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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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New potent steroid sulphatase inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives
PublicationIn the present work, we report a new class of potent steroid sulphatase (STS) inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives. Within the set of new STS inhibitors, 6-(1-(1,2,3-trifluorophenyl)-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate 3L demonstrated the highest activity in the enzymatic assay inhibiting the STS activity to 7.98% at 0.5 µM concentration. Furthermore, to verify...
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Properties and Formation of Mineralized Veins in an Organic-Rich Shale Formation
PublicationAn earlier paper defined mineral and organic matter constituents in weak interfaces in shale formations (Ptaszynska, et. al., 2016). The formation studied in the earlier work and here is the Jurassic, early-Cretaceous Vaca Muerta formation in the Neuquen basin in Argentina. In this earlier work, mineralized "veins" were noted to be prevalent and complicated, sometimes being shear weak interfaces while in other cases they were not....
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Synthesis and biological evaluation of thiophosphate tricyclic coumarin derivatives as steroid sulfatase inhibitors
PublicationSteroid sulfatase (STS) enzyme inhibition is an important approach to the management of hormone-dependent breast cancer. In this paper, we report convenient methods for the synthesis and biological evaluation of thiophosphate tricyclic coumarin analogs exhibiting STS activity. The described methods are based on the straightforward preparation of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-2-one, 3-hydroxy- 7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one,...
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Residence time distribution in rapid multiphase reactors
PublicationResidence time distribution (RTD) provides information about average hydraulic residence time and the distribution of material in the reactor. A method for determining RTD for reactors with very short hydraulic residence times is deconvolution based on extraction of real RTD by the analysis of a non-ideal input signal. The mean residence time and dispersion were determined for the spinning fluids reactor (SFR). For the first time...
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Development and experimental validation of a novel double-stage yield steel slit damper-buckling restrained brace
PublicationThis research is focused on the development and experimental validation of a novel double-stage yield steel slit damper-buckling restrained brace (SSD-DYB) system designed for seismic resistance of steel structures. The SSD-DYB integrates the energy dissipation capability of a steel slit damper (SSD) in its initial segment, enhancing performance in the case of lower seismic intensities levels while employing a larger segment for...
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A Novel Method for Intelligibility Assessment of Nonlinearly Processed Speech in Spaces Characterized by Long Reverberation Times
PublicationObjective assessment of speech intelligibility is a complex task that requires taking into account a number of factors such as different perception of each speech sub-bands by the human hearing sense or different physical properties of each frequency band of a speech signal. Currently, the state-of-the-art method used for assessing the quality of speech transmission is the speech transmission index (STI). It is a standardized way...
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Novel steroid sulfatase inhibitors based on N ‐thiophosphorylated 3‐(4‐aminophenyl)‐coumarin‐7‐O‐sulfamates
PublicationIn 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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From DNA damage to G2 arrest: the many roles of topoisomerase II. W: Prog-ress in Cell Cycle Research. Ed. Meijer L., Jezequel A., Roberge M. London: Plenum Publ. Comp. Ltd**2003 vol. 5 chapt. 30 s. 295-300 Od uszkodzeń DNA do bloku w G2: wiele ról dla topoizomerazy II.
PublicationInhibitory DNA topoizomerazy II sa jednymi z najbardziej szeroko stosowanymi lekami przeciwnowotworowymi. Związki te indukuja pekniecia nici DNA i bloku progresji cyklu komorkowego w fazie G2. Jednak topoizomeraza II jest nie tylko celem molekularnym dla lekow przeciwnowtworowych ale enzym ten pelniwazna role w odpowiedzi komorkowej na dzialanie wielu lekow uszkadzajacych DNA. Topoizomeraza tworzy kompleksy molekularne z bialkami...
