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Diminshed toxicity of C-1748, 4-methyl-9-hydroxyethylamino-1-nitroacridine, compared with its demethyl analog, C-857, corresponds to its resistance to metabolism in HepG2 cells
PublikacjaThe narrow "therapeutic window" of anti-tumour therapy may be the result of drug metabolism leading to the activation or detoxification of antitumour agents. The aim of this work is to examine (i) whether the diminished toxicity of a potent antitumour drug, C-1748, 9-(2'-hydroxyethylamino)-4-methyl-1-nitroacridine, compared with its 4-demethyl analogue, C-857, results from the differences between the metabolic pathways for the...
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Analysis of Corrugated Coaxial Line with the Use of Body of Revolution and Finite Element Method
PublikacjaA combination of the body-of-revolution and finite element methods is utilized to the analysis of coaxial lines with corrugated rod and wall. Both periodic and non-periodic structures can be investigated. As the structure is axially symmetrical the two dimensional scalar-vector finite element method can be used, which allows for the investigation of complex geometries and is computationally efficient. A generalized impedance matrix...
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Progressive failure analysis of laminates in the framework of 6-field nonlinear shell theory
PublikacjaThe paper presents the model of progressive failure analysis of laminates incorporated into the 6-field non-linear shell theory with non-symmetrical strain measures of Cosserat type. Such a theory is specially recommended in the analysis of shells with intersections due to its specific kinematics including the so-called drilling rotation. As a consequence of asymmetry of strain measures, modified laminates failure criteria must...
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Spray pyrolysis of doped-ceria barrier layers for solid oxide fuel cells
PublikacjaGadolinium doped ceria (Ce0.8Gd0.2O2 − x-CGO) layer fabricated by spray pyrolysis is investigated as the diffusion barrier for solid oxide fuel cell. It is deposited between the La0.6Sr0.4FeO3 − δ cathode and the yttria stabilized zirconia electrolyte to mitigate harmful interdiffusion of elements. The parameters of the fabrication process are linked to the measured area specific resistances of the symmetrical cells and the efficiency...
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Phosphoroorganic Metal Complexes in Therapeutics
PublikacjaThe present mini-review highlights recent developments on antitumor activity of metal-based therapeutics which have been a subject of researches for the last few decades. In 1965, Rosenberg found that during an electrolysis on platinum electrodes a complex of Pt is generated which inhibited to a great extent a binary fission in Escherichia coli bacteria. This discovery started a new chapter in medicinal chemistry and the interesting...
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Experimental study of the post tensioned prestressed concrete corbels
PublikacjaThe results of experimental investigation of 6 symmetrical double prestressed corbels of variable shear span to depth ratio and variable location of prestressing bars are presented in the paper. The post ten- sioned corbels were prestressed with Macalloy 1030 bars of 25 mm in diameter. The results of the tests were compared with the cracking and load carrying capacity of corbels reinforced with passive reinforce- ment. As a result...
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Torsional buckling and post-buckling of columns made of aluminium alloy
PublikacjaThe paper concerns torsional buckling and the initial post-buckling of axially compressed thin-walled aluminium alloy columns with bisymmetrical cross-section. It is assumed that the column material behaviour is described by the Ramberg–Osgood constitutive equation in non-linear elastic range. The stationary total energy principle is used to derive the governing non-linear differential equation. An approximate solution of the equation...
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Synthesis of Combretastatin A-4 Analogs and their Biological Activities
PublikacjaCombretastatin A-4 (CA-4) is a natural product, which consists of two phenyl rings, linked by an ethylene bridge. CA-4, inhibitor of polymerization of tubulin to microtubules, possesses a strong antitumor and anti-vascular properties both in vitro and in vivo. Previous studies showed that disodium phosphate salt of CA-4, a water-soluble prodrug is well tolerated at therapeutically useful doses. However, it should be noted that...
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Aggregation of imidazoacridinones - spectroscopic and microcalorimetric approach
PublikacjaImidazoacridinones (IA) belong to a group of polycyclic heteroaromatic antitumor compounds. IA create the aggregated form in water solution. Self-association of substances is a very important phenomenon in many fields of applied chemistry. It is also fundamental model reaction of many kinds of molecular interactions such as the micelle formation of amphiphilic substances and the binding of small organic molecules to macromolecules....
