Search results for "ERAS"

showing 10 items of 4431 documents

Polyoxypregnanes as safe, potent, and specific ABCB1-inhibitory pro-drugs to overcome multidrug resistance in cancer chemotherapy in vitro and in vivo

2021

Multidrug resistance (MDR) mediated by ATP binding cassette subfamily B member 1 (ABCB1) is significantly hindering effective cancer chemotherapy. However, currently, no ABCB1-inhibitory drugs have been approved to treat MDR cancer clinically, mainly due to the inhibitor specificity, toxicity, and drug interactions. Here, we reported that three polyoxypregnanes (POPs) as the most abundant constituents of Marsdenia tenacissima (M. tenacissima) were novel ABCB1-modulatory pro-drugs, which underwent intestinal microbiota-mediated biotransformation in vivo to generate active metabolites. The metabolites at non-toxic concentrations restored chemosensitivity in ABCB1-overexpressing cancer cells v…

ABCC1 ATP binding cassette subfamily C member 1IC50 half maximal inhibitory concentrationMultidrug resistancePharmacologyNADPH reduced nicotinamide adenine dinucleotide phosphateF bioavailabilitychemistry.chemical_compoundPCR polymerase chain reaction0302 clinical medicineMDR multidrug resistanceECL electrochemiluminescencet1/2 elimination half-lifeLC–MS liquid chromatography coupled with mass spectrometryN.D. not detectedGeneral Pharmacology Toxicology and PharmaceuticsBBB blood–brain barriermedia_commonATF3 activating transcription factor 30303 health sciencesChemistryABC ATP-binding cassetteNMPA National Medical Products AdministrationPXR pregnane X receptorSDS-PAGE sodium dodecyl sulfate-polyacrylamide gel electrophoresisHBSS Hankʹs balanced salt solutionABCB1Combination chemotherapyProdrugMarsdenia tenacissimaCmax peak concentrationPaclitaxelGAPDH glyceraldehyde-3-phosphate dehydrogenase030220 oncology & carcinogenesisBHI brain heart infusionOriginal ArticleAUC0–∞ area under plasma concentration vs. time curveMRT mean residence timeDrugmedia_common.quotation_subjectRM1-950Vd volume of distributionABCB1 ATP binding cassette subfamily B member 1UIC-2 mouse monoclonal ABCB1 antibodyABCG2 ATP binding cassette subfamily G member 2Combination chemotherapyCYP cytochrome P450 isozymePI propidium iodideTEER transepithelial electrical resistance03 medical and health sciencesPBS phosphate buffer salineFBS fetal bovine serumDox doxorubicinIn vivoPOP polyoxypregnanemedicine030304 developmental biologyEVOM epithelial tissue voltohmmeterTmax time for peak concentrationCancerLBE lowest binding energyPE phycoerythrinmedicine.diseaseMultiple drug resistancePolyoxypregnanePapp apparent permeabilityN.A. not applicableCancer cellH&E hematoxylin and eosinMDR1a multidrug resistance protein 1aTherapeutics. PharmacologyqPCR quantitative PCRM. tenacissima Marsdenia tenacissimaCL clearanceSD standard derivationActa Pharmaceutica Sinica B
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Erwinia piriflorinigrans sp. nov., a novel pathogen that causes necrosis of pear blossoms

2010

Eight Erwinia strains, isolated from necrotic pear blossoms in València, Spain, were compared with reference strains of Erwinia amylovora and Erwinia pyrifoliae, both of which are pathogenic to species of pear tree, and to other species of the family Enterobacteriaceae using a polyphasic approach. Phenotypic analyses clustered the novel isolates into one phenon, distinct from other species of the genus Erwinia, showing that the novel isolates constituted a homogeneous phenotypic group. Rep-PCR profiles, PCR products obtained with different pairs of primers and plasmid contents determined by restriction analysis showed differences between the novel strains and reference strains of E. amylovo…

