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showing 10 items of 1641 documents

α-Aminoalkylphosphonates as a tool in experimental optimisation of P1 side chain shape of potential inhibitors in S1 pocket of leucine- and neutral a…

2005

Abstract The synthesis and biological activity studies of the series of structurally different α-aminoalkylphosphonates were performed in order to optimise the shape of the side chain of the potential inhibitors in S1 pocket of leucine aminopeptidase [E.C.3.4.11.1]. Analysis of a series of compounds with aromatic, aliphatic and alicyclic P1 side chains enabled to find out the structural features, optimal for that fragment of inhibitors of LAP. The most active among all investigated compounds were the phosphonic analogues of homo-tyrosine ( K i  = 120 nM) and homo-phenylalanine ( K i  = 140 nM), which even as racemic mixtures were better inhibitors in comparison with the best till now-phosph…

aminophosphonatesStereochemistryleucine aminopeptidaseOrganophosphonatesKidneyAminopeptidasesChemical synthesisAminopeptidaseLeucyl AminopeptidaseStructure-Activity RelationshipAlicyclic compoundLeucineDrug DiscoverySide chainAnimalsLeucyl aminopeptidasePharmacologychemistry.chemical_classificationBinding SitesMolecular StructureAminopeptidase NOrganic ChemistryBiological activityGeneral MedicineHydrogen-Ion Concentrationaminopeptidase NinhibitorEnzymechemistryLeucineEuropean Journal of Medicinal Chemistry
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A measuring instrument of the audience of a web site : the network analysis

1999

Marketing on the Internet upsets the traditional commercial techniques. To optimize the audience of its site, even its sales on this channel, a company needs relevant statistical data. The aim of our research is to renew the approach of Log files analyzers currently available, by showing the contributions of network analysis

analyse réseau[SHS.INFO]Humanities and Social Sciences/Library and information sciences[SHS.INFO] Humanities and Social Sciences/Library and information sciencesaudience de site web
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Procollagen C-proteinase Enhancer Stimulates Procollagen Processing by Binding to the C-propeptide Region Only*

2011

Background: Procollagen C-proteinase enhancer-1 (PCPE-1) is an extracellular glycoprotein that increases activity of certain zinc metalloproteinases involved in tissue development and repair. Results: PCPE-1 binds uniquely to the C-propeptide region of the procollagen molecule. Conclusion: PCPE-1 enhances proteolysis by binding solely to the procollagen C-propeptides. Significance: These data may lead to future applications in the development of antifibrotic therapies.

animal structuresGlycosylationBiologyBiochemistryBone morphogenetic protein 1Protein Structure SecondaryBone Morphogenetic Protein 103 medical and health scienceschemistry.chemical_compoundMetalloprotease0302 clinical medicineHumansBinding siteEnhancerMolecular Biology030304 developmental biologyCell Line TransformedGlycoproteinschemistry.chemical_classification0303 health sciencesMetalloproteinaseExtracellular Matrix ProteinsBinding Sitesintegumentary systemCell BiologyEnzymatic ProcessingFibrosisExtracellular MatrixProcollagen peptidaseCollagen Type IIIchemistryBiochemistry030220 oncology & carcinogenesisembryonic structuresEnzymologyCollagenGlycoproteinProtein Processing Post-TranslationalTriple helixThe Journal of Biological Chemistry
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Context-dependent Pax-5 repression of a PU.1/NF-κB regulated reporter gene in B lineage cells

2001

Enhancers located in the 3' end of the locus in part regulate immunoglobulin heavy chain (IgH) gene expression. One of these enhancers, HS 1,2, is developmentally regulated by DNA binding proteins like NF-kappaB, Pax-5 and the protein complex NF-alphaP in B lineage cells. Here we report that NF-alphaP is the ets protein PU.1. A glutathione-S-transferase (GST)-pulldown assay demonstrated that PU.1 can physically interact with NF-kappaB in solution. Experiments in COS cells showed that PU.1 and NF-kappaB (p50/c-Rel) can activate transcription of an enhancer linked reporter gene. The paired domain protein Pax-5 has previously been shown to repress enhancer-dependent transcription. Additional c…