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Isolation and structure of a covalent cross-link adduct between mitomycin C and DNA
PublikacjaA DNA cross-link adduct of the antitumor agent mitomycin C (MC) to DNA has been isolated and characterized; the results provide direct proof for bifunctional alkylation of DNA by MC. Exposure of MC to Micrococcus luteus DNA under reductive conditions and subsequent nuclease digestion yielded adducts formed between MC and deoxyguanosine residues. In addition to the two known monoadducts, a bisadduct was obtained. Reductive MC activation...
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3D POINT-CLOUD SPATIAL EXPANSION BY TOTAL LEAST-SQUARES LINE FITTING
PublikacjaPoint-cloud spatial expansion (PCSE) allows the creation of a new pointcloud form that presents an alternative geometry of an entire object in a single spatial view. Spatial expansion facilitates the analysis process and introduces an additional spatial parameter describing the point cloud. An important element of the PCSE method is determining the position of the axis of symmetry of a symmetrical object: the procedure for determining...
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Impact of cross-section centers estimation on the accuracy of the Point cloud spatial expansion using robust M-estimation and Monte Carlo simulation
PublikacjaThe point cloud spatial expansion (PCSE) method creates an alternative form of representing the shape of symmetrical objects and introduces additional descriptive geometric parameters. An important element of the procedure is determining the course of the axis of symmetry of cylindrical objects based on cross-sections of point clouds. Outliers occurring in laser measurements are of great importance in this case. In this study,...
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NANOCRYSTALLINE CATHODES FOR SOLID OXIDE FUEL CELLS MADE OF NOBLE METALS
PublikacjaCathodes for solid oxide fuel cells prepared by the infiltration method at 600 °C are presented. The infiltration method allows to produce stable, nanostructured electrodes. Cathodes were prepared using gold, platinum, La2NiO4+δ (L2N) and La0.6Sr0.4Co0.2Fe0.8O3 δ (LSCF). Symmetrical cathode/electrolyte/cathode samples were prepared and examined with SEM microscopy and electrochemical impedance spectroscopy. Despite successful deposition...
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Spatially variant PSF modeling in confocal macroscopy
PublikacjaThe point spread function (PSF) of imaging systems plays an essential role in image reconstruction. In the context of confocal microscopy, optical performance degrades towards the edge of the field of view. In confocal macroscopy, the related artifacts are even stronger, as the field of view is much larger. Because the related PSFs are strongly spatially variant, it is essential to be able to model them with few parameters. The...
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Algorytmy wyodrębniania składowych symetrycznych sygnału pomiarowego napięcia w przypadku asymetrii sieci trójfazowej
PublikacjaW artykule zaprezentowano działanie wybranych algorytmów wykorzystywanych do wyodrębniania składowych symetrycznych z sygnałów pomiarowych napięcia lub prądu w przypadku wystąpienia asymetrii trójfazowej sieci elektroenergetycznej. Weryfikacji działania algorytmów dokonano na podstawie badań symulacyjnych i laboratoryjnych w układzie w którym jako odbiornik zastosowano stojan maszyny asynchronicznej pierścieniowej. Określono wpływ...
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Utilizing Genome-Wide mRNA Profiling to Identify the Cytotoxic Chemotherapeutic Mechanism of Triazoloacridone C-1305 as Direct Microtubule Stabilization
PublikacjaRational drug design and in vitro pharmacology profiling constitute the gold standard in drug development pipelines. Problems arise, however, because this process is often dicult due to limited information regarding the complete identification of a molecule’s biological activities. The increasing aordability of genome-wide next-generation technologies now provides an excellent opportunity to understand a compound’s diverse eects...
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Design and optimization of a novel compact broadband linearly/circularly polarized wide-slot antenna for WLAN and Wi-MAX applications
PublikacjaA novel topologically modified structure of a compact low profile wide-slot antenna for broadband applications is presented. The antenna comprises a modified E-shaped slot with unequal arm lengths in the ground plane, and a parasitic quasi-rectangular loop placed coplanar with the feedline. For exciting orthogonal modes with equal amplitude, a single-point feeding technique with an asymmetrical geometry of the coplanar waveguide...
