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Search results for: active pharmaceutical ingredients
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Synthesis and biological activity of ester derivatives of mycophenolic acid and acridines/acridones as potential immunosuppressive agents
PublicationImproved derivatives of mycophenolic acid (MPA) are necessary to reduce the frequency of adverse effects, this drug exerts in treated patients. In this study, MPA was coupled with N-(x-hydroxyalkyl)-9-acridone-4-carboxamides or N-(x-hydroxyalkyl)acridine-4-carboxamides to give respective ester conjugates upon Yamaguchi protocol. This esterification required protection of phenol group in MPA. Designed conjugates revealed higher...
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Security and Anonymity in Agent Systems
PublicationMany agent systems have been developed and suggested for commercial application. However, in spite of the significant potential offered by the agent paradigm, the lack of such important properties as security, anonymity and untracebility especially in open dynamical environment, such as the Internet, has blocked the active implementation of agent technologies. Protecting agent systems poses a more demanding challenge comparing...
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THE PHASE SHIFTERS INFLUENCE ON THE POWER SYSTEM STABILITY
PublicationThe paper presents the effect of phase shifters as FACTS devices on the possibility of improving the angle stability. Presented results obtained by the dynamic simulation performed on the mathematical model of the three machine system cooperating with the 400 kV network. The generative blocks models include turbine models with their controllers and models of synchronous generators with their excitation systems and voltage regulation....
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FEX a Fingers Extending eXoskeleton for Rehabilitation and Regaining Mobility
PublicationThis paper presents the design process of an exoskeleton for executing human fingers’ extension movement for the rehabilitation procedures and as an active orthosis purposes. The Fingers Extending eXoskeleton (FEX) is a serial, under-actuated mechanism capable of executing fingers’ extension. The proposed solution is easily adaptable to any finger length or position of the joints. FEX is based on the state-of-art FingerSpine serial...
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Trade differentiation and the characteristics of new imported and exported products - international panel data analysis
PublicationDrawing on o large panel of international economies we have shown how the set of imported and exported products evolves in economic growth process. Strong activity at the extensive margin, manifested through the rise in the number of active export and import lines, is typical for early stages of development. Trade diversification tendency, typical for a predominant mass of observations in our panel, is associated with changes in...
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In silico approaches for better understanding cysteine cathepsin-glycosaminoglycan interactions
PublicationCysteine cathepsins constitute the largest cathepsin family, with 11 proteases in human that are present primarily within acidic endosomal and lysosomal compartments. They are involved in the turnover of intracellular and extracellular proteins. They are synthesized as inactive procathepsins that are converted to mature active forms. Cathepsins play important roles in physiological and pathological processes and, therefore, receive...
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Quenching of bright and dark excitons via deep states in the presence of SRH recombination in 2D monolayer materials
PublicationTwo-dimensional (2D) monolayer materials are interesting systems due to an existence of optically non-active dark excitonic states. In this work, we formulate a theoretical model of an excitonic Auger process which can occur together with the trap-assisted recombination in such 2D structures. The interactions of intravalley excitons (bright and spin-dark ones) and intervalley excitons (momentum-dark ones) with deep states located...
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Investigations on the removal of hydrophobic odorous volatile organic compounds by biotrickling filtration monitored with electronic nose
PublicationThe presented paper presents the results of research on the removal of selected hydrophobic volatile organic compounds (VOCs) from their mixture with air by means of a trickled-bed biofiltration. The efficiency of the removal of toluene and α-pinene, as model VOCs, in a three-section biotrickling filter is evaluated using GCFID and additionally monitored with an electronic nose. The results show that the removal of the model mixture...
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Synthesis and properties of carboxy derivative of Epidian 6 monomethacrylate (in English)
PublicationWe present the synthesis of an oligomer with carboxy and methacrylic groups based on Epidian 6. The effect of the catalyst nature and amount, solvent nature and process temperature on the rate of the reaction between Epidian6 monomethacrylate and adipic acid was examined at 313, 323 and 333 K in the presence of 4-dimethylaminopyridine, 1,4-diazobicyclo[2.2.2]octane, and benzyltriammonium chloride. The synthesized oligomer was characterized...
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Immunosuppressive properties of amino acid and peptide derivatives of mycophenolic acid
PublicationMycophenolic acid (MPA) was coupled with amino acids and biologically active peptides including derivatives of tuftsin to modify its immunosuppressive properties. Both amino acid unit in the case of simple MPA amides and modifications within peptide moiety of MPA - tuftsin conjugates influenced the observed activity. Antiproliferative potential of the obtained conjugates was investigated in vitro and MPA amides with threonine methyl...
