Search results for " sequence"

showing 10 items of 3643 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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Role of AxyZ Transcriptional Regulator in Overproduction of AxyXY-OprZ Multidrug Efflux System in Achromobacter Species Mutants Selected by Tobramycin

2017

ABSTRACT AxyXY-OprZ is an RND-type efflux system that confers innate aminoglycoside resistance to Achromobacter spp. We investigated here a putative TetR family transcriptional regulator encoded by the axyZ gene located upstream of axyXY-oprZ . An in-frame axyZ gene deletion assay led to increased MICs of antibiotic substrates of the efflux system, including aminoglycosides, cefepime, fluoroquinolones, tetracyclines, and erythromycin, indicating that the product of axyZ negatively regulates expression of axyXY-oprZ . Moreover, we identified an amino acid substitution at position 29 of AxyZ (V29G) in a clinical Achromobacter strain that occurred during the course of chronic respiratory tract…

0301 basic medicineAchromobacterCefepime030106 microbiologyPopulationAchromobacterMicrobial Sensitivity TestsBiologymedicine.disease_causeMicrobiology03 medical and health scienceschemistry.chemical_compoundAntibiotic resistanceBacterial ProteinsMechanisms of ResistanceDrug Resistance Multiple BacterialTobramycinmedicineHumansPharmacology (medical)TetRAmino Acid Sequence[SDV.BBM.BC]Life Sciences [q-bio]/Biochemistry Molecular Biology/Biochemistry [q-bio.BM]educationComputingMilieux_MISCELLANEOUSPharmacologyeducation.field_of_studyPseudomonas aeruginosaMembrane Transport Proteins[SDV.BBM.BM]Life Sciences [q-bio]/Biochemistry Molecular Biology/Molecular biologyGene Expression Regulation Bacterialbiology.organism_classification[SDV.MP.BAC]Life Sciences [q-bio]/Microbiology and Parasitology/BacteriologyAnti-Bacterial Agents3. Good healthInfectious DiseasesAmino Acid SubstitutionchemistryPseudomonas aeruginosaTobramycinTrans-ActivatorsEffluxGene DeletionBacterial Outer Membrane Proteinsmedicine.drugAntimicrobial Agents and Chemotherapy
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Co-existence of virulence factors and antibiotic resistance in new Klebsiella pneumoniae clones emerging in south of Italy

2018

Abstract Background Endemic presence of Klebsiella pneumoniae resistant to carbapenem in Italy has been due principally to the clonal expansion of CC258 isolates; however, recent studies suggest an ongoing epidemiological change in this geographical area. Methods 50 K. pneumoniae strains, 25 carbapenem-resistant (CR-Kp) and 25 susceptible (CS-Kp), collected from march 2014 to march 2016 at the Laboratory of Bacteriology of the Paolo Giaccone Polyclinic University hospital of Palermo, Italy, were characterized for antibiotic susceptibility and fully sequenced by next generation sequencing (NGS) for the in silico analysis of resistome, virulome, multi-locus sequence typing (MLST) and core sin…

0301 basic medicineAdultKlebsiellaGenotypeKlebsiella pneumoniae030106 microbiologyVirulenceYersiniabactinPolymorphism Single Nucleotidebeta-Lactamaseslcsh:Infectious and parasitic diseasesMicrobiology03 medical and health scienceschemistry.chemical_compoundBacterial ProteinsGenotypeDrug Resistance BacterialHumanslcsh:RC109-216TypingSicilyPhylogenyAgedAged 80 and overbiologyVirulence factorsMiddle Agedbiology.organism_classificationAnti-Bacterial AgentsBacterial Typing TechniquesKlebsiella InfectionsKlebsiella pneumoniae030104 developmental biologyInfectious DiseaseschemistryCarbapenemsCarbapenem-resistant Klebsiella pneumoniaeMultilocus sequence typingAerobactinMultilocus Sequence TypingResearch Article
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Sodium functions as a negative allosteric modulator of the oxytocin receptor

2017

Abstract The oxytocin receptor, a class A G protein coupled receptor (GPCR), is essentially involved in the physiology of reproduction. Two parameters are crucially important to support high-affinity agonist binding of the receptor: Mg2+ and cholesterol, both acting as positive modulators. Using displacement assays with a high-affinity fluorescent antagonist (OTAN-A647), we now show that sodium functions as a negative allosteric modulator of the oxytocin receptor. In membranes from HEK293 cells stably expressing the oxytocin receptor, oxytocin binding occurred with about 15-fold lower affinity when sodium chloride was increased from 0 to 300 mM, whereas antagonist binding remained largely u…

0301 basic medicineAgonistAllosteric modulatormedicine.drug_classSodiumBiophysicschemistry.chemical_elementBreast NeoplasmsSodium ChlorideOxytocinBiochemistryPotassium Chloride03 medical and health sciencesAllosteric RegulationCell Line TumormedicineHumansAmino Acid SequenceReceptorFluorescent DyesG protein-coupled receptorDose-Response Relationship DrugSequence Homology Amino AcidChemistryCell MembraneCell BiologyOxytocin receptorRecombinant ProteinsCell biologyCholesterolHEK293 Cells030104 developmental biologyOxytocinReceptors OxytocinMutagenesis Site-DirectedCalciumFemaleSequence Alignmenthormones hormone substitutes and hormone antagonistsIntracellularProtein Bindingmedicine.drugBiochimica et Biophysica Acta (BBA) - Biomembranes
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Simultaneous infection of cattle with different Anaplasma phagocytophilum variants.

