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showing 10 items of 10735 documents

Molecular docking-based design and development of a highly selective probe substrate for UDP-glucuronosyltransferase 1A10

2018

Intestinal and hepatic glucuronidation by the UDP-glucuronosyltransferases (UGTs) greatly affect the bioavailability of phenolic compounds. UGT1A10 catalyzes glucuronidation reactions in the intestine, but not in the liver. Here, our aim was to develop selective, fluorescent substrates to easily elucidate UGT1A10 function. To this end, homology models were constructed and used to design new substrates, and subsequently, six novel C3-substituted (4-fluorophenyl, 4-hydroxyphenyl, 4-methoxyphenyl, 4-(dimethylamino)phenyl, 4-methylphenyl, or triazole) 7-hydroxycoumarin derivatives were synthesized from inexpensive starting materials. All tested compounds could be glucuronidated to nonfluorescen…

0301 basic medicineMutantGlucuronidationPharmaceutical ScienceUGT1A10030226 pharmacology & pharmacySubstrate Specificity7-hydroxycoumarin derivativechemistry.chemical_compound0302 clinical medicineDrug DiscoveryCRYSTAL-STRUCTUREGlucuronosyltransferaseta116ta317AFFINITYchemistry.chemical_classificationChemistry3. Good healthMolecular ImagingMolecular Docking Simulation7-hydroxycoumarin317 Pharmacyin silicoMolecular MedicinefluorescenceUDP-glucuronosyltransferaseEXPRESSIONENZYMEStereochemistryIn silicoKineticsFLUORESCENT-PROBETriazoleta311103 medical and health sciencesGlucuronidesMicrosomesXENOBIOTICSHumansUmbelliferonesFluorescent DyesGLUCURONIDATIONta1182glucuronidationfluoresenssiSubstrate (chemistry)drug metabolism030104 developmental biologyEnzymeDRUG-METABOLISMDrug DesignMolecular ProbesMutationMutagenesis Site-DirectedORAL BIOAVAILABILITYDrug metabolism
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Different rates of spontaneous mutation of chloroplastic and nuclear viroids as determined by high-fidelity ultra-deep sequencing

2017

[EN] Mutation rates vary by orders of magnitude across biological systems, being higher for simpler genomes. The simplest known genomes correspond to viroids, subviral plant replicons constituted by circular non-coding RNAs of few hundred bases. Previous work has revealed an extremely high mutation rate for chrysanthemum chlorotic mottle viroid, a chloroplastreplicating viroid. However, whether this is a general feature of viroids remains unclear. Here, we have used high-fidelity ultra-deep sequencing to determine the mutation rate in a common host (eggplant) of two viroids, each representative of one family: the chloroplastic eggplant latent viroid (ELVd, Avsunviroidae) and the nuclear pot…

0301 basic medicineMutation rateChloroplastsViroidvirusesPospiviroidaeArtificial Gene Amplification and ExtensionPlant ScienceSelf-CleavageVirus ReplicationBiochemistryPolymerase Chain ReactionGenomeDatabase and Informatics MethodsSequencing techniquesRibozymeNucleic AcidsRibozymesBiology (General)GeneticsHigh-Throughput Nucleotide Sequencingfood and beveragesRNA sequencingViroidsEnzymesAvsunviroidaeDeletion MutationVirusesPhysical SciencesRNA ViralIn-VivoSequence AnalysisResearch ArticleSubstitution MutationHammerhead RibozymesQH301-705.5Materials by StructureBioinformaticsEvolutionMaterials ScienceImmunologyPlant PathogensGenerationReplicationBiologyMicrobiology03 medical and health sciencesSequence Motif AnalysisVirologyGeneticsSolanum melongenaRNA-PolymeraseMolecular BiologyPotato spindle tuber viroidPlant DiseasesMatter030102 biochemistry & molecular biologyPoint mutationOrganismsBiology and Life SciencesProteinsRNAReverse Transcriptase-Polymerase Chain ReactionRC581-607Plant Pathologybiology.organism_classificationVirologyResearch and analysis methodsMolecular biology techniques030104 developmental biologyMutagenesisOligomersMutationEnzymologyRNAMotifParasitologyImmunologic diseases. AllergyPLOS Pathogens
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Interleukin 1α: a comprehensive review on the role of IL-1α in the pathogenesis and treatment of autoimmune and inflammatory diseases.

