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Wyniki wyszukiwania dla: active pharmaceutical ingredients
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Approaches Towards Better Immunosuppressive Agents
PublikacjaSeveral classes of compounds are applied in clinics due to their immunosuppressive properties in transplantology and the treatment of autoimmune diseases. Derivatives of mycophe-nolic acid, corticosteroids and chemotherapeutics bearing heterocyclic moieties like methotrexate, azathioprine, mizoribine, and ruxolitinib are active substances with investigated mechanisms of action. However, improved synthetic approaches of known drugs...
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Influence of Dielectric Overlay Permittivity on Size and Performance of Miniaturized ESPAR Antenna
PublikacjaIn this paper, influence of dielectric overlay permittivity on miniaturized ESPAR antenna parameters is presented. ESPAR antenna is a low-cost and energy-efficient way to implement beam steering capability to a node and improve network performance. The antenna size reduction is obtained by embedding its active and passive elements in ABS based materials of relative permittivity equal to 4, 5.5 and 7.5 in order to achieve network...
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Experimental study of the multi-disc negative brake for a hydraulic motor
PublikacjaThis paper describes the methodology for experimental testing of a multi-disc brake. The construction of this brake was also present. The brake is dedicated to hydraulic motors with a small working volume. Experimental tests were carried out on a brake with plates immersed in oil and, for comparison, tests were carried out on a dry brake. As a result of the tests, the permissible torque (load) that is able to transfer the brake...
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Anticancer Properties of Amino Acid and Peptide Derivatives of Mycophenolic Acid
PublikacjaBackground: Although Mycophenolic Acid (MPA) is applied as prodrugs in clinic as an immunosuppressant, it also possesses anticancer activity. MPA acts as Inosine-5’-Monophosphate Dehydrogenase (IMPDH) inhibitor, where the carboxylic group at the end of the side chain interacts with Ser 276 of the enzyme via hydrogen bonds. Therefore, MPA derivatives with other polar groups indicated high inhibition too. On the other hand, potent...
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A new cold-adapted beta-D-galactosidase from the Antarctic Arthrobacter sp. 32c - gene cloning, overexpression, purification and properties
PublikacjaThe development of a new cold-active β-D-galactosidases and microorganisms that efficiently ferment lactose is of high biotechnological interest, particularly for lactose removal in milk and dairy products at low temperatures and for cheese whey bioremediation processes with simultaneous bio-ethanol production. In this article, we present a new β-D-galactosidase as a candidate to be applied in the above mentioned biotechnological...
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The role of aluminium in metal–organic frameworks derived carbon doped with cobalt in electrocatalytic oxygen evolution reaction
PublikacjaWater electrolysis is one of the most crucial processes in the development of new energy sources, where ultra-clean fuel is produced - hydrogen. Oxygen evolution reaction (OER) is the sluggish process of overall water splitting. Therefore, this study presents the design, characterization and electrochemical study of cobalt-based electrocatalysts embedded into porous carbons derived from an Al-metal–organic...
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Novel steroid sulfatase inhibitors based on N ‐thiophosphorylated 3‐(4‐aminophenyl)‐coumarin‐7‐O‐sulfamates
PublikacjaIn the present work, we described convenient methods for the synthesis ofN-thiophosphorylated 3-(4-aminophenyl)-coumarin-7-O-sulfamates as steroid sulfatase(STS) inhibitors. To design the structures of the potential STS inhibitors, molecularmodeling techniques were used. A computational docking method was used to deter-mine the binding modes of the synthesized inhibitors as well as to identify potentialinteractions between specified...
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New methodology for determination cationic surfactants in liquid environmental samples
PublikacjaBecause of their specific physical and chemical properties (e.g. amphiphilicity, solubility in polar and nonpolar liquids, ability to form micelles, adsorption at phase boundaries, low toxicity) surfactants (surface-active compounds) are widely applied in industry and in the household. As their applications are on a very large scale, it has become necessary to acquire a more detailed understanding of their environmental fate. Mainly,...
