Search results for "ibi"

showing 10 items of 13473 documents

Auxiliary α2δ1 and α2δ3 Subunits of Calcium Channels Drive Excitatory and Inhibitory Neuronal Network Development

2020

VGCCs are multisubunit complexes that play a crucial role in neuronal signaling. Auxiliary α2δ subunits of VGCCs modulate trafficking and biophysical properties of the pore-forming α1 subunit and trigger excitatory synaptogenesis. Alterations in the expression level of α2δ subunits were implicated in several syndromes and diseases, including chronic neuropathic pain, autism, and epilepsy. However, the contribution of distinct α2δ subunits to excitatory/inhibitory imbalance and aberrant network connectivity characteristic for these pathologic conditions remains unclear. Here, we show that α2δ1 overexpression enhances spontaneous neuronal network activity in developing and mature cultures of …

0301 basic medicineNeurogenesisSynaptogenesisNeurotransmissionInhibitory postsynaptic potentialHippocampusSynaptic Transmission03 medical and health sciencesGlutamatergicMice0302 clinical medicineVGCCsexcitation to inhibition balanceBiological neural networkPremovement neuronal activityAnimalsHumansCalcium SignalingResearch ArticlesNeuronssynaptogenesisChemistryGeneral NeuroscienceGlutamate receptornetwork connectivityRats030104 developmental biologyHEK293 CellsExcitatory postsynaptic potentialalpha2delta subunitsCalcium ChannelsNerve NetNeuroscience030217 neurology & neurosurgeryCellular/MolecularThe Journal of Neuroscience
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In silico and in vitro prediction of the toxicological effects of individual and combined mycotoxins.

2018

3-Acetyldeoxynivalenol (3-AcDON) and 15-acetyldeoxynivalenol (15-AcDON) are converted to deoxynivalenol (DON) in vivo and their simultaneous presence may increase DON intake. Mixtures of DON and its derivatives are a public health concern. In this study DON, 3-AcDON and 15-AcDON were evaluated in vitro and in silico. The in vitro cytotoxicity of DON and its derivatives individually and combined was determined by the Neutral Red (NR) assay in human hepatocarcinoma (HepG2) cells. The concentrations tested were from 1.25 to 15 μM (DON) and from 0.937 to 7.5 μM (DON derivatives). The IC50 values were from >15 to 2.55 μM (DON), from 1.77 to 1.02 μM (3-AcDON), and from 4.05 to 1.68 μM (15-AcDON).…

0301 basic medicineNeutral redCell SurvivalIn silicoComplex MixturesIn Vitro TechniquesToxicologyExcretion03 medical and health scienceschemistry.chemical_compoundInhibitory Concentration 500404 agricultural biotechnologyIn vivoCytochrome P-450 CYP3AHumansComputer SimulationFood scienceMycotoxinCYP3A4Dose-Response Relationship DrugChemistry04 agricultural and veterinary sciencesGeneral MedicineHep G2 CellsMycotoxins040401 food scienceIn vitro030104 developmental biologyGastrointestinal AbsorptionToxicityTrichothecenesFood ScienceFood and chemical toxicology : an international journal published for the British Industrial Biological Research Association
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Identification of noncovalent proteasome inhibitors with high selectivity for chymotrypsin-like activity by a multistep structure-based virtual scree…

2016

Noncovalent proteasome inhibitors introduce an alternative mechanism of inhibition to that of covalent inhibitors, e.g. carfilzomib, used in cancer therapy. A multistep hierarchical structure-based virtual screening (SBVS) of the 65,375 NCI lead-like compound library led to the identification of two compounds (9 and 28) which noncovalently inhibited the chymotrypsin-like (ChT-L) activity (Ki = 2.18 and 2.12 μM, respectively) with little or no effects on the other two major proteasome proteolytic activities, trypsin-like (T-L) and post-glutamyl peptide hydrolase (PGPH) activities. A subsequent hierarchical similarity search over the full NCI database with the most active tripeptide-based inh…

