Search results for "H.P.M."

showing 10 items of 738 documents

Recent advances on CDK inhibitors: An insight by means of in silico methods

2017

The cyclin dependent kinases (CDKs) are a small family of serine/threonine protein kinases that can act as a potential therapeutic target in several proliferative diseases, including cancer. This short review is a survey on the more recent research progresses in the field achieved by using in silico methods. All the "armamentarium" available to the medicinal chemists (docking protocols and molecular dynamics, fragment-based, de novo design, virtual screening, and QSAR) has been employed to the discovery of new, potent, and selective inhibitors of cyclin dependent kinases. The results cited herein can be useful to understand the nature of the inhibitor-target interactions, and furnish an ins…

0301 basic medicineQuantitative structure–activity relationshipMolecular dynamicIn silicoCDKQuantitative Structure-Activity RelationshipAntineoplastic AgentsComputational biologyMolecular Dynamics SimulationBioinformatics01 natural sciencesSerine03 medical and health sciencesCyclin-dependent kinaseNeoplasmsDrug DiscoveryAnimalsHumansProtein Kinase InhibitorsPharmacologyVirtual screeningHVTSbiologyChemistryKinaseQSARDrug Discovery3003 Pharmaceutical ScienceOrganic ChemistryGeneral MedicineCyclin-Dependent Kinases0104 chemical sciencesMolecular Docking Simulation010404 medicinal & biomolecular chemistry030104 developmental biologyDocking (molecular)Drug Designbiology.proteinComputer-Aided DesignIn silico methodMolecular modelling
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Cosavirus, Salivirus and Bufavirus in Diarrheal Tunisian Infants

2016

International audience; Three newly discovered viruses have been recently described in diarrheal patients: Cosa-virus (CosV) and Salivirus (SalV), two picornaviruses, and Bufavirus (BuV), a parvovirus. The detection rate and the role of these viruses remain to be established in acute gastroen-teritis (AGE) in diarrheal Tunisian infants. From October 2010 through March 2012, stool samples were collected from 203 children <5 years-old suffering from AGE and attending the Children's Hospital in Monastir, Tunisia. All samples were screened for CosV, SalV and BuV as well as for norovirus (NoV) and group A rotavirus (RVA) by molecular biology. Positive samples for the three screened viruses were …

0301 basic medicineRNA virusesMaleRotavirusViral DiseasesHuman astrovirusesIdentificationvirusesEnteric viruseslcsh:MedicinePolymerase chain-reactionArtificial Gene Amplification and ExtensionPicornaviridaemedicine.disease_causePathology and Laboratory MedicinePolymerase Chain ReactionPediatricsReverse-transcription-pcrlaw.inventionParvoviruslaw[SDV.MHEP.MI]Life Sciences [q-bio]/Human health and pathology/Infectious diseasesRotavirusMedicine and Health Scienceslcsh:ScienceChildrenPolymerase chain reactionPhylogenyMultidisciplinarybiologyTransmission (medicine)[ SDV.IDA ] Life Sciences [q-bio]/Food engineeringPhylogenetic Analysis3. Good healthGastroenteritisInfectious DiseasesMedical MicrobiologyViral PathogensChild PreschoolViruses[SDV.MP.VIR]Life Sciences [q-bio]/Microbiology and Parasitology/VirologyFemalePathogensAichi virusPediatric InfectionsResearch ArticleDiarrheaTunisia030106 microbiologyGastroenterology and HepatologyResearch and Analysis MethodsMicrobiologyCalicivirusesAstrovirus03 medical and health sciencesKlassevirusParvovirusesAdeno-Associated VirusesmedicineHumansMolecular Biology TechniquesMolecular BiologyMicrobial PathogensRotavirus InfectionMolecular Biology Assays and Analysis TechniquesParvovirusNoroviruslcsh:ROrganismsBiology and Life SciencesInfantSapovirusReverse Transcriptase-Polymerase Chain Reactionbiology.organism_classificationVirology030104 developmental biologyNoroviruslcsh:QDNA viruses
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The SCO1731 methyltransferase modulates actinorhodin production and morphological differentiation of Streptomyces coelicolor A3(2)

