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Search results for: ANTITUMOR DRUG RESISTANCE
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Interaction of antitumor triazoloacridone C-1305 and its analogs with telomeric DNA
PublicationBadaliśmy oddziaływanie pochodnej triazoloakrydonu C-1305 i jego bliskich analogów strukturalnych z oligonukleotydami zawierającycmi sekwencje telomerowe TTAGGG oraz oligonukleotydami sfałdowanymi w strukturę G-kwadrupleksu. Wykazaliśmy, że spośród badanych związków pochodna C-1305 wykazała największą specyficzność w stosunku do telomerowego DNA. Związek ten stabilizował także strukturę G-kwadrupleksu, podczas gdy jego analogi...
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Calculations of the resistance values of 20 thermistors at 100°C
Open Research DataThe presented data set is part of the research aimed at determining the actual characteristics of each thermistor in a package of twenty NTC10k type sensors.
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Prediction of Overall In Vitro Microsomal Stability of Drug Candidates Based on Molecular Modeling and Support Vector Machines. Case Study of Novel Arylpiperazines Derivatives
PublicationOther than efficacy of interaction with the molecular target, metabolic stability is the primary factor responsible for the failure or success of a compound in the drug development pipeline. The ideal drug candidate should be stable enough to reach its therapeutic site of action. Despite many recent excellent achievements in the field of computational methods supporting drug metabolism studies, a well-recognized procedure to model...
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Impact analysis of surface roughness of the plate-plate measuring system on resistance torque in interaction with MR fluid
PublicationMagnetorheological (MR) fluids are complex suspensions of magnetic particles in a non-magnetic carrier fluid. They exhibit ‘smart’ properties that enable them to change their rheological parameters in response to a change in the external magnetic field applied. This behavior is used in some engineering solutions, e.g. MR clutches or brakes. For such systems to work correctly, the resistance torque achieved by contact with the...
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Crack Resistance of Asphalt Concrete Subjected to Environmental Factors
PublicationThe paper presents an analysis of the influence of environmental factors on the cracking susceptibility of asphalt concrete resulting in a change in the durability of asphalt pavement. In order to assess the phenomenon, laboratory tests were carried out taking into account the destructive effects of moisture, freeze-thaw cycle and long-term ageing. The influence of both factors occurring simultaneously was also verified. Due to...
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Calculations of the resistance values of 20 thermistors at 0°C
Open Research DataThe presented data set is part of the research aimed at determining the actual characteristics of each thermistor in a package of twenty NTC10k type sensors.
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TIME-DOMAIN NUMERICAL EVALUATION OF SHIP RESISTANCE AND MOTION IN REGULAR WAVES BY USING THE CFD URANS METHOD
PublicationTaking into account the International Maritime Organisation’s (IMO) strategy to radically reduce the GHG emitted by the shipping industry towards zero emission operation, today's assessment of ship behaviour in waves, its seakeeping characteristics and resistance and their interrelation with fuel consumption and emissions are one of the most attended research subject. There are three methods to conduct this analysis, which are...
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Noise and Rolling Resistance Properties of Various Types of Winter Tyres Compared to Normal Car Tyres
PublicationTo cope with winter weather conditions, potentially including snow and ice, it is common to use winter tyres, or ”all-seasons” tyres assumed to be safe both in summer and winter. In some northern countries, winter tyres are mandatory. Traditionally, it has been assumed that winter tyres are noisier than normal tyres (here called summer tyres) and winter tyres equipped with studs are assumed to be very noisy.This paper presents...
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Development of a Peptide Derived from Platelet-Derived Growth Factor (PDGF-BB) into a Potential Drug Candidate for the Treatment of Wounds
PublicationObjective: This study evaluated the use of novel peptides derived from platelet-derived growth factor (PDGF-BB) as potential wound healing stimulants. One of the compounds (named PDGF2) was subjected for further research after cytotoxicity and proliferation assays on human skin cells. Further investigation included evaluation of: migration and chemotaxis of skin cells, immunological and allergic safety, the transcriptional analyses...