animal structuresLymphomaTranscription GeneticEnhancer RNAsBiologyDNA-binding proteinMiceSOX4Genes ReporterTranscription (biology)CricetinaeProto-Oncogene ProteinsGene expressionGeneticsAnimalsCell LineageBinding siteEnhancerCells CulturedB-LymphocytesReporter geneNF-kappa BPAX5 Transcription FactorNuclear ProteinsGeneral MedicineMolecular biologyGlobinsDNA-Binding ProteinsEnhancer Elements GeneticGene Expression RegulationCOS Cellsembryonic structuresTrans-ActivatorsTranscription FactorsGene
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The Sea Urchin sns Insulator Blocks CMV Enhancer following Integration in Human Cells

2001

Insulators are a new class of genetic elements that attenuate enhancer function directionally. Previously, we characterized in sea urchin a 265-bp-long insulator, termed sns. To test insulator activity following stable integration in human cells, we placed sns between the CMV enhancer and a tk promoter up-stream of a GFP transgene of plasmid or retroviral vectors. In contrast to controls, cells transfected or transduced with insulated constructs displayed a barely detectable fluorescence. Southern blot and PCR ruled out vector rearrangement following integration into host DNA; RNase protection confirmed the enhancer blocking activity. Finally, we demonstrate that two cis-acting sequences, p…

animal structuresSea UrchinVirus IntegrationTransgeneMolecular Sequence DataBiophysicsCytomegalovirusSettore BIO/11 - Biologia MolecolareSimian virus 40BiologyTransfectionPolymerase Chain ReactionBiochemistrySodium ChannelsNAV1.8 Voltage-Gated Sodium ChannelPlasmidTumor Cells CulturedAnimalsHumansEnhancer trapDNA Polymerase Chain ReactionEnhancerBinding Sites; DNA Polymerase Chain Reaction; Recombinant Proteins; Sea Urchins;Tumor Cells Cultured; Enhancer Elements Genetic; Virus Integration;Molecular BiologyVirus IntegrationSouthern blotBinding SitesBase SequenceBinding SiteCell BiologyTransfectionRecombinant ProteinMolecular biologyRecombinant ProteinsChromatinSettore BIO/18 - GeneticaEnhancer Elements GeneticSea UrchinsDNA ViralBiochemical and Biophysical Research Communications
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Polycationic Monomeric and Homodimeric Asymmetric Monomethine Cyanine Dyes with Hydroxypropyl Functionality—Strong Affinity Nucleic Acids Binders

2021

New analogs of the commercial asymmetric monomethine cyanine dyes thiazole orange (TO) and thiazole orange homodimer (TOTO) with hydroxypropyl functionality were synthesized and their properties in the presence of different nucleic acids were studied. The novel compounds showed strong, micromolar and submicromolar affinities to all examined DNA ds-polynucleotides and poly rA–poly rU. The compounds studied showed selectivity towards GC-DNA base pairs over AT-DNA, which included both binding affinity and a strong fluorescence response. CD titrations showed aggregation along the polynucleotide with well-defined supramolecular chirality. The single dipyridinium-bridged dimer showed intercalatio…

antiproliferative activityCircular dichroismSupramolecular chiralityDimerIntercalation (chemistry)cyanine dye010402 general chemistry01 natural sciencesBiochemistryMicrobiologyArticlechemistry.chemical_compoundCell Line TumorHumansCyanineDNA bindingColoring AgentsBiologyMolecular BiologyBinding Sites010405 organic chemistrycyanine dye ; DNA binding ; RNA binding ; fluorescence ; circular dichroism ; antiproliferative activityDNARNA bindingCombinatorial chemistryQR1-502Intercalating Agents3. Good health0104 chemical sciencescircular dichroismchemistryPolynucleotideNucleic acidcyanine dye; DNA binding; RNA binding; fluorescence; circular dichroism; antiproliferative activityfluorescenceDNA
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The Putative Metal Coordination Motif in the Endonuclease Domain of Human Parvovirus B19 NS1 Is Critical for NS1 Induced S Phase Arrest and DNA Damage

