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Search results for: MDRUG DELIVERY
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Inhibitors of glucosamine-6-phosphate synthase as potential antimicrobials or antidiabetics – synthesis and properties
PublicationGlucosamine-6-phosphate synthase (GlcN-6-P synthase) is known as a promising target for antimicrobial agents and antidiabetics. Several compounds of natural or synthetic origin have been identified as inhibitors of this enzyme. This set comprises highly selective L-glutamine, amino sugar phosphate or transition state intermediate cis-enolamine analogues. Relatively low antimicrobial activity of these inhibitors, poorly penetrating...
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Recent progress in the development of steroid sulfatase inhibitors – examples of the novel and most promising compounds from the last decade
PublicationThe purpose of this review article is to provide an overview of recent achievements in the synthesis of novel steroid sulfatase (STS) inhibitors. STS is a crucial enzyme in the biosynthesis of active hormones (including estrogens and androgens) and, therefore, represents an extremely attractive molecular target for the development of hormone-dependent cancer therapies. The inhibition of STS may effectively reduce the availability...
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Advanced polarization sensitive analysis in optical coherence tomography
PublicationThe optical coherence tomography (OCT) is an optical imaging method, which is widely applied in variety applications. This technology is used to cross-sectional or surface imaging with high resolution in non-contact and non-destructive way. OCT is very useful in medical applications like ophthalmology, dermatology or dentistry, as well as beyond biomedical fields like stress mapping in polymers or protective coatings defects detection....
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The KLC Cultures, Tacit Knowledge, and Trust Contribution to Organizational Intelligence Activation
PublicationIn this paper, the authors address a new approach to three organizational, functional cultures: knowledge culture, learning culture, and collaboration culture, named together the KLC cultures. Authors claim that the KLC approach in knowledge-driven organizations must be designed and nourished to leverage knowledge and intellectual capital. It is suggested that they are necessary for simultaneous implementation because no one of...
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Spin-Resolved Band Structure of Hoffman Clathrate [Fe(pz)2Pt(CN)4] as an Essential Tool to Predict Optical Spectra of Metal–Organic Frameworks
PublicationParamount spin-crossover properties of the 3D-Hoffman metalorganic framework (MOF) [Fe(pz)2Pt(CN)4] are generally described on the basis of the ligand field theory, which provides adequate insight into theoretical and simulation analysis of spintronic complexes. However, the ligand field approximation does not take into account the 3D periodicity of the actual complex lattice and surface effects and therefore cannot predict a full-scale...
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Performance and Emission Modelling and Simulation of Marine Diesel Engines using Publicly Available Engine Data
PublicationTo analyse the behaviour of marine diesel engines in unsteady states for different purposes, for example to determine the fuel consumption or emissions level, to adjust the control strategy, to manage the maintenance, etc., a goal-based mathematical model that can be easily implemented for simulation is necessary. Such a model usually requires a wide range of operating data, measured on a test stand. This is a time-consuming process...
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Tailoring optical constants of few-layer black phosphorus coatings: Spectroscopic ellipsometry approach supported by ab-initio simulation
Publication2D black phosphorus (BP) has attracted extensive attention as an anisotropic platform for novel optoelectronic and polarizing optics applications. Insight into the factors that tune the optical and polarizing properties of 2D BP reveals their essential influence on BP-based photonic and optoelectronic devices. In this work, studies of the optical constants of few-layer black phosphorus coatings are studied and discussed, with particular...
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Effect of nitrogen doping on TiOxNy thin film formation at reactive high-power pulsed magnetron sputtering
PublicationThe paper is focused on a study of formation of TiOxNy thin films prepared by pulsed magnetron sputtering of metallic Ti target. Oxygen and nitrogen were delivered into the discharge in the form of reactive gases O2 and N2. The films were deposited by high-power impulse magnetron sputtering working with discharge repetition frequency f = 250 Hz at low (p = 0.75 Pa) and high (p = 10 Pa) pressure. The substrates were on floating...