AD-HOC-COMMITTEEBACTERIALFIRE BLIGHT PATHOGENErwiniaPolymerase Chain ReactionErwinia pyrifoliaePyrusRNA Ribosomal 16SCluster Analysis[SDV.BDD]Life Sciences [q-bio]/Development BiologyPhylogenyNESTED-PCRBase Composition0303 health sciencesPEARbiologyPhylogenetic treeNucleic Acid Hybridizationfood and beveragesGeneral MedicineEnterobacteriaceaeBacterial Typing TechniquesTHERMAL-DENATURATIONPlasmidsDNA BacterialGenotypeMolecular Sequence DataDNA RibosomalMicrobiologyMicrobiology03 medical and health sciencesBacterial ProteinsPhylogeneticsDEOXYRIBONUCLEIC-ACIDEcology Evolution Behavior and SystematicsPlant Diseases030304 developmental biologyIDENTIFICATIONSEQUENCES030306 microbiologyAMYLOVORASequence Analysis DNADNARibosomal RNAbiochemical phenomena metabolism and nutrition16S ribosomal RNAbiology.organism_classificationMolecular TypingSpainErwiniabacteria
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Statins and the squalene synthase inhibitor zaragozic acid stimulate the non-amyloidogenic pathway of amyloid-beta protein precursor processing by su…

2010

Cholesterol-lowering drugs such as statins influence the proteolytic processing of the amyloid-beta protein precursor (AbetaPP) and are reported to stimulate the activity of alpha-secretase, the major preventive secretase of Alzheimer's disease. Statins can increase the alpha-secretase activity by their cholesterol-lowering properties as well as by impairment of isoprenoids synthesis. In the present study, we elucidate the contribution of these pathways in alpha-secretase activation. We demonstrate that zaragozic acid, a potent inhibitor of squalene synthase which blocks cholesterol synthesis but allows synthesis of isoprenoids, also stimulates alpha-secretase activity. Treatment of human n…

ADAM10Blotting Westernchemistry.chemical_compoundSqualeneADAM10 ProteinAmyloid beta-Protein PrecursorCell Line TumormedicineHumansLovastatinRNA Small InterferingProtein precursorLuciferasesLipid raftNeuronsbiologyATP synthaseChemistryReverse Transcriptase Polymerase Chain ReactionTerpenesGeneral NeuroscienceAnticholesteremic AgentsCell MembraneMembrane ProteinsTricarboxylic AcidsZaragozic acidGeneral MedicineBridged Bicyclo Compounds HeterocyclicEnzyme ActivationPsychiatry and Mental healthClinical PsychologyADAM ProteinsCholesterolFarnesyl-Diphosphate FarnesyltransferaseBiochemistrybiology.proteinlipids (amino acids peptides and proteins)LovastatinGeriatrics and GerontologyAmyloid Precursor Protein SecretasesHydroxymethylglutaryl-CoA Reductase InhibitorsAmyloid precursor protein secretasemedicine.drugJournal of Alzheimer's disease : JAD
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Abundance of narG , nirS , nirK , and nosZ Genes of Denitrifying Bacteria during Primary Successions of a Glacier Foreland

2006

ABSTRACT Quantitative PCR of denitrification genes encoding the nitrate, nitrite, and nitrous oxide reductases was used to study denitrifiers across a glacier foreland. Environmental samples collected at different distances from a receding glacier contained amounts of 16S rRNA target molecules ranging from 4.9 × 10 5 to 8.9 × 10 5 copies per nanogram of DNA but smaller amounts of narG , nirK , and nosZ target molecules. Thus, numbers of narG , nirK , nirS , and nosZ copies per nanogram of DNA ranged from 2.1 × 10 3 to 2.6 × 10 4 , 7.4 × 10 2 to 1.4 × 10 3 , 2.5 × 10 2 to 6.4 × 10 3 , and 1.2 × 10 3 to 5.5 × 10 3 , respectively. The densities of 16S rRNA genes per gram of soil increased with…

ALPINE DEVELOPMENTDNA BacterialglacierNitrite ReductasesDenitrificationNitrogenDenitrification pathwayDIVERSITYBiologyNitrate ReductasePolymerase Chain ReactionApplied Microbiology and BiotechnologyCOLONIZATIONMicrobial EcologyDenitrifying bacteriaRNA Ribosomal 16SBotanyIce CoverMICROBIAL COMMUNITIESGlacier forelandPoaPrimary successionEcosystemSoil Microbiology[SDV.EE]Life Sciences [q-bio]/Ecology environmentRhizosphereBacteriaBase SequenceEcologyRHIZOSPHEREQUANTIFICATIONNitrite reductaseSOILSRNA BacterialGenes BacterialAustriaOxidoreductasesSoil microbiologyFood ScienceBiotechnologyApplied and Environmental Microbiology
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Metabolic signatures across the full spectrum of non-alcoholic fatty liver disease.

