Search results for "Farm"

showing 10 items of 3554 documents

Henneguya zschokkei (Myxozoa) infection in cultured whitefish: Age-dependence, seasonality and distribution within host

2017

Abstract Whitefish ( Coregonus lavaretus ) is an important species for European fisheries and aquaculture. Recently, the myxosporean Henneguya zschokkei has been observed to infect the muscles of whitefish in fish farms. Plasmodia of H. zschokkei prevent marketing of the fillet and cause economic losses. The factors associated with occurrence of the parasite in fish farms have not been investigated previously. We studied age-dependence, seasonality, and within-host distribution of H. zschokkei plasmodia in farmed whitefish by examining a total of 1599 fish. Distribution of plasmodia within the fish was not uniform. When the fillet was divided into parts, the number of plasmodia was positive…

0301 basic medicineFish farmingZoologyCoregonus lavaretusAquatic ScienceMyxosporea03 medical and health sciencesfoodStockingCoregonus lavaretusAquacultureparasitic diseasesParasite hostingMyxozoabiologyfood.dishHatchingbusiness.industryHenneguya zschokkei030108 mycology & parasitologybiology.organism_classificationFisheryEuropean whitefishta1181Henneguya zschokkeibusinessAquaculture
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Anthranilamide-based 2-phenylcyclopropane-1-carboxamides, 1,1'-biphenyl-4-carboxamides and 1,1'-biphenyl-2-carboxamides: Synthesis biological evaluat…

2017

Abstract Several anthranilamide-based 2-phenylcyclopropane-1-carboxamides 13a-f, 1,1’-biphenyl-4-carboxamides 14a-f and 1,1’-biphenyl-2-carboxamides 17a-f were obtained by a multistep procedure starting from the (1S,2S)-2-phenylcyclopropane-1-carbonyl chloride 11, the 1,1'-biphenyl-4-carbonyl chloride 12 or the 1,1'-biphenyl-2-carbonyl chloride 16 with the appropriate anthranilamide derivative 10a-f. Derivatives 13a-f, 14a-f and 17a-f showed antiproliferative activity against human leukemia K562 cells. Among these derivatives 13b, 14b and 17b exerted a particular cytotoxic effect on tumor cells. Derivative 17b showed a better antitumoral effect on K562 cells than 13b and 14b. Analyses perfo…

0301 basic medicineG2 Phase2-Phenylcyclopropane-1-carboxamides 11’-biphenyl-4-carboxamides 11’-biphenyl-2-carboxamides G2/M arrest Phospho-ATM and gH2AX increaseDNA RepairDNA repairStereochemistryAntineoplastic AgentsApoptosisChloride03 medical and health scienceschemistry.chemical_compound0302 clinical medicineSettore BIO/10 - BiochimicaDrug DiscoverymedicineCytotoxic T cellHumansortho-AminobenzoatesMode of actionCell ProliferationPharmacologyChemistryOrganic ChemistryGeneral MedicineCell Cycle CheckpointsCell cycleSettore CHIM/08 - Chimica Farmaceutica030104 developmental biologyMechanism of actionApoptosis030220 oncology & carcinogenesismedicine.symptomK562 CellsDNAmedicine.drugDNA Damage
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Parallel paleogenomic transects reveal complex genetic history of early European farmers

2017

In European Neolithic populations, the arrival of farmers prompted admixture with local hunter-gatherers over many centuries, resulting in distinct signatures in each region due to a complex series of interactions. David Reich and colleagues analyse genome-wide data from 180 individuals from the Neolithic and Chalcolithic periods of Hungary, Germany and Spain to study the population dynamics of Neolithization in European prehistory. They examine how gene flow reshaped European populations during the Neolithic period, including pervasive admixture—the interbreeding between previously isolated populations—between groups with different ancestry profiles. In each region, they find that the arri…

