Search results for "rase"

showing 10 items of 4343 documents

Relative expression of cholesterol transport-related proteins and inflammation markers through the induction of 7-ketosterol-mediated stress in Caco-…

2013

Human diets contain sterol oxidation products that can induce cytotoxic effects, mainly caused by cholesterol oxides. However, phytosterol oxides effects have been less extensively investigated. This study evaluates the production of inflammatory biomarkers (IL-1β, IL-8, IL-10, TNFα) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells. These effects were linked to intracellular signaling pathways by using several inhibitors. Results showed 7-ketostigmasterol to have a greater proinflammatory potential than 7-ketocholesterol. In non-p…

media_common.quotation_subjectLipoproteinsInterleukin-1betaStigmasterolDown-RegulationInflammationToxicologyBradykininProinflammatory cytokineGene expressionmedicineHumansRNA MessengerATP Binding Cassette Transporter Subfamily G Member 5Acetyl-CoA C-AcetyltransferaseInternalizationKetocholesterolsmedia_commonInflammationbiologyTumor Necrosis Factor-alphaAnticholesteremic AgentsInterleukin-8Membrane ProteinsMembrane Transport ProteinsBiological TransportGeneral MedicineMetabolismSterolInterleukin-10Up-RegulationBiochemistryHMG-CoA reductasebiology.proteinTumor necrosis factor alphaATP-Binding Cassette TransportersAcyl Coenzyme Amedicine.symptomCaco-2 CellsBiomarkersFood ScienceFood and chemical toxicology : an international journal published for the British Industrial Biological Research Association
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Data from: Temporal relationship between genetic and warning signal variation in the aposematic wood tiger moth (Parasemia plantaginis)

2014

Many plants and animals advertise unpalatability through warning signals in the form of colour and shape. Variation in warning signals within local populations is not expected because they are subject to directional selection. However, mounting evidence of warning signal variation within local populations suggests that other selective forces may be acting. Moreover, different selective pressures may act on the individual components of a warning signal. At present, we have a limited understanding about how multiple selection processes operate simultaneously on warning signal components, and even less about their temporal and spatial dynamics. Here, we examined temporal variation of several w…

medicine and health care2009-2011UV-signalingcolour polymorphismFluctuating PopulationsLife SciencesMedicineParasemia plantaginisMelanization
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Data from: To quiver or to shiver: increased melanisation benefits thermoregulation, but reduces warning signal efficacy in the wood tiger moth

2013

Melanin production is often considered costly, yet beneficial for thermoregulation. Studies of variation in melanization and the opposing selective forces that underlie its variability contribute greatly to understanding natural selection. We investigated whether melanization benefits are traded off with predation risk to promote observed local and geographical variation in the warning signal of adult male wood tiger moths (Parasemia plantaginis). Warning signal variation is predicted to reduce survival in aposematic species. However, in P. plantaginis, male hindwings are either yellow or white in Europe, and show continuous variation in melanized markings that cover 20 to 90 per cent of th…

medicine and health careMedicineaposematismParasemia plantaginisLife sciences
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Data from: Intralocus tactical conflict: genetic correlations between fighters and sneakers of the dung beetle Onthophagus taurus

2015

Males and females differ in their phenotypic optima for many traits, and since the majority of genes are expressed in both sexes, some alleles can be beneficial to one sex but harmful to the other (intralocus sexual conflict; ISC). ISC theory has recently been extended to intrasexual dimorphisms, where certain alleles may have opposite effects on the fitness of males of different morphs that employ alternative reproductive tactics (intralocus tactical conflict; ITC). Here we use a half-sib breeding design to investigate the genetic basis for ISC and ITC in the dung beetle Onthophagus taurus. We found positive heritabilities and intersexual genetic correlations for almost all traits investig…

medicine and health carepolyphenismOnthophagus taurusAlternative Reproductive TacticsMedicinemale dimorphismintrasexual dimorphismLife sciencesconditional strategy
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In vivo evaluation of the interaction between the Escherichia coli IGP synthase subunits using the Bacterial Two-Hybrid system