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Imidazoacridinone antitumor agent C-1311 as a selective mechanism- based inactivator of human cytochrome P450 1A2 and 3A4 isoenzymes.
Publikacja5-Diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311), a promising antitumor agent that is also active against autoimmune diseases, was determined to be a selective inhibitor of the cytochrome P450 (CYP) 1A2 and 3A4 isoenzymes. Therefore, C-1311 might modulate the effectiveness of other drugs used in multidrug therapy. The present work aimed to identify the mechanism of the observed C-1311-mediated inactivation of CYP1A2...
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Recombinant !ermostable AP Exonuclease from Thermoanaerobacter tengcongensis: Cloning, Expression, Purification, Properties and PCR Application
PublikacjaApurinic/apyrimidinic (AP) sites in DNA are considered to be highly mutagenic and must be corrected to preserve genetic integrity, especially at high temperatures. !e gene encoding a homologue of AP exonuclease was cloned from the thermophilic anaerobic bacterium Thermoanaerobacter tengcongensis and transformed into Escherichia coli. The protein product showed high identity (80%) to human Ape1 nuclease, whereas to E. coli exonuclease...
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Knowledge‐Intensive Business Services (KIBS) and Their Role in the Knowledge‐Based Economy
PublikacjaThe importance of the knowledge‐intensive business services sector for the development of the economy is growing. In the 80s and 90s this sector became the fastest growing sector in the OECD countries (OECD, 2001). Many publications stress its close relationship to the levels of innovation and performance of the whole economy (e.g. Hipp, 1999; Tomlinson, 1999; Aslesen and Isaksen, 2007). It is an increasingly common belief that...
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Train the trainer course
PublikacjaThis chapter presents the concept, evaluation and evaluation results for the train the trainer. This concept of train the trainers is prepared within Workpackage 5 of EU-funded project: MASTER BSR (Erasmus+ Strategic Partnership Programme). Due to the nature of adult learning the content is designed for the use of participatory methods (involved, active). This method uses various techniques of active learning e.g. group work,...
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Synthesis, characteristics, and photocatalytic activity of zinc oxide nanoparticles stabilized on the stone surface for degradation of metronidazole from aqueous solution
PublikacjaAbstract Background: The presence of antibiotics such as metronidazole in wastewater even at low concentrations requires searching for a suitable process such as advanced oxidation process (AOP) to reduce the level of pollutants to a standard level in water. Methods: In this study, zinc oxide (ZnO) nanoparticles were synthesized by thermal method using zinc sulfate (ZnSO4) as a precursor, then, stabilized on stone and was used...
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Application of COSMO-RS-DARE as a Tool for Testing Consistency of Solubility Data: Case of Coumarin in Neat Alcohols
PublikacjaCoumarin is a naturally occurring lactone-type benzopyrone with various applications in the pharmaceutical, food, perfume, and cosmetics industries. This hydrophobic compound is poorly soluble in water but dissolves well in protic organic solvents such as alcohols. Despite the extensive use of coumarin, there are only a few reports documenting its solubility in organic solvents, and some reported data are incongruent, which...
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Transport of Particles in Intestinal Mucus under Simulated Infant and Adult Physiological Conditions: Impact of Mucus Structure and Extracellular DNA
PublikacjaThe final boundary between digested food and the cells that take up nutrients in the small intestine is a protective layer of mucus. In this work, the microstructural organization and permeability of the intestinal mucus have been determined under conditions simulating those of infant and adult human small intestines. As a model, we used the mucus from the proximal (jejunal) small intestines of piglets and adult pigs. Confocal...
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Fluorescence studies by quenching and protein unfolding on the interaction of bioactive compounds in water extracts of kiwi fruit cultivars with human serum albumin
PublikacjaThe main aim of this investigation was to characterize new kiwi fruit cultivars after cold storage treatment and to determine the similarities and differences between them, using spectroscopic methods. The chemometric comparison of kiwi fruit cultivars based on physicochemical indices during cold storage was carried out. All kiwi fruit cultivars showed a high level of correlation between the contents of phenolic compounds (polyphenols,...