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DNA-reactive anticancer imidazoacridinone C-1311 is a new inhibitor of hypoxia-inducible factor 1 alpha, vascular endothelial growth factor and tumor angiogenesis
PublikacjaHypoxia-inducible factor 1 (HIF-1) plays a critical role for tumor adaptation to hypoxia and promotes angiogenesis. Antitumor imidazoacridinone C-1311 is a DNA reactive topoisomerase II and FLT3 receptor tyrosine kinase inhibitor selected for phase II clinical trials for breast cancer. Here, we demonstrate the new mechanism of C-1311 action involving HIF-1a, vascular endothelial growth factor (VEGF) and angiogenesis as additional...
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The extended version of restriction analysis approach for the examination of the ability of low-molecular-weight compounds to modify DNA in a cell-free system
PublikacjaOne of the primary requirements in toxicology is the assessment of ability of chemicals to induce DNA covalent modification. There are several well-established methods used for this purpose such as 32P-Postlabeling or HPLC-MS. However, all of these approaches have difficult to overcome limitations, which prevents their use in genotoxin screening. Here, we describe the simple protocol exploiting specificity of restriction enzymes...
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Three electrode configuration measurements of electrolyte-diffusion barrier-cathode interface
PublikacjaMeasurements of a system consisting of cathode/doped ceria diffusion barrier/doped zirconia electrolyte were made using two- and three-electrode configuration. Results obtained on a three-electrode measurement configuration were compared with and reflect the results obtained in two-electrode configuration. Three-electrode measurements allowed separating the impact of the symmetrical interface in the investigated system. They also...
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Commitment Ladder in the Relationship between Service Providers and Customers as Added Value in Sustainable Services Development
PublikacjaThe socioeconomic sphere and the relationships in which commitment occurs are important elements in the development of sustainable services. The study reported in this article identifies the elements that influence the development of the relationship between service providers and their customers and proposes a model that describes the state of the relationship between service providers and customers in terms of symmetrical commitment...
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A novel microstrip dual-layer rat-race coupler with compact size and enhanced bandwidth
PublikacjaMicrowave hybrid couplers are crucial components of mixers, phase shifters, amplifiers and other high-frequency systems. Conventional couplers are characterized by large size which limits their usefulness in modern applications. In this work, a novel compact rat-race coupler with enhanced bandwidth has been proposed. The structure consists of six compact microstrip resonant cells. It is implemented on two separate layers which permits...
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LaNi1-xCoxO3-δ(x=0.4 to 0.7) cathodes for solid oxide fuel cells by infiltration
PublikacjaPerformance of LaNi 1-x Co x O 3−δ (LNC) (x=0.4 to 0.7) as a cathode in solid oxide fuel cell (SOFC) is evaluated. Symmetrical cathode/electrolyte/cathode cells for electrochemical testing are prepared by infiltration of yttria stabilized zirconia (YSZ) backbone with LNC solutions. It is showed that the cathode infiltrated with LaNi 0.5 Co 0.5 O 3−δ (LNC155) has the lowest polarization resistance and activation energy, 197 mΩ cm...
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Experiments and calibration of a bond-slip relation and efficiency factors for textile reinforcement in concrete
PublikacjaTextile reinforcement yarns consist of many filaments, which can slip relative each other. At modelling of the global structural behaviour, interfilament slip in the yarns, and slip between the yarns and the concrete can be considered by efficiency factors for the stiffness and strength of the yarns, and by applying a bond-slip relation between yarns and concrete. In this work, an effective and robust method for calibration of...
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Design Evolution of the Ultrasonic Piezoelectric Motor Using Three Rotating Mode Actuators
PublikacjaThe development process and experimental investigation of the multicell piezoelectric motor is presented in this paper. The proposed design consists of three individual cells integrated into the stator, double rotor, and a preload system. Those elements are combined into a symmetrical structure of the motor. The two new prototypes have been designed, simulated and tested. Finite element numerical analysis is carried out to obtain...
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Influence of fasteners and connections flexibility on deflections of steel building including the stressed skin effect
PublikacjaThe paper presents the analysis of the influence of fasteners and connections flexibility on displacements of symmetrical single-bay pitched-roof steel building, including trapezoidal cladding acting as a diaphragm. The purpose of the article was to compare numerical models with and without taking into consideration fasteners and connections flexibility in order to observe the differences in transverse stiffness of the building...
