Search results for " Screening"

showing 10 items of 898 documents

The Translesion Polymerase Rev3L in the Tolerance of Alkylating Anticancer Drugs

2009

Temozolomide and fotemustine, representing methylating and chloroethylating agents, respectively, are used in the treatment of glioma and malignant melanoma. Because chemoresistance of these tumors is a common phenomenon, identification of the underlying mechanisms is needed. Here we show that Rev3L, the catalytic subunit of the translesion DNA polymerase zeta, mediates resistance to both temozolomide and fotemustine. Rev3L knockout cells are hypersensitive to both agents. It is remarkable that cells heterozygous for Rev3L showed an intermediate sensitivity. Rev3L is not involved in the tolerance of the toxic O6-methylguanine lesion. However, a possible role of Rev3L in the tolerance of O6-…

DNA damageApoptosisDNA-Directed DNA PolymeraseBiologyNitrosourea CompoundsCell LineMiceOrganophosphorus CompoundsREV3LTemozolomidemedicineAnimalsAP siteAntineoplastic Agents AlkylatingPolymeraseMice KnockoutPharmacologyTemozolomideBase excision repairFlow CytometryMolecular biologyDNA-Binding ProteinsDacarbazineMicroscopy FluorescenceCancer researchbiology.proteinMolecular MedicineFotemustineDNA mismatch repairDrug Screening Assays AntitumorDNA Damagemedicine.drugMolecular Pharmacology
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Photogenotoxicity of folic acid.

2013

Folic acid (FA), also named vitamin B9, is an essential cofactor for the synthesis of DNA bases and other biomolecules after bioactivation by dihydrofolate reductase (DHFR). FA is photoreactive and has been shown to generate DNA modifications when irradiated with UVA (360 nm) in the presence of DNA under cell-free conditions. To investigate the relevance of this reaction for cells and tissues, we irradiated three different cell lines (KB nasopharyngeal carcinoma cells, HaCaT keratinocytes, and a melanoma cell line) in the presence of FA and quantified cytotoxicity and DNA damage generation. The results indicate that FA is phototoxic and photogenotoxic by two different mechanisms. First, ext…

DNA damageCell SurvivalAntineoplastic AgentsBiochemistrychemistry.chemical_compoundFolic AcidPhysiology (medical)Cell Line TumorDihydrofolate reductaseHumansCell ProliferationbiologyDNA synthesisChemistrySuperoxide DismutaseCatalasePhotochemical ProcessesNuclear DNAHaCaTTetrahydrofolate DehydrogenaseMethotrexateBiochemistryDNA glycosylaseCell culturebiology.proteinFolic Acid AntagonistsDrug Screening Assays AntitumorDNADNA DamageFree radical biologymedicine
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Ligand-based discovery of novel trypanosomicidal drug-like compounds: In silico identification and experimental support

2010

Abstract Two-dimensional bond-based linear indices and linear discriminant analysis are used in this report to perform a quantitative structure–activity relationship study to identify new trypanosomicidal compounds. A database with 143 anti-trypanosomal and 297 compounds having other clinical uses, are utilized to develop the theoretical models. The best discriminant models computed using bond-based linear indices provides accuracies greater than 90 for both training and test sets. Our models identify as anti-trypanosomals five out of nine compounds of a set of already-synthesized substances. The in vitro anti-trypanosomal activity of this set against epimastigote forms of Trypanosoma cruzi…

Databases FactualMolecular modelCell SurvivalStereochemistryTrypanosoma cruziIn silicoNitro compoundQuantitative Structure-Activity RelationshipComputational biologyLigandsChemometricsDrug DiscoveryAnimalsHumansChagas DiseaseTrypanosoma cruziAmastigotePharmacologychemistry.chemical_classificationLife Cycle StagesbiologyOrganic ChemistryDiscriminant AnalysisBiological activityGeneral MedicineFibroblastsModels Theoreticalbiology.organism_classificationLinear discriminant analysisTrypanocidal AgentsHigh-Throughput Screening AssayschemistryAlgorithmsSoftwareEuropean Journal of Medicinal Chemistry
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An open-source computational and data resource to analyze digital maps of immunopeptidomes