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Performance Evaluation of Asphalt Binder Modified with Shear Thickening Fluid
PublicationThis paper aims at using a dilatant or shear thickening fluid (STF) [a non-Newtonian fluid consisting of particles of nano-silica suspended in a liquid medium, i.e., ethylene glycol (EG), which acts as a carrier fluid; proportion 40:60] as additive or modifier of bitumen in order to enhance its viscoelastic properties. A commonly-used performance grading (PG) system, storage stability test, and different conventional and rheological...
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Approach Manoeuvre During Emergency Ship-to-Ship Transfer Operation with Oil Spill
PublicationOne of the major activities during Ship to Ship (STS) transfer operation at sea is to safe approach the Ship to be Lightered (SBL) which moves on a constant heading with slow speed or drifting. In the paper described the manoeuvring problem for approaching during emergency STS transfer operation with oil spill. The approach manoeuvre is considered as a sequence of navigation manoeuvres in specific navigational environment with...
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Synthesis and biological evaluation of N-acylated tyramine sulfamates containing C-F bonds as steroid sulfatase inhibitors
PublicationSteroid sulfatase (STS) is responsible for the hydrolysis of biologically inactive sulfated steroids into their active un-sulfated forms and promotes the growth of various hormone-dependent cancers (e.g., breast cancer). Therefore, the STS enzyme is a promising therapeutic target for the treatment of steroid-sensitive cancers. Herein, we report the synthesis and biological evaluation of sulfamate analogs as potential STS inhibitors...
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Space-Time Conservation Method applied to numerical solution of water hammer equations
PublicationArtykuł poświęcony jest metodzie czasoprzestrzennych objętości skończonych (STC) zastosowanej do przypadku uderzenia hydraulicznego w stalowym przewodzie pracującym pod ciśnieniem. Metoda STC ze względu na swoje własności numeryczne - m.in. wysoką dokładność - może być interesującą alternatywą dla tradycyjnych metod numerycznych, szczególnie w przypadku, gdy efekty numeryczne mają bardzo silny wpływ na rozwiązanie, tym samym utrudniając...
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Synthesis and biological evaluation of fluorinated 3-phenylcoumarin-7-O-sulfamate derivatives as steroid sulfatase inhibitors
PublicationIn the present work, we report the initial results of our study on a series of 3-phenylcoumarin sulfamate-based compounds containing C-F bonds as a novel inhibitors of steroid sulfatase (STS). The new compounds are potent STS inhibitors, possessing more than 10 times higher inhibitory potency than coumarin-7-O-sulfamate. In the course of our investigation, compounds 2b and 2c demonstrated the highest inhibitory effect in the enzymatic...
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Nadzorowanie drgań układu nośnego robota przemysłowego IRB-6 za pomocą ste-rowania modalnego przy energetycznym wskaźniku jakości. W: Zagadnienia ana- lizy modalnej konstrukcji mechanicznych. Praca zbiorowa pod red. T. Uhla. Kraraków: Kated. Robotyki i Dynam. Masz. AGH**2003 s. 115-122, 2 rys. 1 tab. bibliogr. 4 poz.
PublicationW pracy rozważa się drgania modelowanego dyskretnie niestacjonarnego układunośnego manipulatora IRB6 metodą sztywnych elementów skończonych. Do nadzo-rowania drgań wykorzystano algorytm sterowania optymalnego przy energetycz-nym wskaźniku jakości w dziedzinie współrzędnych modalnych. Uwzględnia on zmianę w czasie, względem trajektorii ruchu zadanego, energii potencjalnej, kinetycznej oraz energii sygnału sterującego.
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Phosphate and Thiophosphate Biphenyl Analogs as Steroid Sulfatase Inhibitors
PublicationIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate and thiophosphate biphenyl derivatives exhibiting steroid sulfatase (STS) activity. The described synthesis is based on straightforward preparation of biphenyl-4-ol and 40-hydroxybiphenyl- 4-carboxylic acid ethyl ester modified with various phosphate or thiophosphate moieties. The inhibitory effects of these compounds were...