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Analysis of the possibility of creep damage detection in T24 heat resistant steel with the help of magnetic nondestestructive testing methods
PublicationThe paper presents the result of an analysis of applicability of various electromagnetic methods of nondestructive evaluation for creep damage detection in a novel heat resistant steel - T24 grade. Two sample sets, cut out from membrane wall tubes, were investigated – the as-delivered one and another exploited for 36,000 h in a power plant. There are described results of magnetic hysteresis loops B(H), Barkhausen noise (BN) and...
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Theory and application of Near-infrared spectroscopy
PublicationIn recent years one can observe a significant increase in the requirements on quality control in all industrial sectors. The growing number of involved analyses makes the traditional, time consuming, requiring use of large quantities of reagents, thus expansive methods inconvenient especially for industrial applications. Fortunately, there is a very fast, cheap and not invasive analytical method that is increasingly used in qualitative...
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INFOGEST inter-laboratory recommendations for assaying gastric and pancreatic lipases activities prior to in vitro digestion studies
PublicationIn vitro digestion studies often use animal digestive enzyme extracts as substitutes of human gastric and pancreatic secretions. Pancreatin from porcine origin is thus commonly used to provide relevant pancreatic enzymes such as proteases, amylase and lipase. Rabbit gastric extracts (RGE) have been recently introduced to provide gastric lipase in addition to pepsin. Before preparing simulated gastric and pancreatic extracts with...
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Enhanced capacitance of composite TiO2 nanotube / boron-doped diamond electrodes studied by impedance spectroscopy
PublicationWe report on the novel composite nanostructures based on boron-doped diamond thin film grown on top of TiO2 nanotubes. The nanostructures made of BDD-modified titania nanotubes showed an increase in activity and performance when used as electrodes in electrochemical environments. The BDD thin films (~200-500 nm) were deposited using microwave plasma assisted chemical vapor deposition (MW PA CVD) onto anodically fabricated TiO2...
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THE APPLICATION EFFECTS OF CONTINUOUS SATELLITE MEASUREMENTS OF RAILWAY LINES
PublicationThe paper presents results of satel lite surveying of the railway's rout es, which have been conducted just after starting in Poland (in 2008) the Active Geodesy Network ASG-EU POS. Afterwards it was possible to effectively utilize the GNSS survey ing results for the inventory of the (exploring) railways in service. Already at the beginning of 2009, the research team from Gdansk University of Technology and Naval Academy in Gdynia,...
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The Effect of Sterols on Amphotericin B Self-Aggregation in a Lipid Bilayer as Revealed by Free Energy Simulations
PublicationAmphotericin B (AmB) is an effective but toxic antifungal drug, known to increase the permeability of the cell membrane, presumably by assembling into transmembrane pores in a sterol-dependent manner. The aggregation of AmB molecules in a phospholipid bilayer is, thus, crucial for the drug’s activity. To provide an insight into the molecular nature of this process, here, we report an atomistic molecular dynamics simulation study...
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The occurence and diagnosis of biomarkers of ethyl alcohol consumption
PublicationEthyl alcohol is a legal and a widely available psychoactive drug. However, its excessive consumption causes addiction. This leads to aggressive behaviors, family battery, difficulties in interpersonal relations, legal offences, suicides, car accidents and deterioration in labor productivity, what causes financial problems. Despite many social actions against alcohol consumption, this problem is still unresolved. Therefore, fast...
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Experimental and Machine-Learning-Assisted Design of Pharmaceutically Acceptable Deep Eutectic Solvents for the Solubility Improvement of Non-Selective COX Inhibitors Ibuprofen and Ketoprofen
PublicationDeep eutectic solvents (DESs) are commonly used in pharmaceutical applications as excellent solubilizers of active substances. This study investigated the tuning of ibuprofen and ketoprofen solubility utilizing DESs containing choline chloride or betaine as hydrogen bond acceptors and various polyols (ethylene glycol, diethylene glycol, triethylene glycol, glycerol, 1,2-propanediol, 1,3-butanediol) as hydrogen bond donors. Experimental...