2021

Abstract The interleukin (IL)-1 family member IL-1α is a ubiquitous and pivotal pro-inflammatory cytokine. The IL-1α precursor is constitutively present in nearly all cell types in health, but is released upon necrotic cell death as a bioactive mediator. IL-1α is also expressed by infiltrating myeloid cells within injured tissues. The cytokine binds the IL-1 receptor 1 (IL-1R1), as does IL-1β, and induces the same pro-inflammatory effects. Being a bioactive precursor released upon tissue damage and necrotic cell death, IL-1α is central to the pathogenesis of numerous conditions characterized by organ or tissue inflammation. These include conditions affecting the lung and respiratory tract, …

0301 basic medicineMyocarditisil-1βmedicine.medical_treatmentAutoimmunity Cancer Cytokines IL-1 IL-1αIL-1β Inflammation Interleukin 1 Receptor Antagonist Protein Receptors Interleukin-1 SARS-CoV-2 COVID-19 Interleukin-1alpha Humansil-1αImmunologyreceptorsInflammationmedicine.disease_causeAutoimmunityPathogenesis03 medical and health sciences0302 clinical medicineSettore MED/38 - Pediatria Generale E Specialisticail-1Interleukin-1alphamedicinecancerImmunology and AllergyHumans030203 arthritis & rheumatologyAnakinrabusiness.industrySARS-CoV-2autoimmunityInterleukinCOVID-19Receptors Interleukin-1medicine.diseasecytokinesRilonaceptInterleukin 1 Receptor Antagonist Protein030104 developmental biologyCytokineinflammationImmunologyautoimmunity; cancer; cytokines; il-1; il-1α; il-1β; inflammation; humans; interleukin 1 receptor antagonist protein; receptors interleukin-1; SARS-COV-2; COVID-19; interleukin-1alphamedicine.symptombusinessinterleukin-1medicine.drugAutoimmunity reviews
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ASO Author Reflections: How Long will We Perform Lymphadenectomy in Endometrial Cancer Patients?

2022

Abstract Objectives To compare survival and progression outcomes between 2 nodal assessment approaches in patients with nonbulky stage IIIC endometrial cancer (EC). Methods Patients with stage IIIC EC treated at 2 institutions were retrospectively identified. At 1 institution, a historical series (2004–2008) was treated with systematic pelvic and para-aortic lymphadenectomy (LND cohort). At the other institution, more contemporary patients (2006–2013) were treated using a sentinel lymph node algorithm (SLN cohort). Outcomes (hazard ratios [HRs]) within the first 5 years after surgery were compared between cohorts using Cox models adjusted for type of adjuvant therapy. Results The study incl…

0301 basic medicineN.A.medicine.medical_specialtymedicine.medical_treatmentSentinel lymph nodeMEDLINEArticleEndometrial CancerDisease-Free Survival03 medical and health sciences0302 clinical medicineLymphadenectomy Endometrial CancerSurgical oncologyAdjuvant therapymedicineHumansStage IIICNeoplasm InvasivenessProgression-free survivalLymph nodeAgedNeoplasm StagingRetrospective Studiesbusiness.industryEndometrial cancerGeneral surgeryObstetrics and GynecologyLymphadenectomymedicine.diseaseEndometrial Neoplasms030104 developmental biologymedicine.anatomical_structureTreatment OutcomeSettore MED/40 - GINECOLOGIA E OSTETRICIASentinel nodeOncology030220 oncology & carcinogenesisLymphatic MetastasisDisease ProgressionLymph Node ExcisionFemaleSurgeryLymphadenectomySentinel Lymph NodebusinessAlgorithmChemoradiotherapyAlgorithmsAnnals of Surgical Oncology
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Neanderthal behaviour, diet, and disease inferred from ancient DNA in dental calculus

2017

Weyrich, Laura S. et al.