2018

AbstractStreptomyces coelicolor is a Gram-positive microorganism often used as a model of physiological and morphological differentiation in streptomycetes, prolific producers of secondary metabolites with important biological activities. In the present study, we analysed Streptomyces coelicolor growth and differentiation in the presence of the hypo-methylating agent 5′-aza-2′-deoxycytidine (5-aza-dC) in order to investigate whether cytosine methylation has a role in differentiation. We found that cytosine demethylation caused a delay in spore germination, aerial mycelium development, sporulation, as well as a massive impairment of actinorhodin production. Thus, we searched for putative DNA…

0301 basic medicineScienceMutantAnthraquinonesStreptomyces coelicolorDecitabineSettore BIO/19 - Microbiologia GeneraleDNA methyltransferaseArticleActinorhodin03 medical and health scienceschemistry.chemical_compoundBacterial ProteinsSpore germinationSpores BacterialRegulation of gene expressionMultidisciplinaryMyceliumbiologyStreptomyces coelicolorfungiQRActinorhodin ProductionCell DifferentiationGene Expression Regulation BacterialMethyltransferasesbiology.organism_classificationTn5 Mutant Strains030104 developmental biologychemistryBiochemistryHypomethylating AgentsStreptomyces coelicolor bacterial differentiation epigenetic cytosine methylationDNA methylationMedicineCytosineCytosine Methylation
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Early life infection and host senescence

2018

IF 3.224 (2017); International audience; Advanced age is often associated with a chronic inflammatory status and inflammatory diseases. It has been suggested that exposure to infectious agents that stimulate the inflammatory response at early ages might have carry over effects in terms of accelerated senescence and increased mortality at late ages. However, not all pathogens and parasites have pro-inflammatory effects. In particular, parasitic nematodes have been shown to dampen the inflammatory response and to prevent or alleviate the symptoms of inflammatory diseases. We, therefore, tentatively predicted that early infection with a parasite that has anti-inflammatory properties might post…

0301 basic medicineSenescenceMaleAgingLPSRodent[SDV.MHEP.PHY] Life Sciences [q-bio]/Human health and pathology/Tissues and Organs [q-bio.TO]LongevityInflammationHeligmosomoides polygyrusBiochemistryHost-Parasite Interactions03 medical and health sciencesMice0302 clinical medicineEndocrinologyBiomarkers of aging[SDV.MHEP.MI]Life Sciences [q-bio]/Human health and pathology/Infectious diseasesbiology.animalGeneticsmedicine[SDV.MHEP.PHY]Life Sciences [q-bio]/Human health and pathology/Tissues and Organs [q-bio.TO]AnimalsMolecular BiologyStrongylida InfectionsNematodeInflammationNematospiroides dubiusbiology[SDV.MHEP.GEG] Life Sciences [q-bio]/Human health and pathology/Geriatry and gerontologyHost (biology)[SDV.MHEP.GEG]Life Sciences [q-bio]/Human health and pathology/Geriatry and gerontologyCell Biologybiology.organism_classificationPhenotype3. Good healthDisease Models Animal030104 developmental biologyNematodeImmunology[SDV.MHEP.MI] Life Sciences [q-bio]/Human health and pathology/Infectious diseasesMice Inbred CBAFemaleHeligmosomoides polygyrusmedicine.symptomBiomarkers[SDV.MHEP]Life Sciences [q-bio]/Human health and pathology030215 immunology
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Variants associated with HHIP expression have sex-differential effects on lung function

2021

Background: Lung function is highly heritable and differs between the sexes throughout life. However, little is known about sex-differential genetic effects on lung function. We aimed to conduct the first genome-wide genotype-by-sex interaction study on lung function to identify genetic effects that differ between males and females. Methods: We tested for interactions between 7,745,864 variants and sex on spirometry-based measures of lung function in UK Biobank (N=303,612), and sought replication in 75,696 independent individuals from the SpiroMeta consortium. Results: Five independent single-nucleotide polymorphisms (SNPs) showed genome-wide significant (P&lt;5x10-8) interactions with sex …

0301 basic medicineSpirometrymedicine.medical_specialtyHHIPMedicine (miscellaneous)Expression ; Genome-wide Interaction Study ; Hhip ; Lung Function ; SexSingle-nucleotide polymorphismBiology3121 Internal medicineGeneral Biochemistry Genetics and Molecular Biology03 medical and health sciences0302 clinical medicineExpression ; Genome-wide interaction study ; HHIP ; Lung function ; SexInternal medicineexpressionmedicinesexAlleleEnhancerGeneLung functionLunggenome-wide interaction studymedicine.diagnostic_test1184 Genetics developmental biology physiologylung functionALSPAC/dk/atira/pure/core/keywords/alspacDifferential effects030104 developmental biologyEndocrinologymedicine.anatomical_structure030228 respiratory system3121 General medicine internal medicine and other clinical medicine3111 Biomedicine
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Evaluation of dipeptide nitriles as inhibitors of rhodesain, a major cysteine protease of Trypanosoma brucei