2011

The non-structural proteins (NS) of the parvovirus family are highly conserved multi-functional molecules that have been extensively characterized and shown to be integral to viral replication. Along with NTP-dependent helicase activity, these proteins carry within their sequences domains that allow them to bind DNA and act as nucleases in order to resolve the concatameric intermediates developed during viral replication. The parvovirus B19 NS1 protein contains sequence domains highly similar to those previously implicated in the above-described functions of NS proteins from adeno-associated virus (AAV), minute virus of mice (MVM) and other non-human parvoviruses. Previous studies have show…

apoptotic cell deathDNA repairDNA damagevirusesAmino Acid MotifsDNA Mutational AnalysisApoptosisSpodopteraViral Nonstructural ProteinsVirus ReplicationApplied Microbiology and Biotechnology03 medical and health scienceschemistry.chemical_compound0302 clinical medicineControl of chromosome duplicationparvoviral infectionParvovirus B19 HumanAnimalsHumansMolecular BiologyEcology Evolution Behavior and SystematicsS phase030304 developmental biology0303 health sciencesbiologyParvovirushost cell DNA damagevirus diseasesHep G2 CellsCell BiologyEndonucleasesbiology.organism_classificationMolecular biology3. Good healthchemistryViral replicationS Phase Cell Cycle CheckpointsMutagenesis Site-Directed030211 gastroenterology & hepatologyDNAMinute virus of miceResearch PaperDNA DamageDevelopmental BiologyInternational Journal of Biological Sciences
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SISTEMI DI COPERTURE INNOVATIVE NEI CONTESTI ANTICHI

2014

La ricerca è indirizzata al tema delle coperture in vetro a protezione di siti archeologici. Tale scelta è stata influenzata dalle seguenti considerazioni: gli ultimi decenni sono stati caratterizzati da un incremento delle coperture trasparenti protettive; il tema delle strutture di copertura in contesti archeologici e ciò che riguarda la loro progettazione, è stato, e continua ad essere oggi, molto dibattuto tra gli esperti in tutto il mondo; la costante evoluzione tecnologica del vetro continua a incrementare le sue possibilità d’uso in architettura. Tale materiale presenta numerosi vantaggi come l’apparente leggerezza e la trasparenza ma in ambito archeologico pone problematiche che rig…

archaeological sitecontesti antichi protezione.siti archeologicivetroglaSettore ICAR/10 - Architettura Tecnicacoperture trasparentitransparent covering structureancient contexts preservation.Settore ICAR/12 - Tecnologia Dell'Architettura
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On site archaeological museums: types of protection

2011

The decision to preserve, in their original context, even the most fragile artefacts, such as floor and wall coverings and to exhibit the delicate stratigraphic or clay manufactures, has favoured the spread of archaeological museums in situ, by interventions aimed at the preservation of archaeological remains. Archaeological museums represent a particular typology capable of relating history through its ruins. Therefore, it is not a museum having typological and functional characteristics that answer to codified museum-graphical and display rules . The arrangement and the public opening of the archaeological sites in recent years have been the object of discussions, debates and interdiscipl…

archaeological sites conservation musealizationSettore ICAR/10 - Architettura TecnicaArchaeological sites Preservation Protection.
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Proteggere e Valorizzare: una buona pratica per i siti archeologici

2014

Tra i beni culturali quelli archeologici hanno più animato il dibattito culturale sul rapporto tra conservazione e loro messa in valore. La fragilità con cui la materia ci viene consegnata dalla storia, la frammentarietà del reperto, la scarsa disponibilità di risorse finanziarie, anche in relazione alla vastità del patrimonio a noi pervenuto, impongono interventi mirati e talvolta urgenti per la salvaguardia e la conservazione dei beni archeologici. Ma la sola conservazione non può però costituire l’obiettivo ultimo dell’intervento: poiché i beni archeologici rappresentano il nostro lontano passato è anche necessario recuperarne il valore e comunicarne l’identità. La conoscenza storica, st…

archaeological sites covers protective systems code of practicesiti archeologici coperture sistemi di protezione codice di praticaSettore ICAR/12 - Tecnologia Dell'Architettura
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