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Experimental and Machine-Learning-Assisted Design of Pharmaceutically Acceptable Deep Eutectic Solvents for the Solubility Improvement of Non-Selective COX Inhibitors Ibuprofen and Ketoprofen
PublicationDeep eutectic solvents (DESs) are commonly used in pharmaceutical applications as excellent solubilizers of active substances. This study investigated the tuning of ibuprofen and ketoprofen solubility utilizing DESs containing choline chloride or betaine as hydrogen bond acceptors and various polyols (ethylene glycol, diethylene glycol, triethylene glycol, glycerol, 1,2-propanediol, 1,3-butanediol) as hydrogen bond donors. Experimental...
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Explicit solvent repulsive scaling replica exchange molecular dynamics ( RS‐REMD ) in molecular modeling of protein‐glycosaminoglycan complexes
PublicationGlycosaminoglcyans (GAGs), linear anionic periodic polysaccharides, are crucial for many biologically relevant functions in the extracellular matrix. By interacting with proteins GAGs mediate processes such as cancer development, cell proliferation and the onset of neurodegenerative diseases. Despite this eminent importance of GAGs, they still represent a limited focus for the computational community in comparison to other classes...
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HDAC Inhibitors: Innovative Strategies for Their Design and Applications
PublicationHistone deacetylases (HDACs) are a large family of epigenetic metalloenzymes that are involved in gene transcription and regulation, cell proliferation, differentiation, migration, and death, as well as angiogenesis. Particularly, disorders of the HDACs expression are linked to the development of many types of cancer and neurodegenerative diseases, making them interesting molecular targets for the design of new efficient drugs...
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Triazoloacridone C-1305 impairs XBP1 splicing by acting as a potential IRE1α endoribonuclease inhibitor
PublicationInositol requiring enzyme 1 alpha (IRE1α) is one of three signaling sensors in the unfolding protein response (UPR) that alleviates endoplasmic reticulum (ER) stress in cells and functions to promote cell survival. During conditions of irrevocable stress, proapoptotic gene expression is induced to promote cell death. One of the three signaling stressors, IRE1α is an serine/threonine-protein kinase/endoribonuclease (RNase) that...
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High-Resolution Discharge Forecasting for Snowmelt and Rainfall Mixed Events
PublicationDischarge events induced by mixture of snowmelt and rainfall are strongly nonlinear due to consequences of rain-on-snow phenomena and snowmelt dependence on energy balance. However, they received relatively little attention, especially in high-resolution discharge forecasting. In this study, we use Random Forests models for 24 h discharge forecasting in 1 h resolution in a 105.9 km 2 urbanized catchment in NE Poland: Biala River....
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Hierarchical dissolved oxygen control for activated sludge processes
PublicationA hierarchical controller for tracking the dissolved oxygen reference trajectory in activated sludge processes is proposed and investigated. The removal of nitrogen and phosphorous from wastewater is considered. Typically, an aeration system itself is a complicated hybrid nonlinear dynamical system with faster dynamics compared to the internal dynamics of the dissolved oxygen in a biological reactor. It is a common approach to...
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Towards application of uncertainty quantification procedure combined with experimental procedure for assessment of the accuracy of the DEM approach dedicated for granular flow modeling
PublicationThere is a high demand for accurate and fast numerical models for dense granular flows found in many industrial applications. Nevertheless, before numerical model can be used its need to be always validated against experimental data. During the validation, it is important to consider how the measurement data sets, as well as the numerical models, are affected by errors and uncertainties. In this study, the uncertainty quantification...
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Privacy-Preserving, Scalable Blockchain-Based Solution for Monitoring Industrial Infrastructure in the Near Real-Time
PublicationThis paper proposes an improved monitoring and measuring system dedicated to industrial infrastructure. Our model achieves security of data by incorporating cryptographical methods and near real-time access by the use of virtual tree structure over records. The currently available blockchain networks are not very well adapted to tasks related to the continuous monitoring of the parameters of industrial installations. In the database...
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Occurrences, sources, and transport of organochlorine pesticides in the aquatic environment of Antarctica
PublicationWe review information on the concentration levels of organochlorine pesticides in the abiotic aquatic environment (in seawater, sea ice, surface freshwater, snow, firn, and glacial ice) and the organisms inhabiting those, in Antarctica. Particular attention is given to the environmental fate of these pollutants, which modifies their impact on the organisms living in the Antarctic. OCPs have been delivered to the Antarctic environment...