2016

A series of dipeptide nitriles known as inhibitors of mammalian cathepsins were evaluated for inhibition of rhodesain, the cathepsin L-like protease of Trypanosoma brucei. Compound 35 consisting of a Leu residue fitting into the S2 pocket and a triarylic moiety consisting of thiophene, a 1,2,4-oxadiazole and a phenyl ring fitting into the S3 pocket, and compound 33 with a 3-bromo-Phe residue (S2) and a biphenyl fragment (S3) were found to inhibit rhodesain in the single-digit nanomolar range. The observed steep structure-activity relationship could be explained by covalent docking simulations. With their high selectivity indices (ca. 200) and the good antitrypanosomal activity (8μM) the com…

0301 basic medicineStereochemistrymedicine.medical_treatmentTrypanosoma brucei bruceiClinical BiochemistryAntitubercular AgentsPharmaceutical ScienceCysteine Proteinase InhibitorsTrypanosoma bruceiBiochemistryCysteine Proteinase InhibitorsStructure-Activity Relationship03 medical and health scienceschemistry.chemical_compoundNitrilesDrug DiscoverymedicineStructure–activity relationshipMoietyMolecular BiologyProteaseDipeptideDose-Response Relationship DrugMolecular StructurebiologyChemistryOrganic ChemistryDipeptidesbiology.organism_classificationCysteine proteaseCysteine Endopeptidases030104 developmental biologyDocking (molecular)Molecular MedicineBioorganic &amp; Medicinal Chemistry Letters
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Development of novel 1,4-benzodiazepine-based Michael acceptors as antitrypanosomal agents

2016

Novel 1,4-benzodiazepines, endowed with a Michael acceptor moiety, were designed taking advantage of a computational prediction of their pharmacokinetic parameters. Among all the synthesized derivatives, we identified a new lead compound (i.e., 4a), bearing a vinyl ketone warhead and endowed with a promising antitrypanosomal activity against Trypanosoma brucei brucei (IC50 = 5.29 µM), coupled with a lack of cytotoxicity towards mammalian cells (TC50>100 µM).

0301 basic medicineTrypanosomaKetonePeptidomimeticPeptidomimeticStereochemistryTrypanosoma brucei bruceiClinical BiochemistryPharmaceutical ScienceTrypanosoma brucei01 natural sciencesBiochemistryCell LineBenzodiazepinesMiceStructure-Activity Relationship03 medical and health scienceschemistry.chemical_compoundparasitic diseasesDrug DiscoveryAnimalsStructure–activity relationshipMoietyCytotoxicityMolecular BiologyMicrowave irradiationchemistry.chemical_classificationDose-Response Relationship DrugMolecular Structurebiology010405 organic chemistryMacrophagesOrganic Chemistrybiology.organism_classificationMichael acceptors Microwave irradiation Peptidomimetics Pharmacokinetic parameters TrypanosomaTrypanocidal Agents0104 chemical sciencesPharmacokinetic parameter030104 developmental biologychemistryMichael reactionMolecular MedicineMichael acceptorLead compoundBioorganic &amp; Medicinal Chemistry Letters
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Tracking zoonotic pathogens using blood-sucking flies as 'flying syringes'

2017

About 60% of emerging infectious diseases in humans are of zoonotic origin. Their increasing number requires the development of new methods for early detection and monitoring of infectious agents in wildlife. Here, we investigated whether blood meals from hematophagous flies could be used to identify the infectious agents circulating in wild vertebrates. To this aim, 1230 blood-engorged flies were caught in the forests of Gabon. Identified blood meals (30%) were from 20 vertebrate species including mammals, birds and reptiles. Among them, 9% were infected by different extant malaria parasites among which some belonged to known parasite species, others to new parasite species or to parasite …