0301 basic medicineGene FlowMale0106 biological sciencesHuman MigrationPopulation DynamicsPopulationDatasets as Topic010603 evolutionary biology01 natural sciencesArticleGene flowPrehistory03 medical and health sciencesSpatio-Temporal AnalysisGermanyGenetic variationHumansDNA AncienteducationTransectHistory Ancient030304 developmental biologyHungary0303 health scienceseducation.field_of_studyGenetic diversityMultidisciplinaryFarmersHuman migrationbusiness.industryEcologyGenetic VariationChalcolithic030104 developmental biologyAncient DNAGeographySpainPeriod (geology)EthnologyFemalebusiness
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Common Hits Approach: Combining Pharmacophore Modeling and Molecular Dynamics Simulations.

2017

We present a new approach that incorporates flexibility based on extensive MD simulations of protein-ligand complexes into structure-based pharmacophore modeling and virtual screening. The approach uses the multiple coordinate sets saved during the MD simulations and generates for each frame a pharmacophore model. Pharmacophore models with the same pharmacophore features are pooled. In this way the high number of pharmacophore models that results from the MD simulation is reduced to only a few hundred representative pharmacophore models. Virtual screening runs are performed with every representative pharmacophore model; the screening results are combined and rescored to generate a single hi…

0301 basic medicineGeneral Chemical EngineeringDrug Evaluation PreclinicalLibrary and Information SciencesMolecular Dynamics Simulationcomputer.software_genreLigandsLigandScoutCommon Hits Approach (CHA)03 medical and health sciencesMolecular dynamicsUser-Computer InterfaceComputational chemistryPharmacophore ModelingFlexibility (engineering)Virtual screeningChemistryFrame (networking)ProteinsGeneral ChemistryInto-structureSettore CHIM/08 - Chimica FarmaceuticaComputer Science Applications030104 developmental biologyData miningPharmacophorecomputerJournal of chemical information and modeling
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Effects of 3,5-diiodo-L-thyronine on the liver of high fat diet fed rats

2016

Experimental studies have highlighted that the administration of 3,5-diiodo-L-thyronine (T2) to rats fed diets rich in lipids induces a decrease of cholesterol and triglycerides plasma levels and body weight (BW) without inducing liver steatosis. On the basis of these observations we carried out some experimental <em>in vivo</em> studies to assess the effects of multiple high doses of T2 on the pituitary thyroid axis of rats fed diet rich in lipids. Fifteen male Wistar rats were divided into three groups of five animals each. The first group (N group) received standard diet, the second group was fed with a high fat diet (HFD group), while the third group (HFDT2 group) was additi…

0301 basic medicineHepatic steatosismedicine.medical_specialtyPlant ScienceAdrenocorticotropic hormoneHepatic steatosi010501 environmental sciencesBiologySettore BIO/09 - Fisiologia01 natural sciencesGeneral Biochemistry Genetics and Molecular BiologyPituitary thyroid axis03 medical and health scienceschemistry.chemical_compoundInternal medicinemedicinelcsh:QH301-705.50105 earth and related environmental sciences35-diiodo-L-thyronine; TSH; Thyroid hormone; Hepatic steatosisBiochemistry Genetics and Molecular Biology (all)TriiodothyronineTSHCholesterolBiochemistry (medical)medicine.diseaseSettore CHIM/08 - Chimica Farmaceutica35-diiodo-L-thyronineThyroid hormone030104 developmental biologyEndocrinologylcsh:Biology (General)chemistryThyronineSettore BIO/14 - FarmacologiaAlkaline phosphataseSteatosisHormoneJournal of Biological Research - Bollettino della Società Italiana di Biologia Sperimentale
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Pharmaceutical Approaches to Target Antibiotic Resistance Mechanisms

2017

There is urgent need for new therapeutic strategies to fight the global threat of antibiotic resistance. The focus of this Perspective is on chemical agents that target the most common mechanisms of antibiotic resistance such as enzymatic inactivation of antibiotics, changes in cell permeability, and induction/activation of efflux pumps. Here we assess the current landscape and challenges in the treatment of antibiotic resistance mechanisms at both bacterial cell and community levels. We also discuss the potential clinical application of chemical inhibitors of antibiotic resistance mechanisms as add-on treatments for serious drug-resistant infections. Enzymatic inhibitors, such as the deriv…