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On time-dependent nonlinear dynamic response of micro-elastic solids
PublicationA new approach to the mechanical response of micro-mechanic problems is presented using the modified couple stress theory. This model captured micro-turns due to micro-particles' rotations which could be essential for microstructural materials and/or at small scales. In a micro media based on the small rotations, sub-particles can also turn except the whole domain rotation. However, this framework is competent for a static medium....
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Biofilm bakteryjny uropatogennych szczepów E. coli Dr+ jako czynnik indukujący przewlekłość zakażeń dróg moczowych ograniczający ich leczenie
PublicationZakażenia dróg moczowych (ZUM) stanowią jedne z najczęściej występujących infekcji bakteryjnych, dotykających każdego roku miliony osób na świecie. Problematyka tych zakażeń wynika z ich przewlekłości i nawrotów, pomimo stosowania terapii antybiotykowej oraz ciągle wzrastającej lekooporności uropatogenów je wywołujących. Dominującym czynnikiem etiologicznym ZUM są uropatogenne szczepy E. coli (UPECs), wykazujące zdolność do adhezji,...
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Simultaneous determination of ibuprofen and its metabolites in complex equine urine matrices by GC-EI-MS in excretion study in view of doping control
PublicationA novel assay for the simultaneous determination of ibuprofen (IBU) and its four probable metabolites, 1-hydroxyibuprofen (1-OH IBU), 2-hydroxyibuprofen (2-OH IBU), 3-hydroxyibuprofen (3-OH IBU) and carboxyibuprofen (CBX IBU) in equine urine samples with the application of Gas Chromatography-Electron Ionization-Mass Spectrometry (GC-EI-MS) has been developed and elaborated. The new approach for sample preparation including minimizing...
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A multi‑criteria approach to investigate spatial distribution,sources, and the potential toxicological effect of polycyclic aromatic hydrocarbons (PAHs) in sediments of urban retention tanks
PublicationBottom sediments deposited in retention tanks (RTs) located on two urban streams (Oliwski and Strzyza) in the central part of Gdansk (Poland) were analysed for polycyclic aromatic hydrocarbons’ (PAHs) content. PAHs were extracted from samples with methylene chloride, then the extracts were subjected to clean-up applying the solid phase extraction (SPE) method. Quantitative and qualitative determination of 16 PAHs was performed...
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Bacteriophages as potential tools for use in antimicrobial therapy and vaccine development
PublicationThe constantly growing number of people suffering from bacterial, viral, or fungal infections, parasitic diseases, and cancers prompts the search for innovative methods of disease prevention and treatment, especially based on vaccines and targeted therapy. An additional problem is the global threat to humanity resulting from the increasing resistance of bacteria to commonly used antibiotics. Conventional vaccines based on bacteria...
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Transport of paracetamol in swellable and relaxing polyurethane nanocomposite hydrogels
PublicationPolyurethane hydrogels are potentially attractive materials for biomedical applications. They are able to absorb large amount of water, biological fluids or active substances, and thus, they have potential to be used as absorbents or wound-healing dressings. They are also used for the controlled release of therapeutics because of their capacity to embed biologically active agents in their water-swollen network. The presence of...
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Development of potential candidate reference materials for drugs in bottom sediment, cod and herring tissues
PublicationRegular use of a reference material and participation in a proficiency testing program can improve the reliability of analytical data. This paper presents the preparation of candidate reference materials for the drugs metoprolol, propranolol, carbamazepine, naproxen, and acenocoumarol in freshwater bottom sediment and cod and herring tissues. These reference materials are not available commercially. Drugs (between 7 ng/g and 32...
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In vitro and in silico assessment of anti-inflammatory activity of cocoa powders
PublicationPlants are considered the major sources of biologically active compounds, which provide unlimited opportunities for their use either as medical treatments or as novel drug formulations. Cocoa powder is frequently used in nutrition and is known to have many benefits thanks to its wide range of biological activities. The presented study was focused on th evaluation of the anti-inflammatory potential of extracts obtained from cocoa...
