Search results for "AFRICA"

showing 10 items of 962 documents

Predicting 19F NMR Chemical Shifts: A Combined Computational and Experimental Study of a Trypanosomal Oxidoreductase–Inhibitor Complex

2020

Abstract The absence of fluorine from most biomolecules renders it an excellent probe for NMR spectroscopy to monitor inhibitor–protein interactions. However, predicting the binding mode of a fluorinated ligand from a chemical shift (or vice versa) has been challenging due to the high electron density of the fluorine atom. Nonetheless, reliable 19F chemical‐shift predictions to deduce ligand‐binding modes hold great potential for in silico drug design. Herein, we present a systematic QM/MM study to predict the 19F NMR chemical shifts of a covalently bound fluorinated inhibitor to the essential oxidoreductase tryparedoxin (Tpx) from African trypanosomes, the causative agent of African sleepi…

Trypanosoma brucei bruceiProtozoan ProteinsContext (language use)PyrimidinonesThiophenes010402 general chemistry01 natural sciencesCatalysisquantum chemistryThioredoxinsNMR spectroscopyComputational chemistryOxidoreductasestructural biologyEnzyme InhibitorsNuclear Magnetic Resonance Biomolecularchemistry.chemical_classificationAfrican sleeping sickness010405 organic chemistryChemistryChemical shiftCommunicationGeneral ChemistryNuclear magnetic resonance spectroscopyFluorineOxidoreductase inhibitorLigand (biochemistry)Trypanocidal AgentsCommunications0104 chemical sciencesStructural biologyCovalent bondddc:540Mutationcovalent inhibitorsProtein BindingAngewandte Chemie (International Ed. in English)
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Optimization Strategy of Novel Peptide-Based Michael Acceptors for the Treatment of Human African Trypanosomiasis

2019

This paper describes an optimization strategy of the highly active vinyl ketone 3 which was recognized as a strong inhibitor of rhodesain of Trypanosoma brucei rhodesiense, endowed with a ksecond v...

Trypanosoma brucei rhodesienseStrong inhibitorKetoneStereochemistryProtein ConformationPeptide01 natural sciences03 medical and health sciencesStructure-Activity RelationshipSUBSTRATEDrug DiscoverymedicineHumansAfrican trypanosomiasisSulfonesBIOLOGICAL EVALUATION030304 developmental biologyWARHEADchemistry.chemical_classification0303 health sciencesMolecular StructureChemistryDERIVATIVESTrypanosoma brucei rhodesienseCYSTEINE PROTEASES RHODESAIN BIOLOGICAL EVALUATION CATHEPSIN-L INHIBITORS BRUCEI PEPTIDOMIMETICS FALCIPAIN-2 DERIVATIVES SUBSTRATE WARHEADBRUCEImedicine.diseaseFALCIPAIN-2Trypanocidal Agents0104 chemical sciences010404 medicinal & biomolecular chemistryCysteine EndopeptidasesTrypanosomiasis AfricanCYSTEINE PROTEASES RHODESAINCATHEPSIN-LMolecular MedicineINHIBITORSPEPTIDOMIMETICS
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Development of Novel Benzodiazepine-Based Peptidomimetics as Inhibitors of Rhodesain from Trypanosoma brucei rhodesiense.

2020

Starting from the reversible rhodesain inhibitors 1 a-c, which have Ki values towards the target protease in the low-micromolar range, we have designed a series of peptidomimetics, 2 a-g, that contain a benzodiazepine scaffold as a β-turn mimetic; they are characterized by a specific peptide sequence for the inhibition of rhodesain. Considering that irreversible inhibition is strongly desirable in the case of a parasitic target, a vinyl ester moiety acting as Michael-acceptor was introduced as the warhead; this portion was functionalized in order to evaluate the size of corresponding enzyme pocket that could accommodate this substituent. With this investigation, we identified an irreversibl…

Trypanosoma brucei rhodesiensehuman African trypanosomiasiStereochemistryPeptidomimeticmedicine.medical_treatmentSubstituentAntiprotozoal AgentsTrypanosoma bruceiCysteine Proteinase Inhibitors01 natural sciencesBiochemistrychemistry.chemical_compoundBenzodiazepinesStructure-Activity RelationshipDrug DevelopmentParasitic Sensitivity TestsDrug DiscoverymedicineMoietyTrypanosoma bruceiGeneral Pharmacology Toxicology and PharmaceuticsPeptide sequencePharmacologyrhodesainProteasebiologyDose-Response Relationship DrugMolecular Structure010405 organic chemistryOrganic ChemistryTrypanosoma brucei rhodesiensebenzodiazepine scaffoldbiology.organism_classificationpeptidomimetic0104 chemical sciences010404 medicinal & biomolecular chemistryCysteine EndopeptidaseschemistryMolecular MedicinePeptidomimeticsMichael acceptorLead compoundChemMedChem
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Distribution et abondance des mouches piqueuses (Glossinidae, Stomoxys et Tabanidae) dans deux parcs nationaux du Gabon.

