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Search results for: UDP-GLUCURONOSYLTRANSFERASES
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Novel Resveratrol-Based Substrates for Human Hepatic, Renal, and Intestinal UDP-Glucuronosyltransferases
PublicationTrans-Resveratrol (tRes) has been shown to have powerful antioxidant, anti-inflammatory, anti-carcinogenic, and anti-aging properties; however, its use as a therapeutic agent is limited by its rapid metabolism into its conjugated forms by UDP-Glucuronosyltransferases (UGTs). The aim of the current study was to test the hypothesis that the limited bioavailability of tRes can be improved by modifying its structure to create analogs...
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Human UDP-Glucuronosyltransferases: Effects of altered expression in breast and pancreatic cancer cell lines.
PublicationIncreased aerobic glycolysis and de novo lipid biosynthesis are common characteristics of invasive cancers. UDP-glucuronosyltransferases (UGTs) are phase II drug metabolizing enzymes that in normal cells possess the ability to glucuronidate these lipids and speed their excretion; however, de-regulation of these enzymes in cancer cells can lead to an accumulation of bioactive lipids, which further fuels cancer progression. We hypothesize...
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Biotransformation of abused synthetic cannabinoids, JWH-018 and JWH-073, by human cytochromes P450 and UDP-glucuronosyltransferases
PublicationZwiązki oznaczone symbolami JWH-018 i JWH-073 są syntetycznymi pochodnymi kanabinoidów, obecnymi w preparatach o działaniu psychoaktywnym (K2/Spice). Wcześniejsze badań wykazały, że u osób przyjmujących tzw. ''legalną marihuanę'', głównymi produktami biotransformacji obecnymi w moczu były hydroksylowe pochodne obu związków, jak również ich glukuronidy. W związku z tym celem prowadzonych badań było określenie roli poszczególnych...
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Acridinone antitumor agents, C-1305 and C-1299 are metabolized rather by flavin-containing monooxygenases and UDP-glucuronosyltransferases than cytochromes P450
PublicationStwierdzono, że to monooksygenazy flawinowe, a nie enzymy cytochromu P450, są głównymi enzymami frakcji mikrosomalnej, odpowiedzialnymi za detoksyfikacyjny metabolizm dwóch badanych pochodnych triazoloakrydonu. Dodatkowo C-1305 ulega sprzęganiu w czasie drugiej fazy metabolizmu z kwasem glukuronowym do postaci O-glukuronidu
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Role of Human UDP-Glucuronosyltransferases in the Biotransformation of the Triazoloacridinone and Imidazoacridinone Antitumor Agents C-1305 and C-1311 : Highly Selective Substrates for UGT1A10
Publication5-Diethylaminoethylamino-8-hydroxyimidazoacridinone, C-1311 (NSC-645809), is an antitumor agent shown to be effective against breast cancer in phase II clinical trials. A similar compound, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone, C-1305, shows high activity against experimental tumors and is expected to have even more beneficial pharmacological properties than C-1311. Previously published studies showed that these...
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Drug-drug interaction potential of antitumor acridine agent C-1748: The substrate of UDP-glucuronosyltransferases 2B7, 2B17 and the inhibitor of 1A9 and 2B7
PublicationBackground The compound 9-(2′-hydroxyethylamino)-4-methyl-1-nitroacridine (C-1748), the promising antitumor agent developed in our laboratory was determined to undergo phase I metabolic pathways. The present studies aimed to know its biotransformation with phase II enzymes – UDP-glucuronosyltransferases (UGTs) and its potential to be engaged in drug-drug interactions arising from the modulation of UGT activity. Methods UGT-mediated...