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Design and Experiments of a Piezoelectric Motor Using Three Rotating Mode Actuators
PublikacjaThis paper represents a numerical and experimental investigation of the multicell piezoelectric motor. The proposed design consists of three individual cells that are integrated into the stator, double rotor, and a preload system combined into a symmetrical structure of the motor. Each of the cells is characterized by a traveling wave and rotating mode motor. A finite element numerical analysis is carried out to obtain optimal...
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Numerical Analysis of Impact of Energy Buoy Anchoring Configurations on its Motion and Efficiency
PublikacjaThis paper presents a numerical analysis of the impact of energy buoy mooring configurations on its movement on the wave and effectiveness. The method used to analyse the buoy movement modelling in six degrees of freedom was described in a paper presented at the Conference 2011. Simulations of the buoy movement in regular wave and power calculations were conducted for several configurations of anchoring systems and position of...
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Comparative study of flow condensation in conventional and small diameter tubes
PublikacjaFlow boiling and flow condensation are often regarded as two opposite or symmetrical phenomena, however their description with a single correlation has yet to be suggested. In the case of flow boiling in minichannels there is mostly encountered the annular flow structure, where the bubble generation is not present. Similar picture holds for the case of inside tube condensation, where annular flow structure predominates. In such...
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TMSCL as a rate accelerating additive in acylations of amines with 5-(α- amino-α'-hydroxy)methylene meldrum's acids
PublikacjaAspects are presented of the acylation of amines, alcohols and thiols with 5-(α-amino- α'-hydroxy)methylene Meldrum's acids. We placed special emphasis on the acylation reaction of secondary amines with 5-(α-amino- α'-hydroxy)methylene Meldrum's acids, which, due to their basicity, caused problems concerning salt formation with a Meldrum acid derivative. We found that secondary amines, which react at the slowest rate and with a...
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Tmscl as a rate accelerating additive in acylations of amines with 5-(α-amino- α'-hydroxy)methylene meldrum's acids
PublikacjaAspects are presented of the acylation of amines, alcohols and thiols with 5-(α-amino- α'-hydroxy)methylene Meldrum's acids. We placed special emphasis on the acylation reaction of secondary amines with 5-(α-amino- α'-hydroxy)methylene Meldrum's acids, which, due to their basicity, caused problems concerning salt formation with a Meldrum acid derivative. We found that secondary amines, which react at the slowest rate and with a...
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Bioavailability of Tannins and Other Oligomeric Polyphenols: a Still to Be Studied Phenomenon
PublikacjaPurpose of Review Polyphenols are a group of plant secondary metabolites characterized with the presence ofmultiples of phenol structural units. Tannins are plant originated phenolic substances, which play an important role in plant defense system as well as have found applications in medicine, industry, and other fields of human activity. Despite these, the mechanisms of bioavailability of these substances are poorly studied and...
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The Effect of Conjugation with Octaarginine, a Cell-Penetrating Peptide on Antifungal Activity of Imidazoacridinone Derivative
PublikacjaAcridine cell-penetrating peptide conjugates are an extremely important family of compounds in antitumor chemotherapy. These conjugates are not so widely analysed in antimicrobial therapy, although bioactive peptides could be used as nanocarriers to smuggle antimicrobial compounds. An octaarginine conjugate of an imidazoacridinone derivative (Compound 1-R8) synthetized by us exhibited high antifungal activity against reference...
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Enhanced Activity of P4503A4 and UGT1A10 Induced by Acridinone Derivatives C-1305 and C-1311 in MCF-7 and HCT116 Cancer Cells: Consequences for the Drugs’ Cytotoxicity, Metabolism and Cellular Response
PublikacjaActivity modulation of drug metabolism enzymes can change the biotransformation of chemotherapeutics and cellular responses induced by them. As a result, drug-drug interactions can be modified. Acridinone derivatives, represented here by C-1305 and C-1311, are potent anticancer drugs. Previous studies in non-cellular systems showed that they are mechanism-based inhibitors of cytochrome P4503A4 and undergo glucuronidation via UDP-glucuronosyltranspherase...
