Search results for "MIM"

showing 10 items of 645 documents

Synthesis and Molecular Modeling Studies of Derivatives of a Highly Potent Peptidomimetic Vinyl Ester as Falcipain-2 Inhibitors

2012

Herein we report the synthesis of a set of constrained peptidomimetics endowed with an electrophilic vinyl ester warhead and structurally related to a previously identified lead compound, a potent and irreversible inhibitor of falcipain-2 (FP-2). FP-2 is the main hemoglobinase of the malaria parasite P. falciparum. The new compounds were evaluated for their inhibition against FP-2, and the results were rationalized on the basis of docking experiments. These studies underscore the pivotal role of both the ester function at the P1' site and the trifluoromethyl group of the P3 side chain in determining the correct orientation of the Michael acceptor warhead in the catalytic site, and as a cons…

peptidomimeticdMolecular modelPeptidomimeticStereochemistryPlasmodium falciparumVinyl esterBiochemistrycysteine proteasesfalcipain-2 inhibitorsAntimalarialschemistry.chemical_compoundCatalytic DomainDrug DiscoverySide chainHumansEnzyme InhibitorsMalaria FalciparumGeneral Pharmacology Toxicology and PharmaceuticsPharmacologyTrifluoromethylOrganic Chemistrydocking studiescysteine proteases; peptidomimeticd; docking studies; falcipain-2 inhibitorsMolecular Docking SimulationCysteine EndopeptidaseschemistryDocking (molecular)Michael reactionMolecular MedicinePeptidomimeticsLead compoundChemMedChem
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Synthesis of Hybrid Tripeptide Peptidomimetics Containing Dehydroamino Acid and Aminophosphonic Acid in the Chain and Evaluation of Their Activity to…

2021

Synthesis of a new group of hybrid phosphonodehydropeptides composed of glycyl-(Z)-dehydrophenylalanine and structurally variable aminophosphonates alongside with investigations of their activity towards cathepsin C are presented. Obtained results suggest that the introduction of (Z)- dehydrophenylalanine residue into the short phosphonopeptide chain does induce the ordered conformation. Investigated peptides appeared to act as weak or moderate inhibitors of cathepsin C.

phosphonopeptidesmolecular modelingMolecular ConformationBioengineeringGeneral ChemistryGeneral MedicineBiochemistryCathepsin Cdehydropeptidesstructure-activity relationinhibitorsMolecular MedicinePeptidomimeticsDPPIPeptidesMolecular BiologyChemistry & Biodiversity
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Sopravvivenze del mimetismo animale: lo sguardo, l’aptico e il postumano

2022

La ricerca di Roger Caillois sul mimetismo animale, avviata in ambito surrealista già negli anni Trenta, si fondava su alcuni interessi per l’entomologia e le società primitive, su solidi studi sul mito e alcune incursioni nella psicopatologia, mentre le spiegazioni fornite riconducevano il fenomeno a una necessità di assimilazione allo spazio e a una inerzia dello slancio di vita, in aperto contrasto con le teorie darwiniane della selezione naturale. Una interpretazione non utilitaristica faceva del mimetismo un “lusso dispendioso” di alcune specie animali che, per ragioni non adattive, mettono in campo alcune tipologie precise di comportamenti: l’invisibilità, il travestimento e l’initimi…

posthumanmimetismo animalesguardoanimal mimicrySettore L-FIL-LET/14 - Critica Letteraria E Letterature ComparatemediaRoger Cailloipostumanogaze
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Mobile - käyttöliittymä Michel Butorin tekstikoneeseen

2014

poststructuralismreceptionmyytitrepresentationvastaanottohypertekstigenretButor Micheltulkintamythmetafiktiointertextualitypoststrukturalismiintertekstuaalisuusmimesisdialogisuussimulacrumopen worktekstilajitmultimodaalisuustekijyys
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Hard to catch: Experimental evidence supports evasive mimicry

2021

Most research on aposematism has focused on chemically defended prey, but the signalling difficulty of capture remains poorly explored. Similar to classical Batesian and Müllerian mimicry related to distastefulness, such ‘evasive aposematism' may also lead to convergence in warning colours, known as evasive mimicry. A prime candidate group for evasive mimicry areAdelphabutterflies, which are agile insects and show remarkable colour pattern convergence. We tested the ability of naive blue tits to learn to avoid and generalizeAdelphawing patterns associated with the difficulty of capture and compared their response to that of birds that learned to associate the same wing patterns with distast…

prey defence0106 biological sciencesEvolutionComputer scienceAposematismModels Biological010603 evolutionary biology01 natural sciencesGeneral Biochemistry Genetics and Molecular BiologyMüllerian mimicryPredationSongbirds03 medical and health sciencesAvoidance learningGeneralization (learning)AnimalsWings AnimalGeneral Environmental Science030304 developmental biology[SDV.EE]Life Sciences [q-bio]/Ecology environment0303 health sciencesWingconvergenceGeneral Immunology and Microbiologybiology[SDV.BA]Life Sciences [q-bio]/Animal biologyBiological MimicryGeneral MedicineAdelphabiology.organism_classificationBiological EvolutionBatesian mimicrypredator learningEvolutionary biologyPredatory Behavior1181 Ecology evolutionary biologyMimicryevasive aposematismAdelphaGeneral Agricultural and Biological SciencesdistastefulnessButterflies
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Wstydliwy problem erotyzmu