2022

Funder: European Commission

ALTtype 2 diabetes mellitusROC receiving operator characteristicaspartate aminotransferaseHSDLDL low-density lipoproteinUHPLC ultrahigh-performance liquid chromatographyROCHCCNon-alcoholic steatohepatitisGCPCANASHGastroenterology2-HB 2-hydroxybutanoic acid; 3-HB 3-hydroxybutanoic acid; ALT alanine aminotransferase; AST aspartate aminotransferase; CE cholesterol ester; Cer ceramide; FFA free fatty acid; FLIP Fatty Liver Inhibition of Progression; Fibrosis; GC gas chromatography; HCC hepatocellular carcinoma; HSD honest significant difference; LC lipid cluster; LDL low-density lipoprotein; LM lipid and metabolite; LMC lipid metabolite and clinical variable; LPC lysophosphatidylcholine; Lipidomics; Mass spectrometry; Metabolomics; NAFL non-alcoholic fatty liver; NAFLD non-alcoholic fatty liver disease; NAS NASH activity score; NASH non-alcoholic steatohepatitis; NIDDK NASH-CRN National Institute of Digestive Diseases and Kidney NASH Clinical Research Network; NRR non-rejection rate; Non-alcoholic steatohepatitis; PC(O) ether PC; PC phosphatidylcholine; PCA principal component analysis; PE phosphatidylethanolamine; QTOFMS quadrupole-time-of-flight mass spectrometry; ROC receiving operator characteristic; SAF steatosis activity and fibrosis; SM sphingomyelin; T2DM type 2 diabetes mellitus; TG triacylglycerol; UHPLC ultrahigh-performance liquid chromatographySAFSAF steatosis activity and fibrosisLM lipid and metabolitehonest significant differenceHSD honest significant differenceTG triacylglycerolnon-rejection ratecholesterol esterPCPEGC gas chromatographyfree fatty acidFLIPNASH non-alcoholic steatohepatitisNIDDK NASH-CRN National Institute of Digestive Diseases and Kidney NASH Clinical Research NetworkBIOMARKERST2DMPE phosphatidylethanolamineLDLlipidNAFLDFFA free fatty acid2-HBMetabolomicsNAFL non-alcoholic fatty liverLMCphosphatidylcholineScience & TechnologySM sphingomyelinGastroenterology & HepatologyMass spectrometryactivitynutritional and metabolic diseasesT2DM type 2 diabetes mellitusACIDSreceiving operator characteristicdigestive system diseasesquadrupole-time-of-flight mass spectrometryLC lipid clusterlow-density lipoproteinNAS2-HB 2-hydroxybutanoic acidNAS NASH activity scoreQTOFMSether PCNRRSCORING SYSTEMprincipal component analysisgas chromatographyLC2-hydroxybutanoic acidPROGRESSIONAST aspartate aminotransferaseLMPC phosphatidylcholinePC(O)MARKERSUHPLCsteatosisTOOLImmunology and AllergyINSULIN-RESISTANCECerSMFatty Liver Inhibition of Progressionhepatocellular carcinoma2-HB 2-hydroxybutanoic acid NIDDK NASH-CRN National Institute of Digestive Diseases and Kidney NASH Clinical Research Network NRR non-rejection rate Non-alcoholic steatohepatitis PC(O) ether PC PC phosphatidylcholine PCA principal component analysis PE phosphatidylethanolamine QTOFMS quadrupole-time-of-flight mass spectrometry ROC receiving operator characteristic SAF steatosis activity and fibrosis SM T2DM type 2 diabetes mellitus TG triacylglycerol UHPLC ultrahigh-performance liquid chromatographyultrahigh-performance liquid chromatographyCELPC3-HBNAFLnon-alcoholic fatty liverTGtriacylglycerolNRR non-rejection rateLife Sciences & BiomedicineNAFLD non-alcoholic fatty liver diseaseFLIP Fatty Liver Inhibition of Progressionalanine aminotransferasemetaboliteCer ceramideCE cholesterol estersphingomyelinlysophosphatidylcholineand fibrosisALT alanine aminotransferaseInternal MedicineceramideNational Institute of Digestive Diseases and Kidney NASH Clinical Research NetworkAST3-HB 3-hydroxybutanoic acidQTOFMS quadrupole-time-of-flight mass spectrometryPCA principal component analysisLPC lysophosphatidylcholineHepatologynon-alcoholic fatty liver diseaseand clinical variablePC(O) ether PC3-hydroxybutanoic acidFibrosisNASH activity scoreNIDDK NASH-CRNlipid clusterlipid and metabolitephosphatidylethanolamineLipidomicsLMC lipid metabolite and clinical variableFFAHCC hepatocellular carcinomaJHEP reports : innovation in hepatology
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Cannabinoid type 1 receptor modulates intestinal propulsion by an attenuation of intestinal motor responses within the myenteric part of the peristal…