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Synthesis and steroid sulfatase inhibitory activities of N-alkanoyl tyramine phosphates and thiophosphates
PublicationA series of phosphate and thiophosphate analogs based on the frameworks of N-alkanoyl tyramines have been synthesized and biologically evaluated. Their binding modes have been modeled using docking techniques. The inhibitory effects of the synthesized compounds were tested on STS isolated from the human placenta as well as the MCF-7, MDA-MB-231 and SkBr3 cancer cell lines. Most of the new STS inhibitors possessed potent activity...
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Synthesis of bicoumarin thiophosphate derivatives as steroid sulfatase inhibitors
PublicationBased on the frameworks of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy- 7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c] chromen-6-one, a series of bicoumarin thiophosphate analogs have been synthesized and biologically evaluated. Additionally, their binding modes have been modeled using docking techniques. The inhibitory properties of the synthesized compounds...
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Synthesis and steroid sulfatase inhibitory activities of N-phosphorylated 3-(4-aminophenyl)-coumarin-7-O-sulfamates
PublicationIn the present work, we report convenient methods for the synthesis and biological evaluation of N-phosphorylated derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as potential steroid sulfatase (STS) inhibitors. Their binding modes were modeled using docking techniques. The inhibitory effects of the synthesized compounds were tested on STS isolated from human placenta. All of the newly synthesised coumarin derivatives were...
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The Influence of Iron Doping on Performance of SrTi1-XFexO3-δ Perovskite Oxygen Electrode for SOFC
PublicationSolid Oxide Fuel Cells (SOFC) are based on electrolytes and mixed ionic and electronic conductivity (MIEC) materials. The need to reduce costs causes an increase in interest of new compounds suitable for operating temperatures between 600 °C and 800 °C. The SrTi1-xFexO3 (STF) perovskite material is a perspective material that could be used for the oxygen electrodes. In this work STF materials with different content of iron (x =...
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How it audit can help your communications branch company increase effectiveness of using it technologies and contributes to implementation of business
PublicationText based on the example of Cable Television Ltd. Co. in Koszalin.
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Steroid Sulfatase Inhibitors Based on Phosphate and Thiophosphate Flavone Analogs
PublicationA series of phosphate and thiophosphate flavone derivatives were synthesized and biologically evaluated in vitro for inhibition of steroid sulfatase (STS) activity. The described synthesis includes the straightforward preparation of 7-hydroxy-2-phenyl-4H-chromen-4-one 3a, 2-(4-fluorophenyl)-7-hydroxy-4H-chromen-4-one 3b, 7-hydroxy-2-(4-(trifluoromethyl)phenyl)-4H-chromen-4-one 3c, 7-hydroxy-2-(p-tolyl)-4H-chromen-4-one 3d modified...
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Using evidence based arguments to support trust
PublicationWprowadzono podstawowe koncepcje metodyki TRUST-IT: argumentu i dowodu, modelu argumentacji, szablonu argumentacji, oceny argumentu oraz kontekstu aplikacyjnego. Przedstawiono zakres funkcjonalności, modele udostepniania oraz politykę bezpieczeństwa informacji związane z usługami NOR-STA wspomagającymi zastosowania metodyki TRUST-IT. Przedstawiono również dotychczasowe doświadczenia związane z wdrażaniam uzług NOR-STA w różnych...
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Synthesis and biological evaluation of fluorinated N-benzoyl and N-phenylacetoyl derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as steroid sulfatase inhibitors
PublicationIn the present work, we report convenient methods for the synthesis of 3-(4-aminophenyl)-coumarin-7-O-sulfamate derivatives N-acylated with fluorinated analogues of benzoic or phenylacetic acid as steroid sulfatase (STS) inhibitors. The design of these potential STS inhibitors was supported by molecular modeling techniques. Additionally, computational docking methods were used to determine the binding modes of the synthesized inhibitors...
