemistryMesenchymal stem cellBioprintingMesenchymal Stem CellsGeneral MedicineCell biologybody regionsRUNX2Printing Three-DimensionalAlkaline phosphataseInkcirculatory and respiratory physiologyBiotechnologyBiofabrication
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