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Contribution of UDP-glucuronosyltransferases (UGTs) in metabolism of acridinone antitumor agents, C-1311, C-1305, and their less active structural analogues, C-1330 and C-1299
PublicationCelem prowadzonych badań było określenie roli UDP-glukuronylotransferaz, uważanych za najważniejsze enzymy detoksykujące, w metabolizmie pochodnych imidazo- i triazoloakrydonu. Wykazano, że najbardziej aktywne przeciwnowotworowo związki z obu grup, tj. C-1311 i C-1305 są transformowane do O-glukuronidów, w przeciwieństwie do ich metoksylowych analogów, odpowiednio związku C-1330 i C-1299. Analiza składu mieszanin reakcyjnych zawierających...
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Enzymes of UDP-GlcNAc biosynthesis in yeast
PublicationD-glukozamina stanowi ważny składnik budulcowy głównych elementów strukturalnych grzybowej ściany komórkowej: chityny, chitozanu i mannoprotein. Inne aminocukry, takie jak D-mannozamina i D-galaktozamina, stosunkowo powszechne w komórkach wyższych organizmów eukariotycznych, rzadko występują u grzybów i są praktycznie nieobecne w komórkach drożdży i drożdżaków. Zawierający glukozaminę nukleotyd cukrowy UDP-GlcNAc jest syntezowany...
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Desensitization of glucosamine-6-phosphate synthase to inhibition by UDP-GlcNAc
PublicationGlucosamine-6-phosphate (GlcN-6-P) synthase, known also as L-Glutamine: D-fructose-6-phosphate amidotransferase, catalyzes the first committed step in the pathway leading to the ultimate formation of UDP-GlcNAc. The final product of this pathway is an activated precursor of numerous macromolecules containing amino sugars, including chitin and mannproteins in fungi, peptidoglycan and lipopolysaccharides in bacteria, and glycoproteins...
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UDP-glukuronylotransferazy - białka siateczki śródplazmatycznej. Struktura i mechanizm działania
PublicationIzoenzymy UDP-glukuronylotransferazy (EC. 2.4.1.17), UGT, katalizują w organizmach ssaków reakcję koniugacji grupy glikozylowej pochodzącej z nukleotydu UDPGA z aglikonem. UDPGA jest przyłączany do odpowiedniej grupy funkcyjnej metabolitu I fazy, rzadziej związku wyjściowego, przez co polarność aglikonu i zdolność jego wydalania z komórki zwiększa się, a to w konsekwencji obniża efekt toksyczny.Struktura UGT zawiera 2 domeny. Domena...
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Synthesis of conjugates of MDP and nor-MDP linked to tuftsin derivatives as potential immunomodulators
PublicationZsyntetyzowano nowe koniugaty muramylodipeptydu (MDP) i nor-muramylo-dipeptydu (nor-MDP) z pochodnymi tuftsyny zawierającymi wiązanie izopeptydowe na epsilon-aminowej grupie lizyny jako potencjalne immunomodulatory. Do syntezy wykorzystano metodę mieszanych bezwodników z chloromrówczanem izobutylu i N-metylomorfoliną w bezwodnym DMF. Końcowe produkty charakteryzowno za pomocą NMR, analizy elementarnej i analizy aminokwasowej na...
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UDP-glukuronylotranferazy w metabolizmie detoksykacyjnym i aktywacyjnym związków endogennych oraz ksenobiotyków
PublicationGlukuronidacja jest główną drogą koniugacji w szlakach metabolizmu i wydalania związków endogennych oraz ksenobiotyków. Reakcja ta jest katalizowana przez UDP-glukuronylotransferazy, UGT, dla których substratami są bilirubina, hormony steroidowe, tyroidowe i kwasy żółciowe, oraz związki egzogenne, w tym leki, związki kancerogenne, chemiczne zanieczyszczenia środowiska i składniki żywności. Z terapeutycznego punktu widzenia szczególnie...
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Niezawodność transmisji danych protokołu UDP w elektroenergetycznychsystemach teletransmisyjnych współpracujących z siecią Internet
PublicationW artykule przedstawiono istotę niezawodności transmisji danych przesyłanych - na podstawie zorientowanego bezpołączeniowo protokołu komunikacyjnego UDP - w elektroenergetycznych systemach teletransmisyjnych współpracujących z siecią Internet. Problematyka ta dotyczy szczególnie niewielkich (często bezobsługowych) obiektów elektroenergetycznych, w przypadku których proces monitorowania może być realizowany za pośrednictwem powszechnie...