2007

Cannabinoid-1 (CB1) receptor activation affects gastrointestinal propulsion in vivo. It was our aim to further characterize the involved myenteric mechanisms in vivo and in vitro. In CB1(-/-) mice and wild-type littermates we performed in vivo transit experiments by charcoal feeding and in vitro electrophysiological recordings in mouse small intestinal smooth muscle. Ascending neuronal contraction (ANC) following electrical field stimulation was studied in rat ileum in a partitioned organ bath separating the aboral stimulation site from the oral recording site. The knockout animals displayed an accelerated upper gastrointestinal transit compared to control animals. The CB1 receptor antagoni…

AM251Malemedicine.medical_specialtyCannabinoid receptorPhysiologyPolyunsaturated Alkamidesmedicine.medical_treatmentNeuromuscular JunctionMotilityStimulationArachidonic AcidsBiologyNeuromuscular junctionMembrane PotentialsMiceOrgan Culture TechniquesPiperidinesReceptor Cannabinoid CB1Internal medicineCannabinoid Receptor ModulatorsReflexmedicineAnimalsRNA MessengerIntestinal MucosaRats WistarReceptorMice KnockoutMyoelectric Complex MigratingEndocrine and Autonomic SystemsReverse Transcriptase Polymerase Chain ReactionGastroenterologyMuscle SmoothEndocannabinoid systemElectric StimulationRatsIntestinesEndocrinologymedicine.anatomical_structurePyrazolesPeristalsisCannabinoidmedicine.drugEndocannabinoidsNeurogastroenterology and motility : the official journal of the European Gastrointestinal Motility Society
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Study of molecular mechanisms of stress response in Oenococcus oeni and implementation of tools for the functional exploration of enological genes

2015

O. oeni is responsible for wine malolactic fermentation. As any organism, O. oeni tries to adapt its physiology to environmental fluctuations by producing Hsp proteins encoded by the hsp genes. In O. oeni, CtsR is currently the only regulator of hsp genes. As an alternative to the lack of genetic tool, with the goal of understanding the mechanisms of O. oeni stress response, we developed a new expression vector, the pSIPSYN, to produce antisense RNA targeting of hsp18 mRNA. The synthesis of hsp18 asRNA leads to the decrease in the protein level of Lo18 and induced a loss of cultivability after heat or acid shock showing for the first time in vivo involvement of Lo18 in thermotolerance and a…

ARN antisens et estérases EstA2 & EstA7[SDV.AEN] Life Sciences [q-bio]/Food and NutritionStress responseSHsp Lo18Transcriptionnal repressor CtsRAntisense RNA and esterases EstA2 & EstA7Réponse au stressRégulateur transcriptionnel CtsROeonococcus oeni[SDV.BBM.BM] Life Sciences [q-bio]/Biochemistry Molecular Biology/Molecular biology
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Inducible ASABF-Type Antimicrobial Peptide from the Sponge Suberites domuncula: Microbicidal and Hemolytic Activity in Vitro and Toxic Effect on Moll…

2011

Since sponges, as typical filter-feeders, are exposed to a high load of attacking prokaryotic and eukaryotic organisms, they are armed with a wide arsenal of antimicrobial/cytostatic low-molecular-weight, non-proteinaceous bioactive compounds. Here we present the first sponge agent belonging to the group of ASABF-type antimicrobial peptides. The ASABF gene was identified and cloned from the demospongeSuberites domuncula. The mature peptide, with a length of 64 aa residues has a predicted pI of 9.24, and comprises the characteristic CSαβ structural motif. Consequently, the S. domuncula ASABF shares high similarity with the nematode ASABFs ; it is distantly related to the defensins. The recom…