0301 basic medicineImipenemmedicine.drug_classAvibactam030106 microbiologyAntibioticsDrug resistancePharmacologyBiologySettore BIO/19 - Microbiologia Generalemedicine.disease_causeMicrobiology03 medical and health scienceschemistry.chemical_compoundAntibiotic resistanceDrug DiscoverymedicineHumansPseudomonas InfectionsBeta-Lactamase InhibitorsPseudomonas aeruginosaDrug Discovery3003 Pharmaceutical ScienceEnterobacteriaceae InfectionsDrug Resistance MicrobialSettore CHIM/08 - Chimica FarmaceuticaImipenemchemistryMolecular Medicine; Drug Discovery3003 Pharmaceutical ScienceMolecular MedicineEffluxbeta-Lactamase InhibitorsAzabicyclo Compoundsmedicine.drugJournal of Medicinal Chemistry
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Identification of biological targets through the correlation between cell line chemosensitivity and protein expression pattern.

2021

Matching biological data sequences is one of the most interesting ways to discover new bioactive compounds. In particular, matching cell chemosensitivity with a protein expression profile can be a useful approach to predict the activity of compounds against definite biological targets. In this review, we discuss this correlation. First, we analyze case studies in which some known drugs, acting on known targets, show a good correlation between their antiproliferative activities and protein expression when a large panel of tumor cells is considered. Then, we highlight how the application of in silico methods based on the correlation between cell line chemosensitivity and gene/protein expressi…

0301 basic medicineIn silicoCellAntineoplastic AgentsComputational biologyBiologyCorrelationNCI-60 cell lines panel03 medical and health sciences0302 clinical medicineCell Line TumorNeoplasmsDrug DiscoverymedicineHumansComputer SimulationMolecular Targeted TherapyChemosensitivityGeneBiological target; Chemosensitivity; NCI-60 cell lines panel; Protein expression patternPharmacologyBiological dataBiological activitySettore CHIM/08 - Chimica FarmaceuticaBiological target Chemosensitivity NCI-60 cell lines panel Protein expression patternGene Expression Regulation Neoplastic030104 developmental biologymedicine.anatomical_structureCell cultureBiological targetBiological target030220 oncology & carcinogenesisProtein expression patternDrug discovery today
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Synthesis, antitumor activity and CDK1 inhibiton of new thiazole nortopsentin analogues

2017

A new series of thiazole nortopsentin analogues was conveniently synthesized with fair overall yields. The antiproliferative activity of the new derivatives was tested against different human tumor cell lines of the NCI full panel. Four of them showed good antitumor activity with GI(50) values from micro to nanomolar level. The mechanism of the antiproliferative effect of these derivatives, was pro-apoptotic, being associated with externalization of plasma membrane phosphatidylserine and DNA fragmentation. The most active and selective of the new thiazoles confined viable cells in G2/M phase and markedly inhibited in vitro CDK1 activity. (C) 2017 Elsevier Masson SAS.