2017

Usually we are ashamed to touch the issue of eroticism, although it is a ąuite natural one and, in fact, very close to us. It seems that roots of this shyness date back to the biblical paradise and to the original sin committed by the first people. Since the exile from paradise the erotic sphere is a kind of taboo that we are afraid to invade. Bataille measures wits with this problem very courageously, showing that eroticism played a key role in the pagan religions. With a help of eroticism it was possible to make a transgression (exceed ban), reach sacrum and thereby fully experience the existence. Then Christianity distanced to eroticism and, paradoxically, by associating it with unclean …

profamimerotyzmsacrumBatailleprofanumeroseroticismKerenyiEleusistransgressiontransgresjaNowa Krytyka. Czasopismo Filozoficzne
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Nuevos materiales inorgánicos mediante estrategias de síntesis biomiméticas

2015

Hace cincuenta años que un físico llamado Robert Feynman divisó el principio de la era nanotecnológica, en la que actualmente nos estamos adentrando. Lo que no llegó a imaginar, es hasta que punto se multiplicarían las aplicaciones en el mundo de lo extremadamente pequeño. Microrrobots que navegan por nuestras arterias, ordenadores del tamaño de una mota de polvo, materiales con propiedades extraordinarias e incluso algunos sistemas para eliminar residuos, son algunos de los prodigios que anuncia esta disciplina. Algunos ejemplos de los nuevos materiales que se podrían obtener gracias a la nanotecnología podrían ser: nanotubos de carbono para el desarrollo de células o pilas de combustible …

quimica inorgánicabiomimetismoUNESCO::QUÍMICAnanotecnologia:QUÍMICA [UNESCO]ciencia materialessintesis y caracterización materiales inorgánicos
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Mimesis and Mediation in the Semana Santa Processions of Granada

2017

religionmimesisreligious practicesmediationkulkueetSemana Santa
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Demo 161. Resistencia eléctrica de un metal y de un semimetal. Bombillas de filamento incandescente: tungsteno vs. carbono

2021

Se presenta una demostración de aula que muestra que la curva voltaje-intensidad del filamento de una bombilla incandescente es no lineal. Para un filamento de tungsteno se observa que la resistencia eléctrica aumenta con la temperatura del filamento, la cual aumenta con la potencia eléctrica consumida, pues esta se disipa por radiación según la ley de Stefan. Para un filamento de carbono se observa que la resistencia eléctrica disminuye con la temperatura, evidenciando así que no es un metal (sino un semimetal). A classroom demonstration is presented showing that the voltage-intensity curve of the filament of an incandescent light bulb is non-linear. For a tungsten filament, it is observed…

resistor no óhmicobombilla incandescenteUNESCO::FÍSICAcoeficiente de temperatura de la resistividadley de Stefansemimetalecuación de Drude de la conductividad
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Synthesis and biological evaluation of novel peptidomimetics as rhodesain inhibitors

2016

Novel rhodesain inhibitors were developed by combining an enantiomerically pure 3-bromoisoxazoline warhead with a 1,4-benzodiazepine scaffold as specific recognition moiety. All compounds were proven to inhibit rhodesain with Ki values in the low-micromolar range. Their activity towards rhodesain was found to be coupled to an in vitro antitrypanosomal activity, with IC50 values ranging from the mid-micromolar to a low-micromolar value for the most active rhodesain inhibitor (R,S,S)-3. All compounds showed a good selectivity against the target enzyme since all of them were proven to be poor inhibitors of human cathepsin L. Novel rhodesain inhibitors were developed by combining an enantiomeri…

rhodesainPharmacologychemistry.chemical_classificationCathepsinPeptidomimetic010405 organic chemistryChemistryPeptidomimeticProton Magnetic Resonance SpectroscopyenPeptidomimetics; rhodesain; trypanosomaGeneral Medicine01 natural sciencesCombinatorial chemistryIn vitro0104 chemical sciencesCysteine Endopeptidases010404 medicinal & biomolecular chemistryEnzymeDrug DiscoveryIc50 valuesMoietyPeptidomimeticsCarbon-13 Magnetic Resonance SpectroscopytrypanosomaBiological evaluationJournal of Enzyme Inhibition and Medicinal Chemistry
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