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Wear Resistance Enhancement of Al6061 Alloy Surface Layer by Laser Dispersed Carbide Powders
PublicationIn this paper, results of the experimental study on improving wear resistance in sliding friction of Al-based alloy are presented. The technique used involves the formation of a metal matrix composite (MMC) in the alloy surface layer by laser dispersion of carbide powders such as WC, TiC and SiC. For WC and TiC MMC surface coatings fabricated under conditions typical for most of the technologically relevant solid-state lasers (wavelength...
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Study of the Resistance to Influence of Aggressive Liquids on Concrete with Lightweight Aggregate
PublicationThe corrosion of the structure of concrete caused by the aggressive external environment is one of the main problems that can reduce the durability of buildings. The paper analyzes the influence of the type of component on selected properties of lightweight concrete (LWC) exposed to aggressive liquids. When lightweight concrete containing porous aggregates is used, the influence of an aggressive environment may be of particular...
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Experimental Study of the Resistance to Influence of Aggressive Liquids on Lightweight Concrete
PublicationIn light of the scientific research, the corrosion of concrete structures is one of the main problems that may reduce their durability due to the negative impact of the natural environment. The paper analyzes the influence of the type of component on the selected properties of lightweight concrete subjected to the influence of aggressive liquids. Four concrete mixes were prepared with a granular aggregate made of foamed glass (GEGA)...
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Antitumor DNA-Damaging C-1748 is a New Inhibitor of Autophagy that Triggers Apoptosis in Human Pancreatic Cancer Cell Lines
PublicationDespite the enormous progress that has been made over the past decades in diagnosis, treatment and prevention of many types of tumors, survival rates in pancreatic cancer still remain poor. Pancreatic cancer is one of the most malignant and chemoresistant tumors and the profound mechanism supporting these phenomena is the constitutively activated prosurvival autophagy. The antitumor 1-nitroacridine derivative C-1748 belongs to...
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Rolling resistance measurements of studded tires
PublicationW pracy przedstawiono wyniki pomiaru oporu toczenia opon kolcowanych i po usunięciu kolców na nawierzchni poroelastycznej. Badania przeprowadzono na stanowisku bębnowym Katedry Pojazdów i Maszyn Roboczych Politechniki Gdańskiej. Opony kolcowane mają o około 5% wyższy współczynnik oporu toczenia w porównaniu z oponami nie kolcowanymi.
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Voriconazole and multidrug resistance in Candida albicans
PublicationPorównano aktywność grzybostatyczną in vitro worikonazolu, flukonazolu, ketokonazolu i klotrimazolu wobec opornych na flukonazol szczepów klinicznych Candida albicans oraz rekombinowanych szczepów Saccharomyces cerevisiae eksprymujących jeden z genów kodujących białka oporności wielolekowej (MDR) C. albicans: Cdr1p. Cdr2p lub CaMdr1p. Stwierdzono, że nadekspresja genów MDR czyni komórki drożdżaków mniej wrażliwymi na działanie...
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Difficulties with evaluating resistance of materials to cavitation.
PublicationW pracy dokonano analizy wyników Międzynarodowego Testu Erozji Kawitacyjnej (ICET), któremu koordynował Instytut Maszyn Przepływowych Polskiej Akademii Nauk (IMP PAN) w Gdańsku. Kluczowe parametry wpływające na zmianę przebiegu krzywych erozji uzyskanych na stanowiskach badawczych zostały wskazane. Wykazano konieczność przeprowadzenia badań w zakresie oceny wpływu efektu skali. Zaprezentowano wyniki uzyskane na stanowiskach magnetostrykcyjnych...