0301 basic medicineIndolesCell SurvivalStereochemistryMolecular ConformationNortopsentin analogues3-b]pyridinesAntineoplastic AgentsApoptosisMarine alkaloids Nortopsentin analogues Antiproliferative activity Apoptosis CDK1 inhibitors Thiazolyl-1H-pyrrolo[23-b]pyridinesAntiproliferative activity01 natural sciencesStructure-Activity Relationship03 medical and health scienceschemistry.chemical_compoundMarine alkaloidsCDC2 Protein KinaseDrug DiscoveryHumansThiazoleProtein Kinase InhibitorsCell ProliferationPharmacologyCyclin-dependent kinase 1Dose-Response Relationship DrugMarine alkaloids; Nortopsentin analogues; Antiproliferative activity; Apoptosis; CDK1 inhibitors; Thiazolyl-1H-pyrrolo[2; 3-b]pyridines010405 organic chemistryOrganic ChemistryImidazolesGeneral MedicinePhosphatidylserineThiazolyl-1H-pyrrolo[2Settore CHIM/08 - Chimica FarmaceuticaCyclin-Dependent KinasesIn vitro0104 chemical sciencesCDK1 inhibitors030104 developmental biologyMembranechemistryCell cultureApoptosisMCF-7 CellsDNA fragmentationCaco-2 CellsDrug Screening Assays Antitumor
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The potential of neurotrophic tyrosine kinase (NTRK) inhibitors for treating lung cancer

2016

Abstract: Introduction: Molecular alterations in neurotrophic tyrosine kinase (NTRK) genes have been identified in several solid tumors including lung cancer. Pre-clinical and clinical evidence suggested their potential role as oncogenic drivers and predictive biomarkers for targeted inhibition, leading to the clinical development of a new class of compounds blocking the NTRK molecular pathway, which are currently undner early clinical investigation. Area covered: This review describes the biology of the NTRK pathway and its molecular alterations in lung cancer. It focuses on the pre-clinical and clinical development of emerging NTRK inhibitors, which have shown very promising activity in e…

0301 basic medicineLung NeoplasmsNTRKinhibitorsNTRK1/2/3Settore MED/06 - Oncologia Medicamedicine.medical_treatmentReceptor Protein-Tyrosine KinasesEntrectinibPharmacologyTargeted therapy03 medical and health sciences0302 clinical medicineMedicineAnimalsHumansPharmacology (medical)In patientNTRKinhibitorLung cancerProtein Kinase InhibitorsTrkA/B/CPharmacologyNTRK1/2/3; TrkA/B/C; NTRKinhibitors; targeted therapy; lung cancerbiologybusiness.industryPharmacology. TherapyReceptor Protein-Tyrosine KinasesGeneral Medicinemedicine.diseasetargeted therapySettore CHIM/08 - Chimica Farmaceuticalung cancer030104 developmental biology030220 oncology & carcinogenesisbiology.proteinCancer researchbusinessEarly phaseTyrosine kinaseNeurotrophin
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Potential Therapeutic Applications of MDA-9/Syntenin-NF-κB-RKIP Loop in Human Liver Carcinoma

2019

Background Overexpression of MDA-9/Syntenin occurs in multiple human cancer cell lines and is associated with higher grade of tumor classification, invasiveness and metastasis. In some cases, its role in cancer biology depends on relationships between MDA-9/Syntenin and NF-κB. Objective This study aims to analyze the presence of a regulation loop like that between MDA-9/Syntenin - NF-κB - RKIP in human liver carcinoma. Methods Transient transfection was performed with siRNA anti-MDA-9/Syntenin. Expression of different factors was evaluated by Real time-PCR and Western blotting, while NF-κB activation by TransAM assay. Invasion capacity was analyzed by Matrigel Invasion Assay and the effects…

0301 basic medicineMDA-9/Syntenin NF-κB RKIP drug targets HA22T/VGH Hep3B HepG2Carcinoma HepatocellularCurcuminSynteninsPhosphatidylethanolamine Binding ProteinBiochemistry03 medical and health scienceschemistry.chemical_compound0302 clinical medicineDownregulation and upregulationAntineoplastic Combined Chemotherapy ProtocolsHumansGene silencingNeoplasm InvasivenessViability assayMolecular BiologyCell growthMatrigel Invasion AssayLiver NeoplasmsNF-kappa BNF-κBHep G2 CellsGeneral MedicineNeoplasm ProteinsBlot030104 developmental biologychemistryDoxorubicinCell cultureSettore BIO/14 - FarmacologiaCancer researchMolecular MedicineSignal Transduction030215 immunologyCurrent Molecular Medicine
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