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A Convenient Way to Methylated 2-Imidazolines. Syntheses of Fluorene and Triazine Cyclic Diamidines
PublicationOne N-methyl- and 4-substituted 2-imidazolines are described. Fluorene bisimidazolines were obtained in good yield (64-92%), starting from 2,7-dicyanofluorene and ammonium sulfide. In a two-step procedure the crude bisthioamide was reacted with excess diaminoalkane-ethanol (1:1 mixt.) in an oil bath. This new procedure is superior over std. methods. For the sake of comparison, a new triazine bisimidazoline (I) was prepd. by...
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Mineral and Organic Matter Constituents in Weak Interfaces in Shales
PublicationThis paper identifies formation interfaces that would appear to be "weak interfaces", in the Jurassic, Early- Cretaceous Vaca Muerta formation, in the Neuquén Basin, Argentina. Significant distribution of the weak interfaces was observed including contacts between volcanic ash layers of varying thicknesses, calcite-filled veins, and contacts between lithology changes, such as between argillaceous mudstone and mottled carbonates....
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Cloning of the thermostable alpha-amylase gene from Pyrococcus woesei in Escherichia coli.
PublicationGen kodujący alfa-amylazę z Pyrococcus woesei klonowano do plazmidów pET21d(+)lub pYTB2, którymi transformowano komórki Escherichia coli. Otrzymana rekombinantowa alfa amylaza wykazuje maksymalną aktywność przy pH 5.6 w temperaturze 95 stC i przejawia około 24 % początkowej aktywności nawet po 2 godz. inkubacji w 120 stC. Duża termostabilność otrzymanego preparatu świadczy o jego przydatności do enzymatycznego upłynniania skrobi.
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Dirichlet-to-Neumann and Neumann-to-Dirichlet embedding methods for bound states of the Schrodinger equation.
PublicationPrzeformułowano metodę Inglesfielda, stosowaną do obliczania własności stanów związanych równania Schrodingera, stosując formalizm operatorów całkowych Dirichleta-do-Neumanna(DtN) i Neumanna-do-Dirichleta (NtD). Wykorzystano zasady wariacyjne dla energii dopuszczające użycie funkcji próbnych nieciągłych wraz z pochodnymi. Podano metodę konstrukcji jąder operatorów DtN i NtD za pomocą rozwiązań zagadnienia własnego typu Steklova....
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Cieplice dla Sopotu
PublicationArtykuł prezentuje treść informacji o projekcie budynku kąpieliska, wybudowanego przed stu laty w Sopocie.
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Phosphate tricyclic coumarin analogs as steroid sulfatase inhibitors: synthesis and biological activity.
PublicationIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate tricyclic coumarin derivatives as potential steroid sulfatase inhibitors. The described synthesis includes the straightforward preparation of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c]chromen-6-one modified...
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The effect of convective heating and microwave heating on antioxidant enzymes in pooled mature human milk
PublicationThe effects of convective and microwave heating at constant temperature (62.5, 66 and 70 °C) on the activity of antioxidant enzymes (superoxide dismutase, SOD; catalase, CAT; glutathione peroxidase, GPx) in pooled mature human milk were compared. Activities of the enzymes were determined using spectrophotometric kits. Activity of GPx decreased significantly in the first stage of heating when milk samples were warmed to pasteurisation...
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Micro-Raman spectroscopy in the studies of multiphase separated polyurethanes. [online] W: [Proc.] UTECH Europe 2003 . The International Polyurethane Industry Conference and Exhibition. 25/26/27 March 2003, The Hague, Netherlands. London: Crain Communications Ltd. Dostępny w World Wide Web: http://UTECH-2003.com + wydruk.**2003 [s. 123-130 bibliogr. 41 poz.]Mikro-Ramanowska spektroskopia w badaniach poliuretanów wykazujących separację wielofazową.