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Estimation of cavitation erosion resistance of materials
PublicationW pracy przedstawiono ocenę odporności kawitacyjnej 17 materiałów. Do opisu odporności kawitacyjnej zaproponowano nowy wskaźnik liczbowy uwzględniający długość okresu inkubacji, maksymalną prędkość niszczenia oraz czas po którym wystąpi maksymalna prędkość niszczenia materiału. Zaproponowany wskaźnik porównano ze wskaźnikiem δcav, który reprezentuje całą krzywą erozji kawitacyjnej materiału.
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Type of surface and tire rolling resistance
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Full-scale CFD simulations for the determination of ship resistance as a rational, alternative method to towing tank experiments
PublicationResults of ship resistance predictions obtained from towing tank experiments are affected by the method used to extrapolate from a model scale to a ship scale. Selection of method to determine a form factor is subjective and the extrapolation method is accurate for typical hull forms. For innovative hull forms the proper method for calculating the form factor is questionable. Moreover, the influence of the extrapolation method...
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Optimization of biocorrosion resistance and mechanical properties of PM Ti–XAl–2Fe–3Cu alloys by response surface methodology
PublicationIn the current study, the biocorrosion resistance and mechanical properties of the Ti–XAl–2Fe–3Cu (wt%) (X = 6, 4, 2 wt%) alloy produced by powder compact extrusion of blended elemental powders were optimized by using the response surface methodology in order to gain the best combination of processing parameters. To run the optimization process, central composite design with three equal levels of oxygen, hydrogen and aluminum was...
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Dynamic mechanical properties and flexing fatigue resistance of tire sidewall rubber as function of waste tire rubber reclaiming degree
PublicationA stepwise downsizing method of gel particles in reclaimed rubber to a micro-nano scale and its excellent dynamic performance in tire sidewall were introduced by this work. The results showed that the size of gel particles decreased from several micrometers to micro-nanometers with the increase of reclaiming degree, accompanied by reduced molecular weight and widened molecular weight distribution of sol fraction. The addition of...
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Effect of microstructure on mechanical properties and corrosion resistance of 2205 duplex stainless steel
PublicationThis paper presents results of the research on impact of microstructure of austenitic-ferritic steel of duplex type on its mechanical properties and susceptibility to stress corrosion cracking. As showed, improper processing technologies more and more often used in shipbuilding industry for plates and other half-finished products made of duplex steel may cause significant lowering their properties, which frequently makes their...
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Experimental verification of a new method of loop resistance testing in low voltage systems with residual current devices
PublicationA periodical verification of the effectiveness of protection against electric shock shall be performed in low voltage systems. The scope of this verification includes loop impedance/resistance testing. If a residual current device is installed in a tested circuit, this testing is problematic. A residual current device trips out during the test, because of the high value of measurement current. This precludes the execution of the...
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The abrasive wear resistance of coatings manufactured on high-strength low-alloy (HSLA) offshore steel in wet welding conditions
PublicationSome marine and offshore structure elements exploited in the water cannot be brought to the surface of the water as this will generate high costs, and for this reason, they require in-situ repairs. One of the repair techniques used in underwater pad welding conditions is a wet welding method. This paper presents an investigation of the abrasive wear resistance of coatings made in wet welding conditions with the use of two grades...
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Controlled Drug Release by the Pore Structure in Polydimethylsiloxane Transdermal Patches
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Filling of Carbon Nanotubes: Containers for Magnetic Probes and Drug Delivery
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Chemometrics of bi-heterocyclic kind of drug specimens in the THz domain
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Chitosan-Based Nanoparticles as Effective Drug Delivery Systems—A review
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Recent Advances in Polymer-Based Vaginal Drug Delivery Systems
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Mesoporous silica nanoflakes – Biocompatibility, cellular uptake and drug transport
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Rational design, synthesis and biological evaluation of thiadiazinoacridines: a new class of antitumor agents.