2020

ABSTRACT Histidine biosynthesis is one of the most characterized metabolic routes for its antiquity and its central role in cellular metabolism; indeed, it represents a cross-road between nitrogen metabolism and de novo synthesis of purines. This interconnection is due to the activity of imidazole glycerol phosphate synthase, a heterodimeric enzyme constituted by the products of two his genes, hisH and hisF, encoding a glutamine amidotransferase and a cyclase, respectively. Despite their interaction was suggested by several in vitro experiments, their in vivo complex formation has not been demonstrated. On the contrary, the analysis of the entire Escherichia coli interactome performed using…

medicine.disease_causeMicrobiologyInteractomeCyclase03 medical and health scienceschemistry.chemical_compoundBiosynthesisAminohydrolasesTwo-Hybrid System TechniquesEscherichia coliGeneticsmedicineHistidineAmino Acid SequencePurine metabolismMolecular BiologyEscherichia coliHistidine030304 developmental biologyGlutamine amidotransferase0303 health sciencesATP synthasebiologyEscherichia coli Proteins030302 biochemistry & molecular biologyProtein SubunitschemistryBiochemistrybiology.proteinProtein BindingFEMS Microbiology Letters
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Patterns and rates of nucleotide substitution, insertion and deletion in the endosymbiont of antsBlochmannia floridanus

2009

Genome reduction is a general process that has been studied in numerous symbiotic bacteria associated with insects. We investigated the last stages of genome degradation in Blochmannia floridanus, a mutualistic bacterial endosymbiont of the ant Camponotus floridanus. We determined the tempo (rates of insertion and deletion) and mode (size and number of insertion-deletion events) of the process in the last 200,000 years by analysing a total of 16 intergenic regions in several strains of this endosymbiont from different ant populations. We provide the first calculation of the reduction rate for noncoding DNA in this endosymbiont (2.2 x 10(-8) lost nucleotides/site/year) and compare it with th…

medicine.disease_causePolymerase Chain ReactionPolymorphism Single NucleotideGenomeIntergenic regionGeneticsmedicineAnimalsSymbiosisIndelEscherichia coliEcosystemPhylogenyEcology Evolution Behavior and SystematicsSequence DeletionGeneticsGenomeBase SequencebiologyAntsbiology.organism_classificationNoncoding DNADNA Transposable ElementsFloridaMicrosatelliteCamponotus floridanusBuchneraMolecular Ecology
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Quinoline anticancer agents active on DNA and DNA-interacting proteins: From classical to emerging therapeutic targets.

2021

Quinoline is one of the most important and versatile nitrogen heterocycles embodied in several biologically active molecules. Within the numerous quinolines developed as antiproliferative agents, this review is focused on compounds interfering with DNA structure or with proteins/enzymes involved in the regulation of double helix functional processes. In this light, a special focus is given to the quinoline compounds, acting with classical/well-known mechanisms of action (DNA intercalators or Topoisomerase inhibitors). In particular, the quinoline drugs amsacrine and camptothecin (CPT) have been studied as key lead compounds for the development of new agents with improved PK and tolerability…

medicine.drug_classAntineoplastic Agents01 natural sciences03 medical and health scienceschemistry.chemical_compoundDrug DiscoverymedicineHumansAmsacrine030304 developmental biologyCell ProliferationPharmacology0303 health sciencesDNA Intercalators G-quadruplex Topoisomerase Epigenetic targets Antiproliferative compounds SAR studiesbiologyMolecular Structure010405 organic chemistryTopoisomeraseOrganic ChemistryQuinolineGeneral MedicineDNA NeoplasmSettore CHIM/08 - Chimica Farmaceutica0104 chemical sciencesDNA-Binding ProteinsG-QuadruplexesHistonechemistryBiochemistrybiology.proteinQuinolinesHistone deacetylaseCamptothecinDNATopoisomerase inhibitormedicine.drugEuropean journal of medicinal chemistry
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Synergistic cytotoxic interactions between sodium butyrate, MG132 and camptothecin in human retinoblastoma Y79 cells.