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Synthesis of new conjugates of MDP and nor-MDP with retro-tuftsin derivatives as potential immunomodulators
PublicationZsyntetyzowano nowe analogi muramylodipeptydu (MDP) i nor-muramylo-dipeptydu (nor-MDP) z pochodnymi retro-tuftsyny jako potencjalne immunomodulatory. Przedstawiono także syntezę odpowiednich pochodnych retro-tuftsyny. Do syntezy wykorzystano metodę mieszanych bezwodników z chloromrówczanem izobutylu i N-metylomorfoliną w bezwodnym DMF.
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Badanie efektywności transmisji danych z wykorzystaniem protokołów TCP i UDP w systemie TETRA
PublicationW pracy przedstawiono wyniki badań i analiz związanych z efektywnością transmisji danych pakietowych w sieciach opartych na systemie TETRA. W oparciu o przeprowadzone badania symulacyjne, dokonano m.in. porównania efektywności transmisji danych pakietowych z wykorzystaniem protokołów FTP i TFTP, które bazują odpowiednio na protokołach warstwy transportowej: TCP i UDP. Protokoły TCP i UDP zostały porównane zarówno pod względem teoretycznym...
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Long range molecular dynamics study of regulation of eukaryotic glucosamine-6-phosphate synthase activity by UDP-GlcNAc
PublicationGlucosamine-6-phosphate (GlcN-6-P) synthase catalyses the first and practically irreversible step in hexosamine metabolism. The final product of this pathway, uridine 5' diphospho N-acetyl-D-glucosamine (UDPGlcNAc), is an essential substrate for assembly of bacterialand fungal cell walls. Moreover, the enzyme is involved in phenomenon of hexosamine induced insulin resistance in type II diabetes, which makes it a potential target...
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Long range molecular dynamics study of interactions of the eukaryotic glucosamine-6-phosphate synthase with fructose-6-phosphate and UDP-GlcNAc
PublicationGlucosamine-6-phosphate synthase (EC 2.6.1.16) is responsible for catalysis of the first and practically irreversible step in hexosamine metabolism. The final product of this pathway, uridine 5 diphospho Nacetyl- d-glucosamine (UDP-GlcNAc), is an essential substrate for assembly of bacterial and fungal cell walls. Moreover, the enzyme is involved in phenomenon of hexosamine induced insulin resistance in type II diabetes, which...
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Modification of quaternary structure of Candida albicans GlcN-6-P synthase and its desensitization to inhibition by UDP-GlcNAc by site-directed mutagenesis
PublicationSite-directed mutagenesis of the CaGFA1 gene encoding glucosamine-6-phosphate synthase from Candida albicans was performed. Desensitization of the enzyme to inhibition by UDPGlcNAc was achieved upon T487I and H492F substitutions at the UDP-GlcNAc binding site, exchange of D524, S525 and S527 for Ala at the dimer:dimer interface and construction of the tail-lock array (L434R and L460A) at the C-tail region. The first two sets if...
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Estimating and Forecasting GDP in Poland with Dynamic Factor Model
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LDFEM analysis of FDP auger installation in cohesive soil
PublicationThis paper deals with large deformation finite element (LDFE) preliminary modelling of Full Displacement Pile (FDP) installation in cohesive soil deposit located in Jazowa, Poland. The detailed FDP auger geometry is applied and the drilling process is modelled with full 3D Coupled Eulerian-Lagrangian (CEL) formulation. The total stress approach and elastic-perfectly plastic model with rate-dependent Mises plasticity is used. The...
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Modulation of UDP-glucuronidation by acridinone antitumor agents C-1305 and C-1311 in HepG2 and HT29 cell lines, despite slight impact in noncellular systems.