2019

Anaplasma phagocytophilum is a tick-transmitted Gram-negative obligate intracellular bacterium that replicates in neutrophil granulocytes. It causes tick-borne fever in cattle and sheep. We report here the case of a 5-year-old cow from Germany with clinically overt granulocytic anaplasmosis presenting with fever, lower limb oedema and drop in milk-yield. The herd encompassed 10 animals, 8 other animals showed subclinical infection. The strains from the 9 A. phagocytophilum positive cows were molecularly characterized using ankA gene-based and multilocus sequence typing (MLST). Seven of 9 (78%) animals were infected simultaneously with different ankA variants belonging to ankA clusters I and…

0301 basic medicineAnaplasmosis030231 tropical medicineCattle DiseasesBiologymedicine.disease_causeMicrobiologyMicrobiology03 medical and health sciences0302 clinical medicineparasitic diseasesmedicineAnimalsPhylogenySubclinical infectionObligateEhrlichiosisGenetic Variationbacterial infections and mycosesmedicine.disease16S ribosomal RNAbiology.organism_classificationAnaplasma phagocytophilum030104 developmental biologyInfectious DiseasesInsect ScienceSuperinfectionHerdbacteriaMultilocus sequence typingParasitologyCattleFemaleAnaplasmosisAnaplasma phagocytophilumMultilocus Sequence TypingTicks and tick-borne diseases
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Diversity, evolution, and function of myriapod hemocyanins.

2018

Background Hemocyanin transports O2 in the hemolymph of many arthropod species. Such respiratory proteins have long been considered unnecessary in Myriapoda. As a result, the presence of hemocyanin in Myriapoda has long been overlooked. We analyzed transcriptome and genome sequences from all major myriapod taxa – Chilopoda, Diplopoda, Symphyla, and Pauropoda – with the aim of identifying hemocyanin-like proteins. Results We investigated the genomes and transcriptomes of 56 myriapod species and identified 46 novel full-length hemocyanin subunit sequences in 20 species of Chilopoda, Diplopoda, and Symphyla, but not Pauropoda. We found in Cleidogona sp. (Diplopoda, Chordeumatida) a hemocyanin-…

0301 basic medicineArthropodaEvolutionmedicine.medical_treatmentMyriapodaZoologychemical and pharmacologic phenomenacomplex mixturesHemocyaninPauropodaEvolution Molecular03 medical and health sciencesHemolymphmedicineQH359-425AnimalsAmino Acid SequenceRNA MessengerArthropodsEcology Evolution Behavior and SystematicsPhylogenyBinding SitesbiologyBase SequenceMonophenol MonooxygenaseMyriapodaGenetic VariationHemocyaninhemic and immune systemsbiology.organism_classificationRespiratory proteinOxygenProtein Subunits030104 developmental biologyHemocyaninsPhenoloxidaseSubunit diversityArthropodSymphylaCentipedeCopperResearch ArticleBMC evolutionary biology
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Virus-encoded microRNA contributes to the molecular profile of EBV-positive Burkitt lymphomas

2015

Burkitt lymphoma (BL) is an aggressive neoplasm characterized by consistent morphology and phenotype, typical clinical behavior and distinctive molecular profile. The latter is mostly driven by the MYC over-expression associated with the characteristic translocation (8;14) (q24; q32) or with variant lesions. Additional genetic events can contribute to Burkitt Lymphoma pathobiology and retain clinical significance. A pathogenetic role for Epstein-Barr virus infection in Burkitt lymphomagenesis has been suggested; however, the exact function of the virus is largely unknown. In this study, we investigated the molecular profiles (genes and microRNAs) of Epstein-Barr virus-positive and -negative…