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Polymer and graphitic carbon nitride based nanohybrids for the photocatalytic degradation of pharmaceuticals in wastewater treatment – A review
PublikacjaPharmaceuticals, including antibiotics and anti-inflammatory drugs, have been frequently detected in water reservoirs, in concentrations ranging from ng/L to μg/L, owing to their wide use in treatment of human and animal disease. Their uncontrolled use results in their increased release into the environment which is harmful for humans, animals, aquatic life and aquatic system. To remove these pollutants from water bodies, various...
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Elucidation of chemical compounds in different extracts of two Lavandula taxa and their biological potentials: Walking with versatile agents on the road from nature to functional applications
PublikacjaDue to their health-promoting and nutraceutical properties, lavenders are frequently employed in the food and pharmaceutical industries. Here, we focused on investigate the chemical profile of hexane, MeOH, and water extracts of leaf, flower, and root of L. pedunculata and L. stoechas and to assess their antioxidant, enzyme inhibitory, and antibacterial properties. The highest total polyphenolic and flavonoids contents were recorded...
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Regulacja napięcia w sieci nN z rozproszonymi źródłami energii
PublikacjaPodłączanie rozproszonych źródeł energii do sieci energetycznych niskiego napięcia powoduje powstawanie problemów zmienności i niesymetrii napięcia, zwłaszcza w przypadku dużych odległości od transformatora zasilającego. W skrajnych przypadkach zachodzi konieczność redukcji mocy generowanej przez źródło podczas oddawaniu energii do sieci. Rozwiązaniem tego problemu jest zastosowanie energoelektronicznego regulatora napięcia składającego...
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Simultaneous Removal of Al, Cu and Zn Ions from Aqueous Solutions Using Ion and Precipitate Flotation Methods
PublikacjaThis paper presents the results of investigations concerning the simultaneous removal of Al(III), Cu(II), and Zn(II) from dilute aqueous solutions using ion and precipitate flotation methods. The effects of initial solution pH, surface active substance concentration, and the gas velocity on the flotations’ efficiency and course are studied. Experimental results are discussed in terms of physicochemical aspects related to aqueous...
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Structural Factors Affecting Cytotoxic Activity of (E)-1-(Benzo[d ][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one Derivatives
PublikacjaDerivatives of (E)-1-(5-alkoxybenzo[d][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one (1) demonstrated exceptionally high in vitro cytotoxic activity, with IC50 values of the most active derivatives in the nanomolar range. To identify structural fragments necessary for the activity, several analogs deprived of selected fragments were prepared, and their cytotoxic activity was tested. It was found that the activity depends on combined effects...
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Affective computing and affective learning – methods, tools and prospects
PublikacjaEvery teacher knows that interest, active participation and motivation are important factors in the learning process. At the same time e-learning environments almost always address only the cognitive aspects of education. This paper provides a brief review of methods used for affect recognition, representation and processing as well as investigates how these methods may be used to address affective aspect of e-education. The paper...
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Voltage and frequency regulation of a standalone induction generator by reduced-rating power electronic compensators - comparative evaluation
PublikacjaIn this paper are considered two fundamental topologies of power electronic compensators for voltage and frequency control of a standalone self-excited induction generator (IG) system. These are voltage and current source inverter based shunt compensators with energy storage. The aim of this study is to assess main features of both topologies in dynamic and steady-state IG operation. The whole system is modelled with the aid of...
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Visual Lip Contour Detection for the Purpose of Speech Recognition
PublikacjaA method for visual detection of lip contours in frontal recordings of speakers is described and evaluated. The purpose of the method is to facilitate speech recognition with visual features extracted from a mouth region. Different Active Appearance Models are employed for finding lips in video frames and for lip shape and texture statistical description. Search initialization procedure is proposed and error measure values are...