0301 basic medicineNon-covalentVirtual screeningProteasome Endopeptidase ComplexStereochemistryProtein ConformationProteolysisDrug Evaluation PreclinicalTripeptideSubstrate Specificity03 medical and health scienceschemistry.chemical_compoundStructure-Activity RelationshipUser-Computer Interface0302 clinical medicineProtein structureCell Line TumorDrug DiscoverymedicineStructure–activity relationshipChymotrypsinHumansProteasome inhibitorCell ProliferationPharmacologyVirtual screeningmedicine.diagnostic_testOrganic ChemistryGeneral MedicineCarfilzomibPeptide scaffoldMolecular Docking SimulationProteasome inhibitors; Non-covalent; Peptide scaffold; Docking studies; Virtual screening030104 developmental biologyProteasomechemistryBiochemistryDocking (molecular)030220 oncology & carcinogenesisDocking studieProteolysisProteasome InhibitorsEuropean journal of medicinal chemistry
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Lactobacillus plantarum LUHS135 and paracasei LUHS244 as functional starter cultures for the food fermentation industry: Characterisation, mycotoxin-…

2018

Abstract Lactobacillus plantarum LUHS135 and Lactobacillus paracasei LUHS244 from fermented cereals were isolated and their properties (carbohydrate metabolism, gas production, ability to survive at a low pH values, growth performance at different temperatures, antimicrobial properties against Pseudomonas aeruginosa, Staphylococcus aureus, Escherichia coli, Salmonella enterica, Corynebacter spp, Klebsiella pneomoniae, Enterococcus faecalis, Bacillus cereus, Proteus mirabilis, Clostridium spp., Streptococcus spp., resistance to antibiotics, and reducing properties for aflatoxin B1, ochratoxin A, HT-2 toxin, T-2 toxin, zearalenone) were evaluated. Also, the possibilities to use dairy by-produ…

0301 basic medicineOchratoxin AbiologyLactobacillus paracaseiChemistry030106 microbiologyBacillus cereusfood and beverages04 agricultural and veterinary sciencesbiology.organism_classification040401 food scienceEnterococcus faecalis03 medical and health scienceschemistry.chemical_compound0404 agricultural biotechnologyYeast extractFermentationLactobacillus plantarum Lactobacillus paracasei Antimicrobial activity Resistance to antibiotics Mycotoxins Whey EncapsulationFood scienceMycotoxinLactobacillus plantarumFood Science
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L’olfaction dans les troubles dépressifs : intérêts et perspectives

2017

International audience; Research on sensorial interactions with psychiatric diseases and particularly with the depressive syndrome has mainly focused on visual or auditory processes and much less on olfaction. The depressive illness is one of the most frequent psychiatric diagnoses in the community, with approximately one in five women and one in eight men experiencing a major depressive episode during their lifetime. Although genetic, epigenetic, neuroanatomical, neurochemical, neuroendocrinological and neuroimmunological changes can be detected during depression, the etiology of depression remains partly unclear. The current explanatory models are based on two main factors, i.e. pharmacol…

0301 basic medicineOlfactory systemOlfactory sensitivityBipolar disorderContext (language use)OlfactionÉpisode dépressif caractérisé03 medical and health sciences0302 clinical medicineNeurochemicalLimbic systemArts and Humanities (miscellaneous)DiagnosismedicineMajor depressionDiagnosticMajor depressive episodeDepression (differential diagnoses)Olfaction3. Good healthPsychiatry and Mental health030104 developmental biologyMoodmedicine.anatomical_structure[SDV.NEU]Life Sciences [q-bio]/Neurons and Cognition [q-bio.NC]Trouble bipolairemedicine.symptomPsychologyNeuroscienceSensibilité olfactive030217 neurology & neurosurgeryL'Encéphale
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mRCC Outcome in the Treatment of Metastatic Renal Cell Carcinoma - A German Single-center Real-world Experience.

2018

Background/Aim: Since the advent of targeted therapeutics, paradigms in metastatic renal cell carcinoma (mRCC) treatment have changed. We investigated if efficacy and safety data from randomized controlled trials can be transferred into real-world settings. Patients and Methods: All patients with mRCC treated from 2006-2015 at the Department of Urology (Marburg-Germany) were retrospectively analyzed. Collected data include: Patient demographics, tumor characteristics, efficacy, safety, and used therapy sequences. Results: In total, 197 patients with mRCC were identified. About one third of patients reached third-line therapy. Median overall survival in real-world amounted to 25.8 months wit…