0301 basic medicineBART6; Burkitt lymphoma; EBV; miRNA; pathogenesisEpstein-Barr Virus InfectionsHerpesvirus 4 HumanpathogenesiRNA-binding proteinRNA-Binding ProteinEpstein-Barr Virus Infectionhemic and lymphatic diseasesCluster AnalysisViralOligonucleotide Array Sequence AnalysisGeneticsBART6; Burkitt lymphoma; EBV; miRNA; pathogenesis; Burkitt Lymphoma; Cluster Analysis; Cytoskeletal Proteins; Epstein-Barr Virus Infections; Gene Expression Profiling; Gene Expression Regulation Neoplastic; Gene Expression Regulation Viral; Herpesvirus 4 Human; Host-Pathogen Interactions; Humans; Immunohistochemistry; MicroRNAs; Neoplasm Proteins; Oligonucleotide Array Sequence Analysis; Phospholipase C delta; RNA Viral; RNA-Binding Proteins; Reverse Transcriptase Polymerase Chain Reaction; ras Proteins; OncologyReverse Transcriptase Polymerase Chain ReactionpathogenesisMicrofilament ProteinsIntracellular Signaling Peptides and ProteinsBurkitt lymphomaRNA-Binding ProteinsMicroRNAPhenotypeImmunohistochemistryNeoplasm ProteinsHost-Pathogen InteractionGene Expression Regulation NeoplasticOncologyHost-Pathogen InteractionsRNA ViralHumanResearch PaperGene Expression Regulation ViralBART6BiologySettore MED/08 - Anatomia PatologicaVirusNeoplasm Protein03 medical and health sciencesEBVmicroRNACytoskeletal ProteinmedicineHumansEpstein–Barr virus infectionGenemiRNANeoplasticCluster AnalysiOligonucleotide Array Sequence AnalysiGene Expression ProfilingHerpesvirus 4ras Proteinmedicine.diseaseLymphomaGene expression profilingCytoskeletal ProteinsMicroRNAs030104 developmental biologyGene Expression Regulationras ProteinsRNABART6; EBV; burkitt lymphoma; miRNA; pathogenesisPhospholipase C deltaOncotarget
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EvalMSA: A Program to Evaluate Multiple Sequence Alignments and Detect Outliers

2016

8 páginas, 3 figuras, 2 tablas.

0301 basic medicineBiologiaComputer sciencemedia_common.quotation_subjectlcsh:EvolutionBinary numberGappinesscomputer.software_genre03 medical and health scienceslcsh:QH359-425GeneticsQuality (business)Relevance (information retrieval)Ecology Evolution Behavior and SystematicsOriginal Researchgappinessoutlier sequencecomputer.programming_languagemedia_commonSequenceMultiple sequence alignmentOutlier sequenceData scienceComputer Science ApplicationsIdentification (information)030104 developmental biologyOutliermultiple sequence alignmentMultiple sequence alignmentData miningPerlcomputerProgrames d'ordinadorEvolutionary Bioinformatics
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Role of pulmonary surfactant protein Sp-C dimerization on membrane fragmentation: An emergent mechanism involved in lung defense and homeostasis.

2020

Surfactant protein C (SP-C) is a protein present in the pulmonary surfactant system that is involved in the biophysical properties of this lipoprotein complex, but it also has a role in lung defense and homeostasis. In this article, we propose that the link between both functions could rely on the ability of SP-C to induce fragmentation of phospholipid membranes and generate small vesicles that serve as support to present different ligands to cells in the lungs. Our results using bimolecular fluorescence complementation and tunable resistive pulse sensing setups suggest that SP-C oligomerization could be the triggering event that causes membrane budding and nanovesiculation. As shown by flu…

0301 basic medicineBiophysicsBiochemistryCell Line03 medical and health sciencesBimolecular fluorescence complementation0302 clinical medicinePulmonary surfactantProtein DomainsHumansAmino Acid SequenceFragmentation (cell biology)Unilamellar LiposomesChemistryVesicleSurfactant protein CCell BiologyMembrane buddingFlow CytometryPulmonary Surfactant-Associated Protein CEndocytosisRecombinant ProteinsCell biology030104 developmental biology030228 respiratory systemMembrane proteinStructural biologyMicroscopy FluorescencePeptidomimeticsProtein MultimerizationDimerizationBiochimica et biophysica acta. Biomembranes
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The NSL Chromatin-Modifying Complex Subunit KANSL2 Regulates Cancer Stem-like Properties in Glioblastoma That Contribute to Tumorigenesis.

2016

KANSL2 is an integral subunit of the nonspecific lethal (NSL) chromatin-modifying complex that contributes to epigenetic programs in embryonic stem cells. In this study, we report a role for KANSL2 in regulation of stemness in glioblastoma (GBM), which is characterized by heterogeneous tumor stem-like cells associated with therapy resistance and disease relapse. KANSL2 expression is upregulated in cancer cells, mainly at perivascular regions of tumors. RNAi-mediated silencing of KANSL2 in GBM cells impairs their tumorigenic capacity in mouse xenograft models. In clinical specimens, we found that expression levels of KANSL2 correlate with stemness markers in GBM stem-like cell populations. M…

0301 basic medicineCHROMATINMaleCancer ResearchCarcinogenesisCellCell SeparationMice SCIDmedicine.disease_causeMiceCANCER STEM CELLMice Inbred NODHistone AcetyltransferasesOligonucleotide Array Sequence AnalysisBrain NeoplasmsNuclear ProteinsMiddle AgedFlow CytometryImmunohistochemistryChromatinUp-Regulationmedicine.anatomical_structureOncologyGene Knockdown TechniquesNeoplastic Stem CellsHeterograftsFemaleCIENCIAS NATURALES Y EXACTASAdultKANSLOtras Ciencias BiológicasBlotting WesternGLIOBLASTOMABiologyReal-Time Polymerase Chain ReactionArticleCiencias Biológicas03 medical and health sciencesCancer stem cellmedicineBiomarkers TumorGene silencingAnimalsHumansEpigeneticsAgedEmbryonic stem cell030104 developmental biologyCancer cellImmunologyCancer researchCarcinogenesisGlioblastomaCancer research
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