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GaN Nanowire Array for Charge Transfer in Hybrid GaN/P3HT:PC71BM Photovoltaic Heterostructure Fabricated on Silicon
PublikacjaAbstract: We demonstrate that a GaN nanowire array can be used for efficient charge transfer between the organic photovoltaic layer and silicon in a Si/GaN/P3HT:PC71BM inverted hybrid heterostructure. The band alignment of such a material combination is favorable to facilitate exciton dissociation, carrier separation and electron transport into Si. The ordered nature of the GaN array helps to mitigate the intrinsic performance...
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Application of galvanodynamic impedance spectroscopy for studying passive film cracking under mechanical strain
PublikacjaThe paper reports the results of simultaneous mechanical and electrochemical investigations on austenitic (18/8) stainless steel in a 2 % solution of sulphuric acid. The measurements were performed using Galvanodynamic Electrochemical Impedance Spectroscopy (GDEIS). Electrochemical analysis of mechanical passive layer cracking and repassivation conditions during a tensile test was carried out. Application of this methodology allowed...
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Analityka surfaktantów w próbkach środowiskowych
PublikacjaSurfaktanty stanowią grupę związków charakteryzujących się specyficznymi właściwościami fizykochemicznymi (m.in. amfifilowa budowa, zdolność rozpuszczania się w cieczach o różnej polarności, zdolność do tworzenia micelli) i z tego względu są one wykorzystywane w wielu sferach działalności człowieka. Związki powierzchniowo-czynne ulegają różnorodnym przemianom fizykochemicznym, co umożliwia ich migrację między różnymi elementami...
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Vowel recognition based on acoustic and visual features
PublikacjaW artykule zaprezentowano metodę, która może ułatwić naukę mowy dla osób z wadami słuchu. Opracowany system rozpoznawania samogłosek wykorzystuje łączną analizę parametrów akustycznych i wizualnych sygnału mowy. Parametry akustyczne bazują na współczynnikach mel-cepstralnych. Do wyznaczenia parametrów wizualnych z kształtu i ruchu ust zastosowano Active Shape Models. Jako klasyfikator użyto sztuczną sieć neuronową. Działanie systemu...
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Efficiency of service recovery in scale-free optical networks under multiple node failures
PublikacjaIn this paper we examine the properties of scale-free networks in case of simultaneous failures of two networknodes. Survivability assumptions are as follows: end-to-end path protection with two node-disjoint backup pathsfor each working path. We investigate three models of scale-free networks generation: IG, PFP and BA.Simulations were to measure the lengths of active and backup paths and the values of service recovery time.We...
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Determination of pitting corrosion stage of stainless steel by galvanodynamic impedance spectroscopy
PublikacjaThis paper investigates the methodology for differentiation of multistep process of pitting corrosion of AISI 304 stainless steel in the environment of iron (III) chloride. Measurements were performed using Galvanodynamic Electrochemical Impedance Spectroscopy (GDEIS). Application of this methodology allowed monitoring of natural corrosion process without external current (IDC = 0A) nor potential perturbation of the system. Applied...
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New plasmonic platform for enhanced luminescence of Valrubicin
PublikacjaLuminescence enhanced by new structure of plasmonic platform with aluminum oxide (Al2O3) buffer layer deposited on gold nanostructures is investigated. Regularly distributed gold nanostructures of average dimension of 50 nm formed the active part of plasmonic platforms. They were manufactured on Corning 1737 glass substrate by melting of gold thin film. The nanostructures were coated by dielectric Al2O3 thin film with thickness...
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Innovative Railway Stations
PublikacjaIn relation to modern demographic trends, evolving technologies and environmentfriendly solutions increases the potential of rail considered as sustainable form of public transport. Contemporary tendencies of designing railway stations in Europe are focused on lowering energy consumption and reducing carbon emission. The main goal of the designers is to create a friendly and intuitive space for its users and at the same time a...
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Image Processing Techniques for Distributed Grid Applications
PublikacjaParallel approaches to 2D and 3D convolution processing of series of images have been presented. A distributed, practically oriented, 2D spatial convolution scheme has been elaborated and extended into the temporal domain. Complexity of the scheme has been determined and analysed with respect to coefficients in convolution kernels. Possibilities of parallelisation of the convolution operations have been analysed and the results...