PublicationBackground Among the studied antitumor acridinone derivatives developed in our laboratory, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone (C-1305) and 5-diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311) exhibited cytotoxic and antitumor properties against several cancer types and were selected to be evaluated in preclinical and early-phase clinical trials. In the present work, we investigated the impact of C-1305...
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Odorous VOCs From Biosolids Detected By GC-MS/ODP
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The influence of new MDP and tuftsin analogs on cytokines levels in experimentally induced sepsis
PublicationPrzedstawiono wpływ analogów MDP z tuftsyną na poziom cytokin: TNF(alfa), IL6, IL10, INF(gamma). Wszystkie badane związki działały aktywująco na makrofagi narządowe i niezwykle efektywnie na monocyty krwi obwodowej. Na podstawie otrzymanych wyników można stwierdzić, że badane związki są za słabe by mogły działać jako samodzielne terapeutyki. ich zastosowanie w klinice upatruje się raczej w formie adjuwantów.
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Comparative model tests of SDP and CFA pile groups in non-cohesive soil
PublicationThe research topic relates to the subject of deep foundations supported on continuous flight auger (CFA) piles and screw displacement piles (SDP). The authors have decided to conduct model tests of foundations supported on the group of piles mentioned above and also the tests of the same piles working alone. The tests are ongoing in Geotechnical Laboratory of Gdańsk University of Technology. The description of test procedure, interpretation...
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Computationally Efficient Multi-Objective Optimization of and Experimental Validation of Yagi-Uda Antenna
PublicationIn this paper, computationally efficient multi-objective optimization of antenna structures is discussed. As a design case, we consider a multi-parameter planar Yagi-Uda antenna structure, featuring a driven element, three directors, and a feeding structure. Direct optimization of the high-fidelity electromagnetic (EM) antenna model is prohibitive in computational terms. Instead, our design methodology exploits response surface...
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Photovoltaic demonstration set up
PublicationThe use of photovoltaics is growing rapidly in the industry as well as households. Therefore, educating the public will help them understand solar cell technology, which is becoming more common in everyday life. This paper proposes a demonstrational set-up of photovoltaic panel for the purpose of science education. It was used in numerous outreach activities such as science fairs. Moreover, it proved to be a great tool for education...
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Wykorzystanie protokołu UPD do monitorowania obiektów za pośrednictwem publicznej sieci Internet
PublicationW artykule przedstawiono ideę monitorowania stanu rozproszonych obiektów za pośrednictwem publicznej sieci Internet z wykorzystaniem protokołu UDP. Omówiono właściwości różnych metod przesyłania danych oraz rodzaje i źródła błędów komunikacji powodujących utratę danych. Przedstawiono program komputerowy oraz metodykę badania niezawodności komunikacji za pomocą protokołu bezpołączeniowego UDP. Zaprezentowano wyniki badań niezawodności...
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Analogues of muramyl dipeptide (MDP) and tuftsin limit infection and inflammation in murine model of sepsis
PublicationBadano koniugaty MDP z tuftsyną oraz pochodną tuftsyny w leczeniu ciężkich infekcji bakteryjnych takich jak posocznica. Oceniano aktywność żerną komórek układu fagocytów jednojądrzastych, wpływ na klirens bakteryjny kluczowych organów wewnętrznych oraz ekspresję genów dla cytokin pro- i antyzapalnych charakterystycznych dla odpowiedzi immunologicznej w posocznicy i indukowanych działaniem analizowanych zwiazków. W badaniach in...
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Employment and export specialization patterns versus GDP per capita performance - unifying approach
PublicationThis paper analyses the evolution of specialization patterns along the process of economic development. The scope of the paper is twofold: first of all, it aims at understanding if the evolution of employment specialization is reflected in the same manner in trade specialisation patterns. Secondly, it explores the link between the degree of specialization on one side and cross country GDP per capita performance on the other. We...