2015

We present a novel mass spectrometry-based high-throughput workflow and an open-source computational and data resource to reproducibly identify and quantify HLA-associated peptides. Collectively, the resources support the generation of HLA allele-specific peptide assay libraries consisting of consensus fragment ion spectra, and the analysis of quantitative digital maps of HLA peptidomes generated from a range of biological sources by SWATH mass spectrometry (MS). This study represents the first community-based effort to develop a robust platform for the reproducible and quantitative measurement of the entire repertoire of peptides presented by HLA molecules, an essential step towards the de…

Databases FactualimmunopeptidomeQH301-705.5Systems biologyScienceImmunologyComputational biologyBiologyBioinformaticsMass spectrometryGeneral Biochemistry Genetics and Molecular BiologyMass Spectrometry03 medical and health sciencesResource (project management)Fragment (logic)HLA Antigenstargeted mass spectrometryHigh-Throughput Screening AssaysDIAhumanAntigenshuman leukocytes antigenBiology (General)030304 developmental biology0303 health sciencesAntigen PresentationGeneral Immunology and MicrobiologyDigital mappingGeneral Neuroscience030302 biochemistry & molecular biologyQRComputational BiologyGeneral Medicine3. Good healthTools and ResourcesHigh-Throughput Screening AssaysWorkflowTargeted mass spectrometrySWATH-MSMedicinePeptidesComputational and Systems BiologyeLife
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The cost-effectiveness of neonatal versus prenatal screening for congenital toxoplasmosis

2019

BackgroundCongenital Toxoplasmosis (CT) can have severe consequences. France, Austria, and Slovenia have prenatal screening programs whereas some other countries are considering universal screening to reduce congenital transmission and severity of infection in children. The efficiency of such programs is debated increasingly as seroprevalence among pregnant women and incidence of congenital toxoplasmosis show a steady decrease. In addition, uncertainty remains regarding the effectiveness of pre- and postnatal treatments.MethodTo identify cost-effective strategies, prenatal and neonatal screenings were compared using a decision-analytic model based on French guidelines and current knowledge …

Decision AnalysisEconomicsMaternal HealthCost-Benefit AnalysisSloveniaSocial SciencesPediatricsToxoplasmosis CongenitalPregnancy[SDV.MHEP.MI]Life Sciences [q-bio]/Human health and pathology/Infectious diseasesPrenatal DiagnosisMedicine and Health Sciences[SDV.MP.VIR] Life Sciences [q-bio]/Microbiology and Parasitology/Virology[SDV.MHEP.ME] Life Sciences [q-bio]/Human health and pathology/Emerging diseases[SDV.MHEP.ME]Life Sciences [q-bio]/Human health and pathology/Emerging diseasesQRObstetrics and Gynecology[SDV.MHEP.CSC] Life Sciences [q-bio]/Human health and pathology/Cardiology and cardiovascular systemFetal deathAustria[SDV.MP.VIR]Life Sciences [q-bio]/Microbiology and Parasitology/Virology[SDV.MHEP.MI] Life Sciences [q-bio]/Human health and pathology/Infectious diseasesMedicineEngineering and TechnologyFemaleFranceManagement EngineeringToxoplasmosis[SDV.MP.PAR] Life Sciences [q-bio]/Microbiology and Parasitology/ParasitologyResearch ArticleScienceDecision treesClinical Decision-MakingResearch and Analysis MethodsPediatric infectionsNeonatal Screening[SDV.MHEP.CSC]Life Sciences [q-bio]/Human health and pathology/Cardiology and cardiovascular systemParasitic DiseasesHumans[SDV.MP.PAR]Life Sciences [q-bio]/Microbiology and Parasitology/ParasitologyProtozoan InfectionsCost-effectiveness analysisInfant NewbornBiology and Life SciencesNeonatesModels Theoretical[SDV.MP.BAC]Life Sciences [q-bio]/Microbiology and Parasitology/BacteriologyEconomic AnalysisPregnancy ComplicationsBirthWomen's Health[SDV.MP.BAC] Life Sciences [q-bio]/Microbiology and Parasitology/BacteriologyDevelopmental Biology
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Digital holographic microscopy for diabetes screening

2016

A digital holographic microscope operating in telecentric mode could be used to diagnose diabetes and evaluate long-term glycemic control in patients with diabetes.