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Improved cytotoxicity and preserved level of cell death induced in colon cancer cells by doxorubicin after its conjugation with iron-oxide magnetic nanoparticles
PublikacjaA promising strategy for overcoming the problem of limited efficacy in antitumor drug delivery and in drug release is the use of a nanoparticle-conjugated drug. Doxorubicin (Dox) anticancer chemotherapeutics has been widely studied in this respect, because of severe cardiotoxic side effects. Here, we investigated the cytotoxic effects, the uptake process, the changes in cell cycle progression and the cell death processes in the...
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LC-MS/MS dtermination of isoprostanes in plasma samples collected from mice exposed to doxorubicin or tert-butyl hydroperoxide
PublikacjaIsoprostanes are stable products of arachidonic acid peroxidation and are regarded as the most reliable markers of oxidative stress in vivo. Here we describe the LC-MS/MS procedure enabling simultaneous determination of four regioisomers (8-iso prostaglandin F2α, 8-iso-15(R)-prostaglandin F2α, 11β-prostaglandin F2α, 15(R)-prostaglandin F2α) in plasma samples collected from mice. The four plasma isoprostanes are determined by LC–ESI-MS/MS...
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Intercalation complex of imidazoacridinone C-1311, a potential anticancer drug, with DNA helix d(CGATCG)2: stereostructural studies by 2D NMR spectroscopy.
PublikacjaImidazoacridinone C-1311 (Symadex®) is a powerful antitumor agent, which successfully made its way through the Phase I clinical trials and has been recommended for Phase II few a years ago. It has been shown experimentally that during the initial stage of its action C-1311 forms a relatively stable intercalation complex with DNA, yet it has shown no base-sequence specificity while binding to DNA. In this paper, the d(CGATCG)2:C-1311...
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Liquid chromatography techniques for separation of flavonoids from Droseraceae
PublikacjaFlavonoids which are presented in insectivorous plants of the Droseraceae family have wide range of advantageous properties i.e. an antioxidant, anti-inflammatory and antimicrobial activities, antitumor activity was reported as well.The purpose of the research was to develop the most favourable conditions for liquid chromatographic separation and identification of myricetin and quercetin in extracts of insectivorous plants. In...
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Experimental research of the effect of face milling strategy on the flatness deviations
PublikacjaIn this paper the dependencies between face milling strategy of EN AW6082-T6 aluminum alloy samples, with difference thicknesses (6, 8, and 12 mm) and two cold rolling directions, and flatness deviations were presented. Three strategies of milling included different proportions of material removed from both sides of the plates. This approach allowed to control the proportions of residual surface stresses on both sides of the specimens,...
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EM-driven topology evolution for bandwidth enhancement of hybrid quadrature patch couplers
PublikacjaA broad operational bandwidth is one of the key performance figures of hybrid patch couplers. Due to the lack of systematic design procedures, bandwidth enhancement is normally obtained through manual modifications of the structure geometry. In this work, an optimization-based topology evolution for EM-driven design of patch couplers with enhanced bandwidth has been proposed. The method exploits a novel spline-based EM model where...
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Syntheses, Structures and Reactivity of Terminal Phosphido Complexes of Iron(II) Supported by a β-Diketiminato Ligand
PublikacjaWe report the synthesis of the first series of terminal phosphido iron complexes supported by a β‐diketiminato ligand (Dippnacnac) and their catalytic activity in dehydrocoupling of secondary phosphines. Anionic and neutral mono‐ or diphosphido complexes were obtained from the reaction of [(Dippnacnac)FeCl2Li(dme)2] with the R2PLi (R = iPr, tBu, Cy, Ph) phosphides by tuning the stoichiometric ratio, polarity of the solvent, and...
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Cable-stayed bridges. Basic static schemes
PublikacjaThe paper presents an overview of shaping of cable-stayed bridges. Historical background, basic static sketches and overview of selected bridges are included. Selected natural solutions and interesting unrealized projects were presented. Basic ideas and most important principals are discussed. The examples and sketches were given an author's comment. Static diagrams of two pylon structures with three variants of the arrangement...