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Application of analytical procedure based on accelerated solvent extraction and ion chromatography technique for determination of thiocyanate and other inorganic ions in human placenta samples
PublikacjaExposure of a pregnant woman during pregnancy is a special case of exposure to toxic substances. Samples of placenta collected for the studies had been prepared with the technique of accelerated solvent extraction and later analyzed for the presence of thiocyanate ion and other inorganic ions, with the use of the technique of ion chromatography. The concentration of thiocyanate ion in placenta samples collected from active smokers...
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Nanocrystalline cathode functional layer for SOFC
PublikacjaRecently, it was shown that thin functional layers introduced between an electrolyte and cathode might improve cathode performance. However, the mechanism of this improvement still needs analysis. In this paper, a thin (∼140 nm), spin-coated perovskite layer (La0.6Sr0.4Co0.2Fe0.8O3-δ) was placed between a cathode (La0.6Sr0.4Co0.2Fe0.8O3-δ) and an electrolyte (Ce0.8Gd0.2O2-δ) and the effects of this investigated. The microstructure...
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Analysis and bioanalysis: an effective tool for data collection of environmental conditions and processes
PublikacjaReliable information that allows us to estimate the state of the environment and to forecast changes in the ecosystem are constantly required. Increasing environmental consciousness and dynamic development of analytical techniques are the main reasons for determining the wide range of pollutants occurring at very low concentrations in complex matrix samples. The presence and concentration of many of those pollutants in the environment...
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Chemosensitization of multidrug resistant Candida albicans by the oxathiolone fused chalcone derivatives
PublikacjaThree structurally related oxathiolone fused chalcone derivatives appeared effective chemosensitizers, able to restore in part sensitivity to fluconazole of multidrug-resistant C.albicans strains. Compound 21 effectively chemosensitized cells resistant due to the overexpression of the MDR1 gene, compound 6 reduced resistance of cells overexpressing the ABC-type drug transporters CDR1/CDR2 and derivative 18 partially reversed fluconazole...
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Design of synchronous generator two inputs regulator based on hinf control theory.
PublikacjaThe power system is highly nonlinear system, its dynamics depends on system network configuration, system loading… etc. To overcome the above mentioned difficulties and fulfill the performance requirements the different control methods are considered and tested for design of synchronous generator control system. Application of the H optimization method to synchronous generator regulator based on measurement of generator voltage...
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Model prodłużniczy i model prowierzycielski – porównanie skuteczności prawa upadłościowego
PublikacjaBankruptcy in court proceedings has been of interest to researchers for many years. Researchers look for internal and external factors which influence the effectiveness and efficiency of bankruptcy proceedings; for example, the impact of the country’s level of development on the efficiency of bankruptcy proceedings, a system of incentives for the active participation of creditors in bankruptcy proceedings to increase their recovery...
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Pharmacomicrobiomics of cell-cycle specific anti-cancer drugs – is it a new perspective for personalized treatment of cancer patients?
PublikacjaIntestinal bacteria are equipped with an enzyme apparatus that is involved in the active biotrans-formation of xenobiotics, including drugs. Pharmacomicrobiomics, a new area of pharmacology, analyses interactions between bacteria and xenobiotics. However, there is another side to the coin. Pharmacotherapeutic agents can significantly modify the microbiota, which consequently affects their efficacy. In this review, we comprehensively...
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Signal conditioning for examination of shallow-water acoustic noise correlation properties
PublikacjaThe article describes the process of signal conditioning for examination of acoustic noise correlation properties in shallow water. Knowledge of these properties is very important for the design processes of passive and active hydroacoustic systems. This paper focuses on the above issue from the point of view of passive sonar. In sonar systems, signal processing algorithms operate on both useful acoustic signals, and accompanying...
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New approach for the synthesis of Ag3PO4-graphene photocatalysts
PublikacjaA facile and effective plasma sputtering method for the preparation of a visible light active photocatalyst - rhombic dodecahedral silver phosphate Ag3PO4 covered with nanographene (Ag3PO4-GR) with improved stability has been developed. Proposed method allows for the usage of readily available materials for nanographene sputtering and for easy scaling-up. The stability improvement, confirmed by visible light-induced phenol degradation...