PublicationPrzedmiotem badań były trzy próbki poliuretanowe o zawartości 30% segmentówsztywnych otrzymanych z politlenku propylenu, diizocyjanianu difenylometanui butanodiolu. Próbki te wykazują morfologię wielofazową, w której można wy-różnić globule i sferolity rozproszone w matrycy polimerowej.Za pomocą spek-troskopii mikro-Ramana przeprowadzono mikroanalizę chemiczną wszystkich ele-mentów morfologicznych. Stwierdzono odmienny skład...
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Functionalization of electrode surfaces with monolayers of azocompounds and gold clusters.
PublicationWłaściwości monowarstw z azokoron na powierzchni złota były badane przy pomocy woltametrii i STM. Powierzchnia przypadająca na cząsteczkę została wyznaczona przy pomocy woltametrii i wynosi 0,65 nm kwadratowych. Wartość ta jest zgodna z wyznaczoną w oparciu o monowarstwę utworzoną na granicy powietrze-woda techniką Langmir-Blodgett. Tworzenie się klasterów złota i innych struktur obserwowano przy pomocy STM w przypadku gdy złota...
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Challenges in providing support for management of evidence-based arguments
PublicationThe paper considers selected challenges related to the application of evidence based arguments and maps them on the tool support level. In particular, we consider: communication and teamwork, handling large arguments, evidence management and integration, argument assessment and communication, change control and reporting, evidence reuse, user data security and argument portfolio management. Then we explain how these challenges...
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Evaluation of the Influence of Farming Practices and Land Use on Groundwater Resources in a Coastal Multi-Aquifer System in Puck Region (Northern Poland)
PublicationThis study focuses on the modeling of groundwater flow and nitrate transport in a multi-aquifer hydrosystem in northern Poland, adjacent to Puck Bay (Baltic sea). The main goal was to investigate how changes in land use and farming practices may affect groundwater recharge and submarine groundwater discharge (SGD) to the sea and the associated N-NO3 fluxes. An integrated modelling approach has been developed, which couples the...
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Wnioskowanie z danych zapisanych w zewnętrznych źródłach w systemie zarządzania wiedzą
PublicationRozdział prezentuje proces wnioskowania z danych przechowywanych w zewnętrznych źródłach. W procesie tym wykorzystywane są dwie nowe metody: metoda semantycznego wzbogacania źródeł - SED (Semantic Enrichment of Data) oraz wykorzystująca ją metoda wnioskowania z danych zewnętrznych - RED (Reasoning over External Data). Obie te metody zostały w niniejszym rozdziale przedstawione. Metoda SED służy do opisania zewnętrznych źródeł danych...
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Cofka po deszczu
PublicationWody opadowe. Obszary zurbanizowane. Konsekwencje kanalizowania. Unikanie zagrożeń. Potrzeba retencji. Znaczenie czynnika lokalnego. Brak zrozumienia znaczenia problemu i wynikające stąd zagrożenia.
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Efektywne metody lokalizowania terminala ruchomego w systemie WCDMA/FDD
PublicationZaproponowano, poddano analizie i zbadano na drodze symulacyjnej dwie nowe, efektywne metody lokalizowania terminala ruchomego w systemie WCDMA/FDD (Wideband Code Division Multiple Access/Frequency Division Duplex). Metody te umożliwiają estymację położenia terminala ruchomego bez konieczności znajomości różnicy czasów w synchronizacji stacji bazowych RTD (Relative Time Difference). Eliminacja różnicy czasów RTD znacząco upraszcza...
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ECG-based prediction of ventricular fibrillation by means of the PCA
PublicationA Sudden Cardiac Death (SCD) is a death resulting from cardiac failure with no significant symptoms earlier than one hour before occurrence. It is the cause of for approximately 400000 deaths per year in United States and millions of deaths worldwide. The proposed system, including two-stage algorithm and wearable diagnostic device allows for SCD risk estimation and continuous monitoring of high risk patients. A single channel...