2000

This paper studies the effects caused in human retinoblastoma Y79 cells by treatment with combinations of sodium butyrate, the inhibitor of topoisomerase I camptothecin and the inhibitor of 26S proteasome MG132. The combination of sodium butyrate and camptothecin resulted in a strong synergistic cytotoxicity, as revealed by combination indices of 0.77 and 0.52 calculated at IC(50) and IC(75). Synergistic interactions were also demonstrated for combinations of sodium butyrate and MG132, camptothecin and MG132 and for a combination of all three compounds. The cytotoxic effects observed after the combined treatments can be considered a consequence of apoptosis, as suggested by the appearance o…

medicine.drug_classCell SurvivalLeupeptinsSodiumchemistry.chemical_elementApoptosisButyrateBiologyCysteine Proteinase Inhibitorschemistry.chemical_compoundMG132Antineoplastic Combined Chemotherapy ProtocolsmedicineTumor Cells CulturedHumansheterocyclic compoundsEnzyme InhibitorsRetinoblastomaCaspase 3TopoisomeraseRetinoblastomaSodium butyrateDrug SynergismGeneral Medicinemedicine.diseaseeye diseasesEnzyme ActivationButyrateschemistryBiochemistryProto-Oncogene Proteins c-bcl-2CaspasesCancer researchbiology.proteinCamptothecinTopoisomerase I InhibitorsTumor Suppressor Protein p53CamptothecinTopoisomerase inhibitormedicine.drugTumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine
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Synthesis and biological evaluation of sphingosine kinase 2 inhibitors with anti-inflammatory activity.

2019

The synthesis of inhibitors of SphK2 with novel structural scaffolds is reported. These compounds were designed from a molecular modeling study, in which the molecular interactions stabilizing the different complexes were taken into account. Particularly interesting is that 7‐bromo‐2‐(2‐phenylethyl)‐2,3,4,5‐tetrahydro‐1,4‐epoxynaphtho[1,2‐b]azepine, which is a selective inhibitor of SphK2, does not exert any cytotoxic effects and has a potent anti‐inflammatory effect. It was found to inhibit mononuclear cell adhesion to the dysfunctional endothelium with minimal impact on neutrophil–endothelial cell interactions. The information obtained from our theoretical and experimental study can be us…

medicine.drug_classCell SurvivalNeutrophilsFísico-Química Ciencia de los Polímeros ElectroquímicaCellAnti-Inflammatory AgentsPharmaceutical ScienceSYNTHESIS01 natural sciencesPeripheral blood mononuclear cellAnti-inflammatoryANTI-INFLAMMATORY ACTIVITYchemistry.chemical_compoundStructure-Activity RelationshipDrug DiscoverymedicineCell AdhesionHuman Umbilical Vein Endothelial CellsCytotoxic T cellHumansMOLECULAR MODELINGAzepineEnzyme Inhibitors010405 organic chemistryBIOASSAYSCiencias QuímicasSphingosine Kinase 2AdhesionAzepines0104 chemical sciencesMolecular Docking Simulation010404 medicinal & biomolecular chemistrySPHK2Phosphotransferases (Alcohol Group Acceptor)medicine.anatomical_structurechemistrySPHINGOSINE KINASE 2 INHIBITORSDrug DesignCancer researchEpoxy CompoundsEndothelium VascularCIENCIAS NATURALES Y EXACTASProtein BindingArchiv der Pharmazie
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Synthesis of nucleoside and nucleotide conjugates of bile acids, and polymerase construction of bile acid-functionalized DNA.

2010

Aqueous Sonogashira cross-coupling reactions of 5-iodopyrimidine or 7-iodo-7-deazaadenine nucleosides with bile acid-derived terminal acetylenes linked via an ester or amide tether gave the corresponding bile acid–nucleoside conjugates. Analogous reactions of halogenated nucleoside triphosphates gave directly bile acid-modified dNTPs. Enzymatic incorporation of these modified nucleotides to DNA was successfully performed using Phusion polymerase for primer extension. One of the dNTPs (dCTP bearing cholic acid) was also efficient for PCR amplification.

medicine.drug_classDNA-Directed DNA PolymeraseThermococcaceaeNucleic Acid DenaturationBiochemistryPrimer extensionBile Acids and Saltschemistry.chemical_compoundmedicineNucleotidePhysical and Theoretical ChemistryPolymerasechemistry.chemical_classificationbiologyBile acidNucleotidesOrganic ChemistryCholic acidNucleosidesDNAEnzymechemistryBiochemistrybiology.proteinNucleosideDNAOrganicbiomolecular chemistry
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