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A novel hierarchically-porous diamondized polyacrylonitrile sponge-like electrodes for acetaminophen electrochemical detection
PublicationA novel composite electrode material consisting of tangled fibrous polyacrylonitrile-based hierarchically-struc- tured nanocomposites has been produced by wet-spinning, carbonized and decorated with a carbon nano- architecture by microwave plasma-enhanced chemical vapor deposition and investigated as a metal-free electrode for the enhanced electrochemical detection of acetaminophen. Surprisingly, the hierarchical fiber ar- chitecture...
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Targeting DNA Topoisomerase II in Antifungal Chemotherapy.
PublicationTopoisomerase inhibitors have been in use clinically for the treatment of several diseases for decades. Although those enzymes are significant molecular targets in antibacterial and anticancer chemotherapy very little is known about the possibilities to target fungal topoisomerase II (topo II). Raising concern for the fungal infections, lack of effective drugs and a phenomenon of multidrug resistance underlie a strong need to expand...
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Design, synthesis, and biological evaluation of tetrahydroquinolinones and tetrahydroquinolines with anticancer activity
PublicationColorectal cancer (CRC) is the most commonly diagnosed cancer in Europe and the United States and the second leading cause of cancer related mortality. A therapeutic strategy used for the treatment of CRC involves targeting the intracellular levels of reactive oxygen species (ROS). In this study, we synthesized a series of novel tetrahydroquinolinones and assessed their ability to inhibit CRC growth and proliferation by evoking...
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Activation of peroxymonosulfate using carbon black nano-spheres/calcium alginate hydrogel matrix for degradation of acetaminophen: Fe3O4 co-immobilization and microbial community response
PublicationHerein, we focused on the degradation of acetaminophen (ACT) drug in liquid phase by peroxymonosulfate (PMS) activated by carbon black nano-spheres (CBNS). The nanostructured activator was immobilized into calcium alginate hydrogel matrix (CAHM) to avoid the washout of the fine nanostructures. The Langmuir modeling showed an insignificant contribution to the adsorption process in the removal of ACT. The basic pH conditions favored...
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Effect of chemical structure on complexation efficiency of aromatic drugs with cyclodextrins: The example of dibenzazepine derivatives
PublicationIt is widely believed that the hydrophobic effect governs the binding of guest molecules to cyclodextrins (CDs). However, it is also known that high hydrophobicity of guest molecules does not always translate to the formation of stable inclusion complexes with CDs. Indeed, a plethora of other factors can play a role in the efficiency of guest–CD interactions, rendering structure-based prediction of the complexation efficiency with...
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GNSS INVENTORY OF HISTORIC NARROW-GAUGE RAILWAY LINE IN KOSZALIN UNDER EXTREMELY UNFAVORABLE MEASUREMENTS CONDITIONS FROM THE POINT OF VIEW OF SATELLITE SIGNALS AVAILABILITY
PublicationA team of academic researchers from the Gdańsk University of Technology, Gdynia Maritime University and the Polish Naval Academy have been working since 2009 on the methodology of using active GNSS geodetic networks for geodetic inventory of railways and on adapting this measurement technique for designing geometric layouts of railway and tram lines. Over the years, the team tested a variety of configurations of receivers and settings...
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Quantitative Assessment of Operation of Ship Main Diesel Engine
PublicationOperation of ship propulsion system is associated with realization of definite operational goals. If to elements of the system the operational reliability strategy could be applied, the situation would be very simple as existing conditions would unambiguously determine application of means being on hand. However decision to reject application of the strategy (even if hypothetical) becomes obvious with a view of necessity of ensuring...
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The role and importance of the intellectual capital of the academic library – Gdańsk Tech Library Circulation Services case study / Rola kapitału intelektualnego biblioteki akademickiej na przykładzie doświadczeń Sekcji Obsługi Czytelnika Biblioteki Politechniki Gdańskiej
PublicationSkuteczne zarządzanie zasobami kapitału intelektualnego danej sekcji biblioteki akademickiej może być jednym z czynników wpływających na wysokie oceny usług bibliotecznych jej użytkowników. Może ono wpływać na wzrost kapitału intelektualnego biblioteki akademickiej, w strukturach której się znajduje. W sposób pośredni może oddziaływać również na poziom kapitału intelektualnego uczelni. Głównym celem autorek było przedstawienie...