2015

11 pages; International audience; In order to minimize risks of pathogen transmission with the development of ecotourism in Gabon, a seasonal inventory has been performed in five contrasted biotopes in Ivindo (INP) and Moukalaba-Doudou (MDNP) National Parks. A total of 10,033 hematophagous flies were captured. The Glossinidae, with six different species identified, was the most abundant group and constitutes about 60% of the captured flies compared to the Stomoxys (6 species also identified) and Tabanidae with 28% and 12%, respectively. The Glossinidae showed a higher rate of capture in primary forest and in research camps. In INP, the Stomoxys showed a higher rate of capture in secondary f…

Tsetse FliesParks RecreationalPopulation DynamicsClimatic seasons[SDV.BID]Life Sciences [q-bio]/BiodiversityForestsDistributionlcsh:Infectious and parasitic diseasesSpecies SpecificityAnimalslcsh:RC109-216GabonEcosystemNational Parks[ SDV.BID ] Life Sciences [q-bio]/Biodiversity[ SDE.BE ] Environmental Sciences/Biodiversity and EcologyHematophagous fliesDipteraMuscidaeHumidityGrasslandGlossinidaeInsect VectorsTrypanosomiasis AfricanVirus DiseasesSeasons[SDE.BE]Environmental Sciences/Biodiversity and EcologyAnimal DistributionResearch Article
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Il teatro romano di Althiburos (El Medeina, El Kef, Tunisia)

2016

Il contributo presenta le attività della missione archeologica dell'Università di Macerata ad Althiburos per lo studio, lo scavo e la valorizzazione del teatro romano della città. Una missione svolta in collaborazione con l'Institut National du Patrimoine de Tunis ed il Politecnico di Bari a partire dal 2006. Le tre campagne di scavo (2007, 2009 e 2010, alle quali va aggiunta una campagna di ricognizione e ricerca di confronti nel 2014, con il cofinanziamento del MAE) hanno permesso di indagare le fasi più recenti della vita dell'edificio e di redigere un primo rilievo del monumento.

Tunisia Althiburos teatro romano architettura romana Africa proconsolareAlthiburoTunisiateatro romanoarchitettura romanaAlthiburosAfrica proconsolare
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Nouveaux enjeux pour l'école moyenne en Afrique

2005

05113; On constate aujourd'hui une augmentation massive de la scolarité des 12-16 ans dans les pays africains en développement. Ce phénomène est lié au développement voulu et obtenu des scolarités primaires.Pour diverses raisons, l'école moyenneconstitue un cycle terminal pour la grande majorité des enfants qui la fréquentent. Son organisation actuelle, telle qu'on peut l'observer dans différents pays, est cependant très proche du collège secondaire français et donc inapte à fournir le cadre adéquat pour un cycle terminal générateur de progrès économiques et sociaux.Bâti sur cette problématique de l'articulation entre les flux d'élèves, les contenus pédagogiques et les modalités d'organisat…

Tunisia[SHS.EDU]Humanities and Social Sciences/Education[SHS.EDU] Humanities and Social Sciences/EducationEducational systemsOffre d'éducationTunisieDeveloping countriesAfriqueMadagascarPays en éveloppementNigerEducational developmentDéveloppement de l'éducationEnseignement de baseBasic educationMauritanieMauritaniaEconomic analysisTraining supply[ SHS.EDU ] Humanities and Social Sciences/EducationAnalyse économiqueSenegalContenu d'enseignementOrganisation du système éducatifTogoAfricaFranceCurriculum
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La conferenza Pan-Africana sulla gestione integrate delle coste (PACSICOM)

1999

Non disponibile

Tutela del mare Africa
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La protezione della fauna nella Repubblica Centrafricana: un caso sui generis di protezione ambientale in Africa

1996

L'articolo analizza il regime giuridico della protezione dell'ambiente nella Repubblica Centrafricana.

Tutela dell'ambiente Repubblica Centrafricana
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La lotta contro il bracconaggio in Africa: uno sguardo d’insieme

2000

Non disponibile

Tutela dell'ambiente bracconaggio Africa
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Radical analyticity and radical pro-drop scenarios of diachronic change in East and mainland Southeast Asia, West Africa and Pidgins and Creoles

2020

Abstract The paucity or absence of inflectional morphology (radical analyticity) and the omission of verbal arguments with no concomitant agreement (radical pro-drop) are well-known characteristics of East and mainland Southeast Asian languages (EMSEA). Both of them have a special status in typology and linguistic theory. Radical analyticity is known under the term of ‘morphological isolation’ and has recently been described as ‘diachronically anomalous’ (McWhorter 2016), while radical pro-drop is a theoretical challenge since Rizzi (1986). The present paper offers an alternative view on these characteristics based on data from EMSEA languages, radically analytic West African languages and …

TypologyThought experiment050101 languages & linguisticsHistory05 social sciencesGeneral MedicineSoutheast asian050105 experimental psychologyLinguisticsSoutheast asiaWest africaWest africanTheoretical linguistics0501 psychology and cognitive sciencesMainlandAsian Languages and Linguistics
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