DiabetisMaterials sciencebusiness.industryNanotechnology02 engineering and technology021001 nanoscience & nanotechnology01 natural sciencesÒptica Aparells i instruments010309 opticsOpticsDiabetes screening0103 physical sciencesDigital holographic microscopy0210 nano-technologybusinessSPIE Newsroom
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Atom- and Bond-Based 2D TOMOCOMD-CARDD Approach and Ligand-Based Virtual Screening for the Drug Discovery of New Tyrosinase Inhibitors

2008

Two-dimensional atom- and bond-based TOMOCOMD-CARDD descriptors and linear discriminant analysis (LDA) are used in this report to perform a quantitative structure-activity relationship (QSAR) study of tyrosinase-inhibitory activity. A database of inhibitors of the enzyme is collected for this study, within 246 highly dissimilar molecules presenting antityrosinase activity. In total, 7 discriminant functions are obtained by using the whole set of atom- and bond-based 2D indices. All the LDA-based QSAR models show accuracies above 90% in the training set and values of the Matthews correlation coefficient (C) varying from 0.85 to 0.90. The external validation set shows globally good classifica…

DicumarolQuantitative structure–activity relationshipStereochemistryTyrosinaseQuantitative Structure-Activity RelationshipLigandsBiochemistryAnalytical ChemistrySmall Molecule Librarieschemistry.chemical_compoundDrug DiscoveryCluster AnalysisVirtual screeningDrug discoveryChemistryComputational BiologyDiscriminant AnalysisReproducibility of ResultsMatthews correlation coefficientLigand (biochemistry)Linear discriminant analysisCombinatorial chemistryMolecular MedicinePeptidesKojic acidBiotechnologySLAS Discovery
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Dottore, mio figlio non impara a leggere”. I Disturbi Specifici dell’Apprendimento (DSA) e il pediatra di famiglia

2015

Si parla di Disturbo Specifico di Apprendimento (DSA) quando sono presenti delle difficoltà isolate e circoscritte nella lettura (Dislessia) e/o nella scrittura (Disortografia) e/o nel calcolo (Discalculia) nonostante la presenza di adeguate capacità cognitive e opportunità scolastiche. Tali difficoltà hanno carattere evolutivo e persistente, presentandosi con diversa espressività clinica nelle varie fasi dello sviluppo. La prevalenza mondiale del disturbo si attesta tra il 5 e il 15% (DSM 5, 2013). L’incidenza è maggiore nei maschi, con un rapporto M/F stimato intorno a 2:1, 3:1 (DSM 5, 2013). In Italia la stima di prevalenza dei DSA fra i bambini in età scolare oscilla fra il 3 e il 5% (C…

Disturbi Specifici dell’Apprendimento DSA screening precoce questionari osservativiSettore MED/38 - Pediatria Generale E Specialistica
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Synthesis of N-acyl Derivatives of Aminocombretastatin A-4 and Study of their Interaction with Tubulin and Downregulation of c-Myc.

2021

11 p.-9 fig.-4 tab.

Down-RegulationAntineoplastic AgentsMicrotubule dynamicsStructure-Activity RelationshipDownregulation and upregulationMicrotubuleTubulinCell Line TumorDrug DiscoveryHumansMTT assayAminocombretastatin A-4Cell ProliferationbiologyChemistryCell growthIn vitroTubulin ModulatorsMolecular Docking SimulationTubulinc-MycBiochemistryCell cultureDocking (molecular)biology.proteinDrug Screening Assays AntitumorAnti-proliferative activityAnti-mitoticMedicinal chemistry (Shariqah (United Arab Emirates))
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Droplet-to-droplet microarray for drug screening in picoliter scale

2012

Droplet-to-droplet microarray CYP3A4 drug screening inkjet printingSettore CHIM/02 - Chimica Fisica
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