0301 basic medicineOncologyAdultMaleCancer Researchmedicine.medical_specialtymedicine.drug_classmedicine.medical_treatmentSingle CenterGeneral Biochemistry Genetics and Molecular BiologyTyrosine-kinase inhibitorTargeted therapylaw.invention03 medical and health sciences0302 clinical medicineRisk groupsRandomized controlled trialRenal cell carcinomalawRisk FactorsInternal medicineGermanymedicineOverall survivalHumansMolecular Targeted TherapyNeoplasm MetastasisSurvival rateCarcinoma Renal CellProtein Kinase InhibitorsAgedRandomized Controlled Trials as TopicRetrospective StudiesPharmacologybusiness.industryNeoplasms Second PrimaryMiddle Agedmedicine.diseaseProgression-Free Survival030104 developmental biologyTreatment Outcome030220 oncology & carcinogenesisFemalebusinessResearch ArticleIn vivo (Athens, Greece)
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Prognostic clinical factors in patients affected by non-small-cell lung cancer receiving Nivolumab

2020

Background: Immune-checkpoint inhibitors have radically changed the treatment landscape of Non-Small-Cell Lung Cancer (NSCLC). It is still unclear whether specific clinical characteristics might identify those patients benefiting from immunotherapy more than others. The aim of this study was to identify clinical characteristics associated with disease-specific survival (DSS), time-to-treatment failure (TTF), objective responses (OR) and progressive disease (PD) in NSCLC patients treated with Nivolumab. Methods: This was a multicenter retrospective study conducted on 294 patients treated with Nivolumab for advanced NSCLC. Results: Of the more than 50 variables analyzed, five showed a signifi…

0301 basic medicineOncologyAdultMalemedicine.medical_specialtyLung Neoplasmsmedicine.medical_treatmentClinical BiochemistryKaplan-Meier EstimateDisease-Free SurvivalDrug Administration ScheduleNO03 medical and health sciences0302 clinical medicineInternal medicineCarcinoma Non-Small-Cell LungDrug DiscoverymedicineMalignant pleural effusionHumansimmunotherapy; malignant pleural effusion; nivolumab; non-small-cell lung cancerIn patientmalignant pleural effusionLung cancerImmune Checkpoint InhibitorsRetrospective StudiesPharmacologynivolumabbusiness.industryBrain NeoplasmsLiver NeoplasmsImmunotherapymedicine.diseasePrognosisPleural Effusion Malignantrespiratory tract diseases030104 developmental biologyTreatment Outcomenon-small-cell lung cancer030220 oncology & carcinogenesisFemalesense organsNon small cellimmunotherapyNivolumabbusiness
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Human leukocyte antigen-E mismatch is associated with better hematopoietic stem cell transplantation outcome in acute leukemia patients

2017

The immunomodulatory role of human leukocyte antigen (HLA)-E in hematopoietic stem cell transplantation (HSCT) has not been extensively investigated. To this end, we genotyped 509 10/10 HLA unrelated transplant pairs for HLA-E, in order to study the effect of HLA-E as a natural killer (NK)-alloreactivity mediator on HSCT outcome in an acute leukemia (AL) setting. Overall survival (OS), disease free survival (DFS), relapse incidence (RI) and non-relapse mortality (NRM) were set as endpoints. Analysis of our data revealed a significant correlation between HLA-E mismatch and improved HSCT outcome, as shown by both univariate (53% vs. 38%, P=0.002, 5-year OS) and multivariate (hazard ratio (HR)…

0301 basic medicineOncologyAdultMalemedicine.medical_specialtyTransplantation ConditioningAdolescentGenotypemedicine.medical_treatment610Hematopoietic stem cell transplantationHuman leukocyte antigen600 Technik Medizin angewandte Wissenschaften::610 Medizin und GesundheitArticle03 medical and health sciencesYoung Adult0302 clinical medicineCell Therapy & ImmunotherapyInternal medicineMedicineHumansTransplantation Homologousddc:610Potassium Channels Inwardly RectifyingSurvival analysisAllelesAgedBone Marrow TransplantationAcute leukemiabusiness.industryDonor selectionHistocompatibility TestingHazard ratioHistocompatibility Antigens Class IHematopoietic Stem Cell TransplantationHematologyMiddle Agedmedicine.diseasePrognosisSurvival AnalysisTransplantationLeukemiaLeukemia Myeloid Acute030104 developmental biologyTreatment OutcomeImmunologyFemalebusiness030215 immunology
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The Emerging Therapeutic Landscape of ALK Inhibitors in Non-Small Cell Lung Cancer.

