Search results for "inhibitio"

showing 4 items of 594 documents

Dipeptidyl Enoates As Potent Rhodesain Inhibitors That Display a Dual Mode of Action

2015

Dipeptidyl enoates were prepared through a high-yielding two-step synthetic route. They have a dipeptidic structure with a 4-oxoenoate moiety as a warhead with multiple reactive sites. Dipeptidyl enoates were screened against rhodesain and human cathepsins B and L, and were found to be potent and selective inhibitors of rhodesain. Among them (S,E)-ethyl 5-((S)-2-{[(benzyloxy)carbonyl]amino}-3-phenylpropanamido)-7-methyl-4-oxooct-2-enoate (6) was the most potent, with an IC50 value of 16.4 nm and kinact/Ki=1.6×106 m−1 s−1 against rhodesain. These dipeptidyl enoates display a reversible mode of inhibition at very low concentrations and an irreversible mode at higher concentrations. Inhibition…

trypanosomiasisStereochemistrysleeping sicknessCathepsin LDrug Evaluation PreclinicalChemistry Techniques SyntheticInhibition kineticsCysteine Proteinase InhibitorsBiochemistryCathepsin BInhibitory Concentration 50Structure-Activity RelationshipinhibitorsDrug DiscoveryHumansMoietyMolecular Targeted TherapyGeneral Pharmacology Toxicology and PharmaceuticsIC50Volume concentrationrhodesainPharmacologyChemistryOrganic ChemistryDual modeDipeptidesTrypanocidal AgentsCombinatorial chemistryMolecular Docking SimulationCysteine EndopeptidasesKineticsdipeptidyl enoatesTrypanosomiasis AfricanDocking (molecular)Molecular MedicineCysteine thiolateChemMedChem
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2020 ESC Guidelines for the management of acute coronary syndromes in patients presenting without persistent ST-segment elevation

2020

2020 ESC Guidelines for the management of acute coronary syndromes in patients presenting without persistent ST-segment elevation

unstable anginaMyocardial ischaemia[SDV]Life Sciences [q-bio]Vascular damage Radboud Institute for Health Sciences [Radboudumc 16]dual antithrombotic therapyGuidelineheparin030204 cardiovascular system & hematologyPlatelet inhibitionantiplatelet0302 clinical medicineST segmentMedicinedabigatranMyocardial infarctionguidelinesglycoprotein iib/iiia inhibitorsanticoagulationNon-ST Elevated Myocardial InfarctionrivaroxabanComputingMilieux_MISCELLANEOUSreproductive and urinary physiologydiabetesbleedingsbivalirudinatherothrombosiDisease ManagementangioplastyGuidelines • acute cardiac care • acute coronary syndrome • angioplasty • anticoagulation • antiplatelet • apixaban • aspirin • atherothrombosis • betablockers • bleedings • bivalirudin • bypass surgery • cangrelor • chest pain unit • clopidogrel • dabigatran • diabetes • dual antithrombotic therapy • early invasive strategy • edoxaban • enoxaparin • European Society of Cardiology • fondaparinux • glycoprotein IIb/ IIIa inhibitors • heparin • high-sensitivity troponin • minoca • myocardial ischaemia • myocardial infarction • nitrates • non-ST-elevation myocardial infarction • platelet inhibition • prasugrel • recommendations • revascularization • rhythm monitoring • rivaroxaban • stent • ticagrelor • triple therapy • unstable anginaenoxaparinGeneral MedicineClopidogrel3. Good healthearly invasive strategymyocardial infarctiontriple therapy030220 oncology & carcinogenesisHigh sensitivity troponinembryonic structuresCardiologyPlatelet aggregation inhibitorrevascularizationbiological phenomena cell phenomena and immunityCardiology and Cardiovascular MedicineTicagrelormedicine.drugHumanrecommendationAcute coronary syndromemedicine.medical_specialtyaspiringlycoprotein IIb/IIIa inhibitornon-ST-elevation myocardial infarctionapixabanrhythm monitoringEuropean Society of Cardiologyticagrelor03 medical and health sciencesnitrateatherothrombosisbetablockersInternal medicineacute cardiac careminocachest pain unitDiseases of the circulatory (Cardiovascular) systemHumansIn patientAcute Coronary SyndromeclopidogrelUnstable anginaurogenital systemnitratesbusiness.industryfondaparinuxbetablockerArrhythmias Cardiac030229 sport sciencesbleedingmedicine.diseasemyocardial ischaemiaplatelet inhibitionprasugreldiabeteGlycoprotein IIb/IIIa inhibitorsRC666-701bypass surgerySettore MED/11 - MALATTIE DELL'APPARATO CARDIOVASCOLARErecommendationsedoxabanhigh-sensitivity troponinstentbusinessPlatelet Aggregation Inhibitorscangrelor
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Ikääntymisen ja synnynnäisen aerobisen suorituskyvyn vaikutukset varhaiseen tiedonkäsittelyyn rotilla