0301 basic medicineglobal healthForests[SDV.MHEP.MI]Life Sciences [q-bio]/Human health and pathology/Infectious diseases[ SDV.EE.IEO ] Life Sciences [q-bio]/Ecology environment/SymbiosisParasite hostingBiology (General)Pathogen2. Zero hungerEcologyGeneral NeuroscienceQRVertebrateGeneral Medicine3. Good healthTools and Resources[ SDV.MHEP.MI ] Life Sciences [q-bio]/Human health and pathology/Infectious diseasesBloodMedicineepidemiologyPlasmodium parasitesecologyQH301-705.5Science030106 microbiologyWildlifeEarly detectionZoologyBiologytsetse fliesGeneral Biochemistry Genetics and Molecular Biology03 medical and health sciencesBlood suckingbiology.animalmedicineAnimalsParasitesGabonhematophagous flies[ SDE.BE ] Environmental Sciences/Biodiversity and EcologyGeneral Immunology and MicrobiologyDipterafungimedicine.diseaseInsect Vectors[SDV.BA.ZI]Life Sciences [q-bio]/Animal biology/Invertebrate Zoology030104 developmental biologyEpidemiology and Global HealthVector (epidemiology)[SDV.SPEE]Life Sciences [q-bio]/Santé publique et épidémiologieOtherMalaria[SDV.EE.IEO]Life Sciences [q-bio]/Ecology environment/SymbiosiseLife
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Auswirkungen eines neuen Wassersystems auf nosokomiale Kolonisierung oder Infektion mit Pseudomonas aeruginosa

2016

Aim: We aimed to study the impact of new water systems, which were less contaminated with P. aeruginosa, on the incidence of healthcare-associated P. aeruginosa cases (colonizations or infections) in care units that moved to a different building between 2005 and 2014. Methods: Generalized Estimated Equations were used to compare the incidence of P. aeruginosa healthcare-associated cases according to the building. Results: Twenty-nine units moved during the study period and 2,759 cases occurred in these units. No difference was observed when the new building was compared with older buildings overall. Conclusion: Our results did not support our hypothesis of a positive association between wat…

0301 basic medicinelcsh:Public aspects of medicineTrinkwassersystem030106 microbiologylcsh:Rlcsh:QR1-502lcsh:Medicinelcsh:RA1-1270030501 epidemiology610 Medical sciences; Medicineinfection controllcsh:MicrobiologyArticlenosokomiale Infektionen3. Good healthInfektionskontrolle03 medical and health sciences[ SDV.MHEP.MI ] Life Sciences [q-bio]/Human health and pathology/Infectious diseaseswater systemshealthcare-associated infectionsddc: 610[SDV.MHEP.MI]Life Sciences [q-bio]/Human health and pathology/Infectious diseasesNosocomial infectionsPseudomonas aeruginosa0305 other medical scienceGMS Hygiene and Infection Control
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Prevalence of Listeria spp. and characterization of Listeria monocytogenes isolated from food products in Tetouan, Morocco

2018

A total of 1096 food samples were purchased in Tetouan, North-Western of Morocco, to examine the presence of Listeria spp. Eighty (7.3%) of the tested samples were found positive for the presence of Listeria spp., while L. monocytogenes was detected in 16 (1.5%) samples. L. monocytogenes isolates belonged to clonal complexes CC2 (PCR serogroup IVb) and CC199 (PCR serogroup Ila) and to 8 different combined AscI/Apal pulsed-field gel electrophoresis profiles. Core genome multilocus sequence typing (cgMLST) allowed to distinguish 12 different cgMLST types and revealed the presence of 3 clusters of closely-related isolates from different samples, suggesting the existence of common sources of co…

0301 basic medicinemedicine.drug_classListeriaPCR-Serogrouping030106 microbiologyAntibioticsPrevalenceBiologymedicine.disease_causeMicrobiology03 medical and health sciencesListeria monocytogenes[SDV.MHEP.MI]Life Sciences [q-bio]/Human health and pathology/Infectious diseasesmedicineComputingMilieux_MISCELLANEOUS2. Zero hungerGel electrophoresisbusiness.industryPFGEbiology.organism_classificationFood safety[SDV.MP.BAC]Life Sciences [q-bio]/Microbiology and Parasitology/BacteriologyMorocco030104 developmental biology[SDV.MP]Life Sciences [q-bio]/Microbiology and ParasitologyFood productsListeriaMultilocus sequence typingcgMLSTbusiness[SDV.MHEP]Life Sciences [q-bio]/Human health and pathologyFood ScienceBiotechnology
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