0301 basic medicineNeanderthalTime Factorsved/biology.organism_classification_rank.speciesneanderthal01 natural sciencesGenomeBelgiumWoolly rhinocerosCalculusDental CalculusHistory AncientNeanderthalsMultidisciplinarygeography.geographical_feature_categoryStomachCarnivoryMouflonIntestinesCavesHealthVegetarians010506 paleontologyMeatPan troglodytesBiologyMethanobrevibacter03 medical and health sciencesFood PreferencesCavebiology.animalAnimalsHumansDNA AncientSymbiosisancient DNAPerissodactyla0105 earth and related environmental sciencesgeographyMouthSheepved/biologyPenicilliumEnterocytozoonbiology.organism_classificationDietstomatognathic diseases030104 developmental biologyAncient DNAMetagenomicsSpainMethanobrevibacter oralisGenome Bacterial
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Genetic associations at 53 loci highlight cell types and biological pathways relevant for kidney function

2016

Reduced glomerular filtration rate defines chronic kidney disease and is associated with cardiovascular and all-cause mortality. We conducted a meta-analysis of genome-wide association studies for estimated glomerular filtration rate (eGFR), combining data across 133,413 individuals with replication in up to 42,166 individuals. We identify 24 new and confirm 29 previously identified loci. Of these 53 loci, 19 associate with eGFR among individuals with diabetes. Using bioinformatics, we show that identified genes at eGFR loci are enriched for expression in kidney tissues and in pathways relevant for kidney development and transmembrane transporter activity, kidney structure, and regulation o…

0301 basic medicineNephrologyGenetics and Molecular Biology (all)estimated glomerular filtration rateestimated glomerular filtration rate chronic kidney disease genetic determinantsGeneral Physics and AstronomyKidney developmentGenome-wide association studyBiochemistrySettore MED/14 - NEFROLOGIARenal InsufficiencyChronicGeneticsAGEN Consortiumddc:616education.field_of_studyKidneyStage renal-diseaseMultidisciplinaryGenome-wide associationCHARGe-Heart Failure GroupGene Expression Regulation; Genome-Wide Association Study; Genotype; Humans; Renal Insufficiency Chronic; Genetic Predisposition to Disease; Biochemistry Genetics and Molecular Biology (all); Chemistry (all); Physics and Astronomy (all)QChemistry (all)MetaanalysisGene Expression Regulation; Genetic Predisposition to Disease; Genome-Wide Association Study; Genotype; Humans; Renal Insufficiency Chronic/geneticsBiological sciencesSerum creatininemedicine.anatomical_structureEfficientRonyons -- FisiologiaHypertensionICBP ConsortiumTransmembrane transporter activitygenetic association loci kidney functionCARDIOGRAMHumanmedicine.medical_specialtyGenotypeSciencePopulationRenal functionECHOGen ConsortiumReplicationBiologyEnvironmentResearch SupportGeneral Biochemistry Genetics and Molecular BiologyN.I.H.genetic determinants03 medical and health sciencesPhysics and Astronomy (all)GENOME-WIDE ASSOCIATION ; FALSE DISCOVERY RATES ; STAGE RENAL-DISEASE ; SERUM CREATININE ; METAANALYSIS ; VARIANTS ; INDIVIDUALS ; POPULATION ; RISK ; HYPERTENSIONKidney functionResearch Support N.I.H. ExtramuralInternal medicineMD MultidisciplinarymedicineGeneticsJournal ArticleHumanseGFRcrea; eGFRcysGenetic Predisposition to Diseaseddc:610GenetikRenal Insufficiency ChronicMortalityeducationddc:613Biochemistry Genetics and Molecular Biology (all)urogenital systemIndividualsExtramuralGeneral Chemistryta3121medicine.diseaseR1030104 developmental biologyGene Expression RegulationBiochemistry Genetics and Molecular Biology (all); Chemistry (all); Physics and Astronomy (all)570 Life sciences; biologyGenèticachronic kidney diseaseKidney diseaseGenome-Wide Association StudyMeta-Analysis
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Impairment of learning and memory performances induced by BPA Evidences from the literature of a MoA mediated through an ED

2018

International audience; Many rodent studies and a few non-human primate data report impairments of spatial and non-spatial memory induced by exposure to bisphenol A (BPA), which are associated with neural modifications, particularly in processes involved in synaptic plasticity. BPA-induced alterations involve disruption of the estrogenic pathway as established by reversal of BPA-induced effects with estrogenic receptor antagonist or by interference of BPA with administered estradiol in ovariectomized animals. Sex differences in hormonal impregnation during critical periods of development and their influence on maturation of learning and memory processes may explain the sexual dimorphism obs…