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Materiały do budowy sieci wodociągowej Rozdział w publikacji monograficznej
PublicationCechy charakterystyczne materiałów stosowanych do budowy sieci wodociągowej (ciśnieniowej). Konsekwencje wymagań i cech materiałowych wyrobów. Różnice w zachowaniach i wynikające stąd konsekwencje
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Główne grzechy polskiego public relations
PublicationArtykuł analizuje problemy działalności PR w Polsce, najczęściej popełniane błędy - nieprofesjonalizm działań i wynikające stąd trudności w działaniu przedsiębiorstw, mediów i instytucji kształcących.
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Structure and Randomness in Planning and Reinforcement Learning
PublicationPlanning in large state spaces inevitably needs to balance the depth and breadth of the search. It has a crucial impact on the performance of a planner and most manage this interplay implicitly. We present a novel method \textit{Shoot Tree Search (STS)}, which makes it possible to control this trade-off more explicitly. Our algorithm can be understood as an interpolation between two celebrated search mechanisms: MCTS and random...
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A pin-on-disc study of airborne wear particle emissions from studded tyre on concrete road contacts
PublicationStudded tyres wear surfaces of winter roads, generating inhalable airborne particles. In this study, four concrete road materials and two stud geometries were investigated in terms of wear, road material hardness and airborne particle concentration. The sliding contact between studded tyres and road materials was studied using a pin-on-disc machine in a clean chamber. The results show that the normal load and the stud size have...
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Agent-based social network as a simulation of a market behaviour
PublicationRecent years and the outbreak of world's economic crisis in 2008 proved the crucial importance of reliable analysis of market dynamics. However, werarely apply models of proper detail level (the global prosperity forecast of 2007 can be seen as a grim proof). The behaviour of individuals and companies is far from being ideal and rational. Many claims that the economic paradigm of rational expectations (coming from J. Muth and R....
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Odpowiedź na Kilka uwag do artykułu nt. Mostu Uniwersyteckiego w Bydgoszczy
PublicationW materiale zawarto odpowiedź do artykułu "Kilka uwag do artykułu nt. Mostu Uniwersyteckiego w Bydgoszczy" opublikowanego w ne 1/2023 czasopisma "Mosty" na str. 8.
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Zarządzanie zgodnością ze standardami akredytacyjnymi w chmurze obliczeniowej
PublicationRosnące znaczenie akredytacji usług medycznych, w szczególności świadczonych przez szpitale, wymaga rozwoju wsparcia informatycznego. Artykuł przedstawia usługi informatyczne NOR-STA wspomagające i integrujące procesy osiągania, oceny i utrzymania zgodności z normami i standardami. Omówiono zakres usług, sposób ich dostarczania, a także wskazano na główne korzyści takie jak przejrzysty przegląd standardów, uporządkowanie dokumentów,...
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Using Evidence-based Arguments to Support Dependability Assurance-Experiences and Challenges
PublicationThe article introduces to the problem of evidence-based arguments and their applications. Then, based on the experiences collected during commercial deployment of a concrete solution to this problem (system NOR-STA) we overview selected challenges and the ways of addressing them
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Kontrasty, metamorfozy, styl - czyli rozważania o dynamice przemian architektury XX wieku.
PublicationBadanie ciągłych przemian w sposobie kreowania architektury zarówno w teorii jak i praktyce budowania na przestrzeni ostatnich stu lat doprowadziło do wyodrębnienia pewnych matematycznie ujętych zależności.
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Using Evidence-based Arguments to Support Dependability Assurance - Experiences and Challenges
PublicationThe presentation introduces to the problem of evidence-based arguments and their applications. Then, based on the experiences collected during development and commercial deployment of a concrete solution to this problem (system NOR-STA) we overview selected challenges and the ways of addressing them.
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Luminance Distribution Measurements in CAVE-Type Virtual Reality Systems
PublicationIn this article, the immerse 3D visualization lab just opened at the Gdańsk University of Technology is presented. The effect of user “immersion,” it such virtual reality systems, is largely dependent on the optical properties of projected images. Luminance distribution of screens was measured and the luminance uniformity was determined and discussed.