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A Generalized SDP Multi-Objective Optimization Method for EM-Based Microwave Device Design
PublicationIn this article, a generalized sequential domain patching (GSDP) method for efficient multi-objective optimization based on electromagnetics (EM) simulation is proposed. The GSDP method allowing fast searching for Pareto fronts for two and three objectives is elaborated in detail in this paper. The GSDP method is compared with the NSGA-II method using multi-objective problems in the DTLZ series, and the results show the GSDP method...
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Optical activity and electro-optic effect of l-arginine doped KDP single crystals
PublicationWe have used the modified polarimetric methods to study optical activity (OA) in the potassium dihydrogenphosphate (KDP) crystals doped with 0.7, 1.4 and 3.8 wt% L-arginine (L-arg) amino acid. Crystals were grown by the temperature reduction method. Small changes of the absolute eigen waves ellipticity and OA values in doped crystals were noted. We have experimentally determined the signs of OA in the [1 00] and [01 0] directions...
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Badania terenowe przemieszczeniowych pali i kolumn wkręcanych typu SDP i SDC
PublicationPrzedstawiono opis badań pali i kolumn wkręcanych typu SDP i SDC na terenowym poletku doświadczalnym, wykonanych w ramach projektu badawczego MNiSW. Badania statyczne pali i kolumn wykonano z pomiarem rozdziału siły w trzonach i w powiązaniu z badaniami CPT podłoża gruntowego. Określono wartości oporów jednostkowych gruntów niespoistych wzdłuż pobocznicy i pod podstawą pali wkręcanych oraz przedstawiono je w relacji do oporów gruntu...
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10Kin1day: A Bottom-Up Neuroimaging Initiative
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10Kin1day: A bottom-up neuroimaging initiative
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Fabrication and Characterization of Flexible Medical-Grade TPU Filament for Fused Deposition Modeling 3DP Technology
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LDFEM analysis of pore water pressure development in cohesive soil due to FDP auger drilling
PublicationThis paper presents the preliminary modelling of FDP auger drilling in soft soil with emphasis on excess pore water pressure (EPWP) development using CEL formulation and Abaqus software suit. The EPWP generation in single points is investigated and the results of a numerical analysis are compared with the field measurements. It is found that numerical model qualitatively reflects the field measurements. However,...
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Fabrication and Characterization of Flexible Medical-Grade TPU Filament for Fused Deposition Modeling 3DP Technology
PublicationThe possibility of using additive manufacturing (AM) in the medicine area has created new opportunities in health care. This has contributed to a sharp increase in demand for 3D printers, their systems and materials that are adapted to strict medical requirements. We described herein a medical-grade thermoplastic polyurethane (S-TPU) which was developed and then formed into a filament for Fused Deposition Modeling (FDM) 3D printers...
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Low-Cost Multi-Objective Optimization Yagi-Uda Antenna in Multi-Dimensional Parameter Space
PublicationA surrogate-based technique for fast multi-objective optimization of a multi-parameter planar Yagi-Uda antenna structure is presented. The proposed method utilizes response surface approximation (RSA) models constructed using training samples obtained from evaluation of the low-fidelity antenna model. Utilization of the RSA models allowsfor fast determination of the best possible trade-offs between conflicting objectives in multi-objective...
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Damage Analysis of Tensioning Cable Anchorage Zone of a Bridge Superstructure, Using CDP Abaqus Material Model
PublicationNumerical analysis of the tensioning cables anchorage zone of a bridge superstructure is presented in this paper. It aims to identify why severe concrete cracking occurs during the tensioning process in the vicinity of anchor heads. In order to simulate the tensioning, among others, a so-called local numerical model of a section of the bridge superstructure was created in the Abaqus Finite Element Method (FEM) environment. The...
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Relationship among Economic Growth (GDP), Energy Consumption and Carbon Dioxide Emission: Evidence from V4 Countries
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Numerical simulation of extreme flooding in a built-up area
PublicationPrzedstawiono dwie numeryczne symulacje propagacji gwałtownej fali powodziowej przez schematyczny model obszaru zabudowanego. Do obliczeń wykorzystano równania przepływu wody płytkiej. Wyniki obliczeń porównano z dostępnymi pomiarami wykonanymi w laboratorium hydraulicznym ENEL-CESI w Mediolanie. Uzyskano zadowalającą zgodność symulacji z eksperymentami.