2020

The treatment of metastatic non-small cell lung cancer (NSCLC) has undergone a paradigm shift over the last decade. Better molecular characterization of the disease has led to the rapid improvement of personalized medicine and the prompt delivery of targeted therapies to patients with NSCLC. The discovery of the EML4-ALK fusion gene in a limited subset of patients affected by NSCLC and the subsequent clinical development of crizotinib in 2011 has been an impressive milestone in lung cancer research. Unfortunately, acquired resistances regularly develop, hence disease progression occurs. Afterward, modern tyrosine kinase inhibitors (TKIs), such as ceritinib, alectinib, brigatinib, and lorlat…

0301 basic medicineOncologyAlectinibALK inhibitorsmedicine.medical_specialtybrigatinibBrigatinibmedicine.medical_treatmentPharmaceutical Sciencenon-small cell lung cancer (NSCLC)lcsh:Medicinelcsh:RS1-441ReviewALK inhibitorTargeted therapylcsh:Pharmacy and materia medica03 medical and health sciences0302 clinical medicinelorlatinibInternal medicineDrug DiscoveryMedicineAnaplastic lymphoma kinaseceritinibalectinibensartinibcrizotinibCrizotinibCeritinibbusiness.industrylcsh:Rmedicine.diseaseLorlatinibrespiratory tract diseasesnon-small cell lung cancer (NSCLC)030104 developmental biologytyrosine kinase inhibitors (TKIs)030220 oncology & carcinogenesisMolecular Medicinebusinessmedicine.drugPharmaceuticals (Basel, Switzerland)
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Recommendations for the implementation of BRCA testing in the care and treatment pathways of ovarian cancer patients

2016

In the last 20 years, following the identification of the BRCA1 and BRCA2 genes (hereinafter referred to as the BRCA genes), preventive pathways have been developed for the identification and clinical management of individuals at high risk of developing breast and ovarian cancer due to the presence of a pathogenic variant in either of these genes. These pathways are aimed at educating high-risk subjects on programs targeted toward early diagnosis and cancer risk reduction. The approval of a novel class of drugs, the PARP enzyme inhibitors, for the treatment of ovarian cancer patients carrying high-risk BRCA pathogenic variants has changed this scenario. BRCA testing, in addition to providin…

0301 basic medicineOncologyCancer ResearchGenes BRCA2Genes BRCA1Brca testingBRCA1; BRCA2; genetic testing; germline mutations; ovarian cancer; PARP inhibitors; somatic mutations; Oncology; Cancer ResearchSettore MED/03 - GENETICA MEDICA0302 clinical medicineClinical decision makingInformed consentsomatic mutationBRCA1 BRCA2 genetic testing germline mutations somatic mutations ovarian cancer PARP inibitorsDisease management (health)PARP inhibitorsOvarian NeoplasmsTumorInformed Consentmedicine.diagnostic_testDisease ManagementGeneral MedicinePrognosisBRCA1; BRCA2; genetic testing; germline mutations; ovarian cancer; PARP inhibitors; somatic mutations; Biomarkers Tumor; Clinical Decision-Making; Disease Management; Female; Genes BRCA1; Genetic Variation; Germ-Line Mutation; Humans; Informed Consent; Mutation; Ovarian Neoplasms; Prognosis; Genes BRCA2; Genetic Testing; Oncology; Cancer Researchovarian cancergermline mutationOncology030220 oncology & carcinogenesisgermline mutationsFemaleHumanmedicine.medical_specialtyPrognosiClinical Decision-MakingMEDLINEgenetic testing03 medical and health sciencesPARP inibitorsInternal medicinemedicineBiomarkers TumorHumansGerm-Line MutationGenetic testingGynecologyBRCA1; BRCA2; PARP inhibitors; genetic testing; germline mutations; ovarian cancer; somatic mutationsbusiness.industryOvarian NeoplasmGenetic Variationmedicine.diseaseBRCA1BRCA2030104 developmental biologyPARP inhibitorGenesMutationsomatic mutationsOvarian cancerbusinessBiomarkers
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