2016

Fyysisen aktiivisuuden vaikutukset aivojen toimintaan ja kognitiivisiin kykyihin ovat viime aikoina herättäneet kiinnostusta tutkijoiden keskuudessa. Näitä teemoja tutkii myös Active, Fit and Smart (AFIS) -tutkimushanke, jonka päämääränä on selvittää liikunnan yhteyksiä oppimiseen ja sen edellytyksiin elämän eri vaiheissa. Tämä tutkielma on toteutettu osana AFIS-projektia, ja se lähestyy aihetta aerobisen suorituskyvyn näkökulmasta. Tutkielman tavoitteena on selvittää, miten synnynnäinen aerobinen suorituskyky ja ikääntyminen vaikuttavat varhaiseen tiedonkäsittelyyn, joka sijoittuu aivan kognitiivisen tiedonkäsittelyketjun alkuun. Tämä tapahtui vertailemalla kahta synnynnäiseltä aerobiselta…

varhainen tiedonkäsittelyikääntyminenstartle-habituaatioprepulse inhibitioaerobinen suorituskyky
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(A,B) In vivo GCaMP6f signals recorded in layers M1, M5 and M9/10 of Mi1 (A) and Tm3 (B) neurons, before (blue, green) and after (gray, red) applicat…

2019

Sensory systems sequentially extract increasingly complex features. ON and OFF pathways, for example, encode increases or decreases of a stimulus from a common input. This ON/OFF pathway split is thought to occur at individual synaptic connections through a sign-inverting synapse in one of the pathways. Here, we show that ON selectivity is a multisynaptic process in the Drosophila visual system. A pharmacogenetics approach demonstrates that both glutamatergic inhibition through GluClα and GABAergic inhibition through Rdl mediate ON responses. Although neurons postsynaptic to the glutamatergic ON pathway input L1 lose all responses in GluClα mutants, they are resistant to a cell-type-specifi…

visionQH301-705.5GABA AgentsScienceModels Neurological610Sensory systemBiologyStimulus (physiology)distributed codingGeneral Biochemistry Genetics and Molecular BiologySynapseglutamatergic inhibition03 medical and health sciencesGlutamatergic0302 clinical medicinePostsynaptic potentialOff pathwayInterneuronsAnimalsVisual PathwaysExcitatory Amino Acid AgentsBiology (General)030304 developmental biology0303 health sciencesGeneral Immunology and MicrobiologyGABAergic inhibitionD. melanogasterON selectivityGeneral Neurosciencefeature extractionQRGeneral MedicineD. melanogaster; GABAergic inhibition; ON selectivity; distributed coding; feature extraction; glutamatergic inhibition; neuroscience; visionVisual PerceptionMedicineGabaergic inhibitionDrosophilaSelectivityNeuroscience030217 neurology & neurosurgeryResearch ArticleNeuroscience
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