0301 basic medicineNervous systemNervous systemendocrine systemmedicine.drug_classEndocrine disruptionBiologyEndocrine DisruptorsBiochemistryLearning and memory03 medical and health scienceschemistry.chemical_compound0302 clinical medicineEndocrinologyMESH: PhenolsBisphenol APhenolsMemorymedicineMESH: Benzhydryl CompoundsAnimalsHumansBenzhydryl compoundsMESH: MemoryBenzhydryl CompoundsMode of actionMolecular BiologyBehavior Animalurogenital systemBrainCognitionEnvironmental exposureEnvironmental ExposureReceptor antagonistMESH: Endocrine Disruptors030104 developmental biologymedicine.anatomical_structurechemistrySynaptic plasticity[SDV.SPEE]Life Sciences [q-bio]/Santé publique et épidémiologieSignal transductionNeuroscience030217 neurology & neurosurgeryhormones hormone substitutes and hormone antagonists
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Allopregnanolone augments epileptiform activity of an in-vitro mouse hippocampal preparation in the first postnatal week.

2019

Abstract In the immature brain the neurotransmitter γ-amino butyric acid (GABA) mediates a membrane depolarization and can contribute to both, inhibition and excitation. Therefore the consequences of a positive modulation of GABA(A) receptors by neurosteroids on epileptiform activity are hard to predict. In order to analyze whether neurosteroids attenuate or exaggerate epileptiform activity in the immature brain, we investigated the effect of the neurosteroid allopregnanolone on epileptiform activity in an in-toto hippocampus preparation of early postnatal mice (postnatal days 4–7) using field potential recordings. These in-vitro experiments revealed that 0.5 μmol/L allopregnanolone had no …

0301 basic medicineNeuroactive steroidPatch-Clamp TechniquesPregnanoloneHippocampal formationHippocampusMembrane Potentials03 medical and health scienceschemistry.chemical_compoundMice0302 clinical medicineAnimalsPicrotoxinIctalGABA-A Receptor AntagonistsNeurotransmitterGABAA receptorAllopregnanoloneDepolarizationnervous system diseases030104 developmental biologynervous systemNeurologychemistryGABAergicNeurology (clinical)Neuroscience030217 neurology & neurosurgeryEpilepsy research
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Asymmetry Between Pre- and Postsynaptic Transient Nanodomains Shapes Neuronal Communication.

2020

Synaptic transmission and plasticity are shaped by the dynamic reorganization of signaling molecules within pre- and postsynaptic compartments. The nanoscale organization of key effector molecules has been revealed by single-particle trajectory (SPT) methods. Interestingly, this nanoscale organization is highly heterogeneous. For example, presynaptic voltage-gated calcium channels (VGCCs) and postsynaptic ligand-gated ion channels such as AMPA receptors (AMPARs) are organized into so-called nanodomains where individual molecules are only transiently trapped. These pre- and postsynaptic nanodomains are characterized by a high density of molecules but differ in their molecular organization an…

0301 basic medicineNeuronsCell signalingNeuronal PlasticityVoltage-dependent calcium channelEffectorChemistryGeneral NeuroscienceAMPA receptorNeurotransmissionSynaptic Transmission03 medical and health sciencesMolecular dynamics030104 developmental biology0302 clinical medicinePostsynaptic potentialSynapsesBiophysicsHumansReceptors AMPA030217 neurology & neurosurgeryIon channelTrends in neurosciences
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Ochratoxin A and T-2 Toxin Induce Clonogenicity and Cell Migration in Human Colon Carcinoma and Fetal Lung Fibroblast Cell Lines

2016

T-2 toxin and Ochratoxin A (OTA) are toxic secondary metabolites produced by various fungi, and together they contaminate feedstuffs worldwide. T-2 toxin and OTA may exert carcinogenic action in rodent. Despite the various in vivo experiments, carcinogenicity of these two mycotoxins has not yet been proven for human. In this current study, we proposed to investigate, in Human colon carcinoma cells and fetal lung fibroblast-like cells transfected with MYC, the effect of T-2 toxin and OTA on cell clonogenicity and cell migration. Results of the present investigation showed that T2-toxin as well as OTA has an important clonogenic effect in all cell lines, suggesting that these mycotoxins could…

0301 basic medicineOchratoxin AHealth Toxicology and MutagenesisCellBiologyToxicologymedicine.disease_causeBiochemistryMicrobiology03 medical and health scienceschemistry.chemical_compoundIn vivomedicineClonogenic assayMolecular BiologyToxinCell migrationGeneral MedicineTransfection3. Good health030104 developmental biologymedicine.anatomical_structurechemistryCell cultureCancer researchMolecular MedicineJournal of Biochemical and Molecular Toxicology
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