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Designing digital displays and interactive media in today’s cities by night. Do we know enough about attracting attention to do so?
PublicationWith the huge transformation in the development of digital screen technology and its consistently decreasing cost, digital billboards are progressively replacing traditional static, two-dimensional poster advertisements in our cities1. Previously, due to the substantial expenditure involved, they were only available to major international brands with vast promotional resources to build their brand fame. Today, however, they are...
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Review of Recent Advancement on Nature/Bio-inspired Antenna Designs
PublicationThis article presents an extensive examination of antennas rooted in nature and biology, showcasing their remarkable performance across a wide spectrum of frequencies—from microwave to terahertz. The limitations of traditional antenna design have become increasingly evident in the face of burgeoning demands for novel communication technologies. Conventional analytical-equation-based approaches struggle to deliver the combined performance...
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Game-based Sprint retrospectives: multiple action research
PublicationIn today’s fast-paced world of rapid technological change, software development teams need to constantly revise their work practices. Not surprisingly, regular reflection on how to become more effective is perceived as one of the most important principles of Agile Software Development. Nevertheless, running an effective and enjoyable retrospective meeting is still a challenge in real environments. As reported by several studies,...
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Funkcjonowanie zespołów napędu hydraulicznego maszyn w niskich temperaturach otoczenia
PublicationW pracy przedstawiono cztery warianty klasyfikacji rozruchów oziębionego napędu hydraulicznego. Pierwsza sytuacja dotyczy zagadnienia, w którym wszystkie zespoły układu napędowego wraz z olejem mają taką samą niską temperaturę podczas rozruchu. Pozostałe warianty odnoszą się do rozruchu w warunkach szoku termicznego wywołanych zasilaniem ciepłym czynnikiem roboczym oziębionych zespołów hydraulicznych. Rozruch zespołów...
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First report on echinocandin resistant Polish Candida isolates
PublicationPurpose: Candida spp. are ranked as one of the four major causative agents of fungal infections. The number of infections caused by Candida species resistant to fluconazole, which is applied as the first line drug in candidiasis treatment, increases every year. In such cases the application of echinocandin is necessary. Echinocandin susceptibility testing has become a routine laboratory practice in many countries due to the increasing...
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Modification of gradient HPLC method for determination of small molecules' affinity to human serum albumin under column safety conditions: Robustness and chemometrics study
PublicationIn the early stages of drug discovery, beyond the biological activity screening, determining the physicochemical properties that affect the distribution of molecules in the human body is an essential step. Plasma protein binding (PPB) is one of the most important investigated endpoints. Nevertheless, the methodology for measuring %PPB is significantly less popular and standardized than other physicochemical properties, like lipophilicity....
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Mechanism of reaction of RNA-dependent RNA polymerase from SARS-CoV-2
PublicationWe combine molecular dynamics, statistical mechanics, and hybrid quantum mechanics/molecular mechanics simulations to describe mechanistically the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) RNA-dependent RNA polymerase (RdRp). Our study analyzes the binding mode of both natural triphosphate substrates as well as remdesivir triphosphate (the active form of drug), which is bound preferentially over ATP by RdRp while...
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Effect of choline chloride based natural deep eutectic solvents on aqueous solubility and thermodynamic properties of acetaminophen
PublicationIn this work, natural deep eutectic solvents (NADESs) containing choline chloride as hydrogen bond acceptor and 1,2-propanediol, malic acid and tartaric acid as hydrogen bond donors have been synthesized and applied to enhance the aqueous solubility of model sparingly water-soluble drug – acetaminophen. The results indicate that the greatest impact on the solubility of acetaminophen have deep eutectic solvents based on 1,2-propanediol...
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TiO2-based magnetic nanocomposites with core-shell structure
PublicationThe main aim of the doctoral dissertation was preparation and characterization of photocatalysts, with particular emphasis on modified titanium (IV) oxide photocatalysts, which can be applied for the degradation of organic pollutants not susceptible to biodegradation. A particularly important aspect of the work was the development of preparation method of nanocomposites with the magnetic core-shell and photocatalyst shell (TiO2)...