PublicationZsyntetyzowano serię związków o potencjalnej zdolności do wiązania się z DNA z grupy tiadiazinoakrydyn poprzez cyklizację odpowiednich pochodnych 9-imino-4-nitro-9,10-dihydroakrydyny. Zbadano ich zdolność do wiązania się z DNA oraz cytotoksyczność względem kilku linii komórek nowotworwych. Badania aktywności przeciwnowotworowej wobec białaczki P388 wskazały na zgodność tych wyników z wynikami cytotoksyczności in vitro. Wykazano,...
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Structural determinants of imidazoacridinones facilitating antitumor activity are crucial for substrate recognition by ABCG2
PublicationW pracy zidentyfikowaliśmy elementy struktury chemicznej dla 23 pochodnych imidazoakrydonu odpowiedzialne za ich rozpoznawanie przez transporter typu ABC, białko ABCG2. za transport tych związków przez pompę ABCG2 odpowiedzialne jest grupa hydroksylowa w pozycjach R1, R2 i R3 chromoforu. Stwierdziliśmy także, że zwiększanie ilości grup metylenowych łańcucha bocznego imidazoakrydonów powodowało zmniejszenie aktywnego transportu...
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Natural and synthetic acridines/acridones as antitumor agents: their biological activities and methods of synthesis.
PublicationPraca stanowi przegląd opisanych w literaturze chemicznej modyfikacji struktur naturalnych i syntetycznych pochodnych akrydyny i akrydonu. Artykuł obejmuje swym zakresem metody syntezy, a także wpływ budowy cząsteczek tych związków na ich aktywność przeciwnowotworową oraz mechanizm działania.
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Interleukin 12 and indomethacin exert a synergistic, angiogenesis-dependent antitumor activity in mice
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Corrosion Resistance and Surface Bioactivity of Ti6Al4V Alloy after Finish Turning under Ecological Cutting Conditions
PublicationThe influence of cooling conditions and surface topography after finish turning of Ti6Al4V titanium alloy on corrosion resistance and surface bioactivity was analyzed. The samples were machined under dry and minimum quantity lubrication (MQL) conditions to obtain different surface roughness. The surface topographies of the processed samples were assessed and measured using an optical profilometer. The produced samples were subjected...
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Bortezomib induces methylation changes in neuroblastoma cells that appear to play a significant role in resistance development to this compound
PublicationThe anticancer activity of bortezomib (BTZ) has been increasingly studied in a number of indications and promising results for the use of this treatment have been shown in neuroblastoma. As BTZ treatment is usually administered in cycles, the development of resistance and side effects in patients undergoing therapy with BTZ remains a major challenge for the clinical usage of this compound. Common resistance development also means...
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Calculations of the resistance values of 20 thermistors at 50°C
Open Research DataThe presented data set is part of the research aimed at determining the actual characteristics of each thermistor in a package of twenty NTC10k type sensors.
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Successive cytotoxicity control by evolutionary surface decorated electronic push-pull green ZnCr-LDH nanostructures: Drug delivery enlargement for targeted breast cancer chemotherapy
PublicationThe reason for the increasing bioavailability and biocompatibility of the porous nanomaterials in the presence of different (bio)molecules is still unknown. The role of difference functional groups and their interactions with the potential bioavailability and biocompatibility is of great importance. To investigate the potential contribution of the electronic effects (especially on the surface of the porous nanomaterials) on their...
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Relieving the Measuring System of the Trailer for Tyre/Road Rolling Resistance Measurements from the Inertia Force
PublicationIn the article the principle of measuring of tyre/road rolling resistance tyres in road conditions applied in a special measuring trailer is presented. This trailer was built in Faculty of Mechanical Engineering at Gdansk University of Technology. The construction of two special devices used in this trailer was discussed. These devices eliminate the influence of some chosen confounding measurements factors such as: the inertia...
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Evaluation of the resistance of steel–concrete adhesive connection in reinforced concrete beams using guided wave propagation
PublicationThe development of the nondestructive diagnostic methods is of significant importance in the last decades. A special attention is paid to diagnostics of reinforced concrete structures, which are very popular in the civil engineering field. A possible use of the guided waves in the estimation of the resistance of steel–concrete adhesive connection is studied in the following paper. The relationships relating adhesive connection...