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Hydraulic resistance analyses of selected elements of the prototype Stirling engine
PublikacjaThe paper presents the results of simulation tests of hydraulic resistance and temperature distribution of the prototype Stirling alpha engine supplied with waste heat. The following elements were analyzed: heater, regenerator and cooler. The engine uses compressed air as a working gas. Analyses were carried out for three working pressure values and different engine speeds. The work was carried out in order to optimize the configuration...
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A Simple-Topology Compact Broadband Circularly Polarized Antenna With Unidirectional Radiation Pattern
PublikacjaIn this letter, a geometrically simple, reflector-backed single-point-fed circularly polarized (CP) antenna with unidirectional radiation pattern is presented. The structure comprises a simple coplanar waveguide (CPW) feeding circuit with an open slot etched on one side of the coplanar ground. The enhanced CP bandwidth is obtained by combining the loop mode, the slot mode, and the asymmetrical configuration of the coplanar ground...
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Blogi jako platforma komunikowania na przykładzie blogów uczelnianych
PublikacjaW artykule stawiam tezę o istotnej roli blogów jako niezwykle skutecznej platformie komunikacyjnej w dobie konwergencji mediów. Szczególnie ważną rolę to specyficzne narzędzie komunikacyjne może odegrać w działaniach public relations uczelni: jako narzędzie za pomocą którego można najpełniej realizować funkcje uczelni i te, które realizuje najwyższy poziom rozwoju PR - w komunikacji dwukierunkowej symetrycznej zgodnie z modelem...
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Centrally Pivoted Tilting Pad Thrust Bearing with Carbon-Based Coated Collar—Experimental Results of Low- and Medium-Speed Operation
PublikacjaExperimental results of the research on a tilting pad thrust bearing with symmetrical pad support in the conditions of high loads and low speeds are presented in the paper. As described in the literature review, experimental results of tilting pad bearings at low speed/high load regime and transient conditions are rare. Unusual material selection - steel pad against a DLC-type coating on the collar was utilized. Such material combination...
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Antiproliferative, Antiangiogenic, and Antimetastatic Therapy Response by Mangiferin in a Syngeneic Immunocompetent Colorectal Cancer Mouse Model Involves Changes in Mitochondrial Energy Metabolism
PublikacjaIn spite of the current advances and achievements in cancer treatments, colorectal cancer (CRC) persists as one of the most prevalent and deadly tumor types in both men and women worldwide. Drug resistance, adverse side effects and high rate of angiogenesis, metastasis and tumor relapse remain one of the greatest challenges in long-term management of CRC and urges need for new leads of anticancer drugs. We demonstrate that CRC...
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DNA-damaging imidazoacridinone C-1311 induces autophagy followed by irreversible growth arrest and senescence in human lung cancer cells
PublikacjaImidazoacridinone 5-diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311) is an antitumor inhibitor of topoisomerase II and FMS-like tyrosine kinase 3 receptor. In this study, we describe the unique sequence of cellular responses to C-1311 in human non-small cell lung cancer (NSCLC) cell lines, A549 and H460. In A549 cells, C-1311 (IC80 = 0.08 µM) induced G1 and G2/M arrests, whereas H460 cells (IC80 = 0.051 µM) accumulated...
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The role of glucuronidation in drug resistance
PublikacjaThe final therapeutic effect of a drug candidate, which is directed to a specific molecular target strongly depends on its absorption, distribution, metabolism and excretion (ADME). The disruption of at least one element of ADME may result in serious drug resistance. In this work we described the role of one element of this resistance: phase II metabolism with UDP-glucuronosyltransferases (UGTs). UGT function is the transformation...
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CYP3A4 overexpression enhances apoptosis induced by anticancer agent imidazoacridinone C-1311, but does not change the metabolism of C-1311 in CHO cells
PublikacjaWe examine whether CYP3A4 overexpression influences the rate and pattern of antitumor imidazoacridinone C-1311 metabolism, in relation to the impact of this overexpression on cell cycle progression and final cellular response of CHO cells following C-1311 treatment. Methods: Three CHO cell lines: CHO-WT, wild type, CHO-HR, overexpressing cytochrome P450 reductase (CPR) and CHO-HR-3A4, coexpressing CPR and CYP3A4 were applied....