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(4-(Bis(4-Fluorophenyl)Methyl)Piperazin-1-yl)(Cyclohexyl)Methanone Hydrochloride (LDK1229): A New Cannabinoid CB1 Receptor Inverse Agonist from the Class of Benzhydryl Piperazine Analogs
PublikacjaSome inverse agonists of cannabinoid receptor type 1 (CB1) have been demonstrated to be anorectic antiobesity drug candidates. However, the first generation of CB1 inverse agonists, represented by rimonabant (SR141716A), otenabant, and taranabant, are centrally active, with a high level of psychiatric side effects. Hence, the discovery of CB1 inverse agonists with a chemical scaffold distinct from these holds promise for developing...
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Structural studies of a cold-adapted dimeric Beta-D-galactosidase from Paracoccus sp. 32d
PublikacjaThe crystal structure of a novel dimeric [beta]-D-galactosidase from Paracoccus sp. 32d (Par[beta]DG) was solved in space group P212121 at a resolution of 2.4 Å by molecular replacement with multiple models using the BALBES software. This enzyme belongs to glycoside hydrolase family 2 (GH2), similar to the tetrameric and hexameric [beta]-D-galactosidases from Escherichia coli and Arthrobacter sp. C2-2, respectively. It is the second...
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Rotation Triggers Nucleotide-Independent Conformational Transition of the Empty β Subunit of F1-ATPase
PublikacjaF1-ATPase (F1) is the catalytic portion of ATP synthase, a rotary motor protein that couples proton gradients to ATP synthesis. Driven by a proton flux, the F1 asymmetric γ subunit undergoes a stepwise rotation inside the α3β3 headpiece and causes the β subunits’ binding sites to cycle between states of different affinity for nucleotides. These concerted transitions drive the synthesis of ATP from ADP and phosphate. Here, we study...
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Book Review
PublikacjaActing over the last three decades as an Editor and Associate Editor for a number of international journals in the general area of cybernetics and AI, as well as a Chair and Co-Chair of numerous conferences in this field, I have had the exciting opportunity to closely witness and to be actively engaged in the stimulating research area of machine learning and its important augmentation with deep learning techniques and technologies. From...
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Possibility of Using Tea Fungus for Fermentation of Beetroot and Carrot Pomace Beverages
PublikacjaFermented beverages obtained from plant-based raw materials are becoming more popular due to their beneficial effects on human health. These include kombucha beverages, which are obtained by fermenting tea brew using the so-called tea fungus, which includes acetic acid bacteria and osmophilic yeast. A consortium of these microorganisms could also be used to prepare functional fermented beverages obtained from extracts of vegetable...
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Modified Preisach model of hysteresis in multi air gap ferrite core medium frequency transformer
PublikacjaThis article presents the modified Preisach model of hysteresis for a 3-phase medium frequency transformer in a 100 kW dual active bridge converter. The transformer magnetic core is assembled out of ferrite I-cores, which results in multiple parasitic air gaps. For this transformer, the hysteresis loops were measured and parameters of the Preisach model were determined. The Preisach distribution function is approximated with a...
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Labour resources in Azerbeijan
PublikacjaThe article aims to assess the changes of the Azerbaijani labour resources through deductive analysis of historical data and observation of changes in the structure of resources based on generally available macroeconomic data. Analysis shows that, during the period considered, the population of Azerbaijan increased, with a majority living in cities. Universal access to education enabled a growing group of Azerbaijanis to complete...
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Efficiency of exciton splitting in organic photovoltaic cells within EQE spectrum
PublikacjaThe paper presents a procedure of estimating the efficiency of exciton splitting at ED/EA interface. The procedure consists in evaluation of splitting of excitons into electron-hole pairs on the basis of the external quantum efficiency spectra of planar cells and spectra of absorbance of active organic layers. The fitting parameters are the exciton splitting probabilities at ED/EA interface. The presented procedure was applied...