ASABFAntimicrobial peptidesGastropodaMolecular Sequence DataPharmaceutical SciencePeptideMicrobial Sensitivity TestsGram-Positive BacteriaReal-Time Polymerase Chain ReactionArticleMicrobiology03 medical and health sciencesantimicrobial peptidesAnti-Infective AgentsSequence Analysis ProteinDrug DiscoveryAnimalsBittium sp.Structural motiflcsh:QH301-705.5Pharmacology Toxicology and Pharmaceutics (miscellaneous)spongesPhylogeny030304 developmental biologychemistry.chemical_classification0303 health sciencesbiology030306 microbiologyEffectorHemolytic AgentsapoptosisGeologyBittium spsponges; <em>Suberites domuncula</em>; ASABF; antimicrobial peptides; apoptosis; <em>Bittium</em> sp.biology.organism_classificationSuberites domunculasponges ; Suberites domuncula ; ASABF ; antimicrobial peptides ; apoptosis ; Bittium sp.Recombinant ProteinsSuberites domunculaSpongeEnzymelcsh:Biology (General)chemistryMolluscaSuberitesSuberitesAntimicrobial Cationic PeptidesMarine Drugs
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Selective downregulation of the MDR1 gene product in Caco-2 cells by stable transfection to prove its relevance in secretory drug transport.

2005

Considerable interest is focused on overcoming multidrug resistance (MDR) in cancer chemotherapy. The in vitro experiments to characterize P-glycoprotein's (P-gp) function and to decrease its effects have led to a variety of strategies such as addition of competitors or supplementation of the medium with oligonucleotides complementary to the 5'-end of the MDR1-mRNA. For the Caco-2 cell line, an in vitro model for absorption screening, expressing multiple transporters including P-gp, which pumps substances back into the apical solution, P-gp activity might mask other relevant transport proteins' activity. The objective of the present study was to construct a Caco-2 subline with reduced P-gp …

ATP Binding Cassette Transporter Subfamily BTime FactorsPharmaceutical ScienceDown-RegulationBiologyTransfectionPermeabilityPropanolaminesDownregulation and upregulationDrug DiscoveryHumansNorthern blotOligonucleotideReverse Transcriptase Polymerase Chain ReactionElectroporationBiological TransportTransfectionFlow CytometryMolecular biologyIn vitroTransport proteinClone CellsMutagenesis InsertionalVerapamilCell cultureMolecular MedicineCaco-2 CellsGenes MDRMolecular pharmaceutics
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A melanocortin 1 receptor (MC1R) gene polymorphism is useful for authentication of Massese sheep dairy products

2011

Massese is an Italian sheep breed, with black or grey coat colour, mainly reared in the Tuscany and Emilia Romagna regions. Recently, the emerging interests in this breed have resulted in the production of Pecorino cheese obtained with only Massese milk. In order to be profitable, this marketing link between Massese breed and its products should be defended against fraudsters who could include milk of other sheep breeds or cow milk in Massese labelled productions. To identify the genetic factors affecting coat colour in sheep, we have recently analysed the melanocortin 1 receptor (MC1R) gene and identified several single nucleotide polymorphisms (SNPs). In this work, as a first step to set …

AUTHENTICATION OF FOOD PRODUCTSCoatVeterinary medicineSNPFood ContaminationSingle-nucleotide polymorphismBiologyPolymerase Chain ReactionPolymorphism Single NucleotideSensitivity and SpecificityMASSESECow milkSettore AGR/17 - Zootecnica Generale E Miglioramento GeneticoGene FrequencySpecies SpecificityCheesePolymorphism (computer science)MC1RAnimalsAlleleGeneticsSheepfood and beveragesDNAGeneral MedicineBreedMilkFemaleAnimal Science and ZoologyDairy Productsauthentication Massese MC1R mono-breed products sheep breeds SNPReceptor Melanocortin Type 1DAIRY SHEEPPolymorphism Restriction Fragment LengthMc1r geneFood ScienceMelanocortin 1 receptor
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