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SPECTRAL DYNAMIC ANALYSIS OF A STATIONARY JACK-UP PLATFORM
PublicationThe paper refers to the dynamic short-term response analysis of the Baltic steel drilling platform (see Fig.2) in a random sea-state represented by one-dimensional wave spectrum proposed by Striekalov and Massel and it is recommended for the Baltic Sea area. The Baltic drilling platform is a jack-up type platform for the exploration and exploitation of oil under the Baltic Sea. The analysis presented deals with the stationary...
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Low cost set-up for supercapacitors parameters evaluation
PublicationSupercapacitors are capable to store relatively high amount of energy comparing to its mass. Growing number of these devices applications requires development of new testing methods. Standard methods of evaluation of supercapacitor parameters, as cycling voltammetry, CV, galvanostatic cycling with potential limitation, GCPL, impedance measurements, require equipment of high cost...
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Selected problems of sensitivity and reliability of a jack-up platform
PublicationThe paper deals with sensitivity and reliability applications to numerical studies of an off-shore platform model. Structural parameters and sea conditions are referred to the Baltic jack-up drilling platform. The study aims at the influence of particular basic variables on static and dynamic response as well as the probability of failure due to water waves and wind loads. The paper presents the sensitivity approach to a generalized...
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Low cost set-up for supercapacitors parameters evaluation
PublicationWe propose a use of a power amplifier in the circuit of voltage to current converter (current driver) for supercapacitor charging/discharging in controlled conditions. The current driver is controlled by DAC output of DAQ board and voltage of DUT is measured and a control loop is realized by software. In the circuit the DC current method of evaluation of capacitance and equivalent series...
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Axial capacity of steel built-up battened columns
PublicationThis paper deals with the numerical investigation aimed to study the axial capacity of pin-ended steel built-up columns. Three methods of calculating forces in chords and batten, taking into account the material and geometric imperfections specified in the Eurocode 3 are considered. The aim of this study was to compare different methods allowing the calculation of the column load capacity and determine a simpler and faster method...
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Detoxification of the tricyclic antidepressant opipramol and its analog – IS-noh by UGT enzymes before and after activation by phase I enzymes in rat liver microsomes
PublicationThe present studies were carried out to evaluate the simultaneous one-pot metabolism of opipramol (IS-opi) and analog (IS-noh) by phase I and phase II enzymes present in rat liver microsomes (RLM) as an alternative to separate testing with recombinant enzymes. This approach allows for more time-saving and cost-effective screening of the metabolism of newly discovered drugs. We also considered that the lack of results for phase...
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The Economic Legacy of Mega Sporting Events. The Impact of Hosting European Olympic Games on GDP Growth Through Infrastructure Development
PublicationIntroduction. The positive legacy of the Olympics is often cited by the International Olympic Committee and national or-ganizers. Some scholars, however, question an uncritical approach to an exclusively positive economic legacy. The aim of this study is to evaluate the impact of hosting the Olympics on infrastructure development, with a potential impact on economic growth in the form of Gross Domestic Product (GDP) in three phases...
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T cell Activation Is Driven by an ADP-Dependent Glukosinase Linking Enhanced Glycolysis with Mitochondrial Reactive Oxygen Species Generation
PublicationMitochondria-originating reactive oxygen species control T cell receptor (TCR)-induced gene expression. Here, we show that TCR-triggered activation of ADP-dependent glucokinase (ADPGK), an alternative, glycolytic enzyme typical for Archaea, mediates generation of the oxidative signal. We also show that ADPGK is localized in the endoplasmic reticulum and suggest that its active site protrudes toward the cytosol. The ADPGK-driven...
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Tracheotomy in the age of the COVID-19 pandemic: up-to-date review
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