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Enhancing the Seismic Resistance of Columns by GFRP Confinement Using Flexible Adhesive-Experimental Study
PublicationIn this paper, the results of two experiments, focused on testing the effectiveness of a method of enhancing the seismic (dynamic) resistance of masonry columns with the use of flexible polymer adhesive, are shown. The first experiment was devoted to investigate the damping properties of a polymer working between two stiff layers, whereas the aim of the second one was to verify if the identified damping properties of the polymer...
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Functionalization of graphene oxide coatings with phosphorus atoms and their corrosion resistance in sodium chloride environment
PublicationIn this work, we compared corrosion resistance of graphene oxide, and phosphorus functionalized reduced graphene oxide coatings obtained as a result of electrophoretic deposition on the copper substrate. Doping graphene oxide with phosphorus atoms was performed by a hydrothermal method in the presence of different amounts of phosphoric acid. Structural studies confirmed the insertion of phosphorus atoms into the graphene oxide...
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Glutathione conjugation of the antitumor-active 1-nitroacridine derivatives compounds C-857 and C-1748 – the major role of glutathione S-transferase M1-1
Open Research DataObjectives: C-857 and C-1748 are antitumor-active agents, monomers of unsymmetrical bisacridine derivatives. The aim of this study was to analyze their glutathione (GSH) conjugation in vitro in the presence of glutathione S-transferase (GST) M1-1.
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The treatment of wastewater containing pharmaceuticals in microcosm constructed wetlands: the occurrence of integrons (int1–2) and associated resistance genes (sul1–3, qacEΔ1)
PublicationThe aim of this study was to analyze the occurrence of sulfonamide resistance genes (sul1–3) and other genetic elements as antiseptic resistance gene (qacEΔ1) and class 1 and class 2 integrons (int1–2) in the upper layer of substrate and in the effluent of microcosm constructed wetlands (CWs) treating artificial wastewater containing diclofenac and sulfamethoxazole (SMX), which is a sulfonamide antibiotic. The bacteria in the substrate...
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Antibiotic Resistance of Uropathogens Isolated from Patients Hospitalized in District Hospital in Central Poland in 2020
PublicationThe aim of this study was to determine antibiotic resistance patterns and the prevalence of uropathogenes causing urinary tract infections (UTIs) in patients hospitalized in January–June 2020 in central Poland. Antimicrobial susceptibility testing was performed using the disk-diffusion method. Escherichia coli (52.2%), Klebsiella pneumoniae (13.7%), Enterococcus faecalis (9.3%), E. faecium (6.2%), and Proteus mirabilis (4,3%) were...
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Antibiotic resistance in Staphylococcus aureus strains isolated from cows with mastitis in the eastern Poland and analysis of susceptibility of resistant strains to alternative non-antibiotic agents: lysostaphin, nisin and polymyxin B.
PublicationThe aim of the studies was analysis of resistance of Staphylococcus aureus isolates from bovine mastitis in eastern part of Poland to a set of 20 antibiotics and three alternative agents: lysostaphin, nisin and polymyxin B. Eighty-six out of 123 examined isolates were susceptible to all of 20 tested antibiotics (70 %). The highest percentage of resistance was observed in the case of β-lactam antibiotics: amoxicillin (n=22, 17.9...
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A strong preference for the TA/TA dinucleotide step discovered for an acridine-based, potent antitumor dsDNA intercalator, C-1305: NMR-driven structural and sequence-specificity studies
PublicationTriazoloacridinone C-1305, a potent antitumor agent recommended for Phase I clinical trials, exhibits high activity towards a wide range of experimental colon carcinomas, in many cases associated with complete tumor regression. C-1305 is a well-established dsDNA intercalator, yet no information on its mode of binding into DNA is available to date. Herein, we present the NMR-driven and MD-refined reconstruction of the 3D structures...
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