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Chiral-based optical and electrochemical biosensors: Synthesis, classification, mechanisms, nanostructures, and applications
PublicationThis review seeks to collect, summarize, classify and discuss the latest advances in chiral-based optical biosensors. Starting from the identification of chiral molecules, photoluminescence, and electrochemical sensors, applications of chiral structures in biosensing molecules are reviewed. Then, biosensors working on the basis of chirality are classified, followed by summarizing the outcomes of research works on design, synthesis,...
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Cloning, expression, and biochemical characterization of a coldactive GDSL-esterase of a Pseudomonas sp. S9 isolated from Spitsbergen island soil
PublicationAn estS9 gene, encoding an esterase of the psychrotolerant bacterium Pseudomonas sp. S9 was cloned and sequenced. The deduced sequence revealed a protein of 636 amino acid residues with a molecular mass of 69 kDa.Further amino acid sequence analysis revealed that the EstS9 enzyme contained a G-D-S-L motif centered at a catalytic serine, an N-terminal catalytic domain and a C-terminal autotransporter domain. Two recombinant E. coli...
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Study of anticorrosion and microwave absprption properties of NiZn ferrite pigments
PublicationPurpose - The purpose of this paper is to report the electrochemical verification of anticorrosive properties of NiZn ferrites as pigments in protective coatings and evaluation of their microwave absorbing properties. Design/methodology/approach - Ferrites, represented by formula NixZn(1-x)Fe2O4, where x=0, 0.2, 0.4, 0.6, 0.8, 1.0, were synthesized using a ceramic method. The samples of ferrites were examined by X-ray diffraction...
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Wear of electroplated diamond tools in lap-grinding of Al2O3 ceramic materials
PublicationCurrent development of modern products, together with ever-increasing demands for their operation and usage, necessitate the search for new processing methods. Abrasive machining is widely used in many industrial areas, especially for processing difficult-to-machine materials such as advanced ceramics. Grinding with lapping kinematics, also called lap-grinding, is still one of the innovative methods of abrasive processing being...
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Diamond-Based Supercapacitors with Ultrahigh Cyclic Stability Through Dual-Phase MnO2-Graphitic Transformation Induced by High-Dose Mn-Ion Implantation
PublicationWhile occasionally being able to charge and dischargemore quickly than batteries, carbon-based electrochemical supercapacitors(SCs) are nevertheless limited by their simplicity of processing, adjustableporosity, and lack of electrocatalytic active sites for a range of redox reactions.Even SCs based on the most stable form of carbon (sp3carbon/diamond)have a poor energy density and inadequate capacitance retention during longcharge/discharge...
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Nonlinear Control of a Doubly Fed Generator Supplied by a Current Source Inverter
PublicationNowadays, wind turbines based on a doubly fed induction generator (DFIG) are a commonly used solution in the wind industry. The standard converter topology used in these systems is the voltage source inverter (VSI). The use of reverse-blocking insulated gate bipolar transistor (RB-IGBT) in the current source inverter topology (CSI), which is an alternative topology, opens new possibilities of control methods. This paper presents...
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Bee Bread Exhibits Higher Antimicrobial Potential Compared to Bee Pollen
PublicationThis study aimed at investigation of the antimicrobial potential of ethanolic extracts of bee bread (BB) and bee pollen (BP) and suspensions of these products in MHB (Mueller Hinton Broth). We covered 30 samples of BP and 19 samples of BB harvested in Polish apiaries. Slightly lower activity was observed against Gram-negative bacteria compared to Gram-positive staphylococci. BB extracts exhibited higher inhibitory potential with...
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Visible light photocatalysis employing TiO2/SrTiO3-BiOI composites: Surface properties and photoexcitation mechanism
PublicationA series of binary TiO2/SrTiO3 and ternary TiO2/SrTiO3_BiOI composites have been synthesized using multistep preparation method. Characterization of the obtained photocatalysts covered complex analysis including morphology + y (SEM), BET specific surface area, porosity, optical properties (DRS), chemical composition of surface (XPS), crystal structure and crystal size (XRD). UV–vis and Vis ligh induced photocatalytic activity was...
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Power Electronic Transformer For Smart Grid Application
PublicationIn this paper the control system of Power Electronic Transformer (PET) for the Smart Grid application is proposed. The structure of PET is based on two Cascaded H-bridge (CHB) converters. The electrical energy is transferred between converters using Dual-Active-Bridges (DAB) and high-frequency transformers. This type of coupling has been used to connect the DC-links of all H-bridges. The proposed control system for PET makes it...
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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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Molecular geometry and optical activity of helically chiral N-nitrosamines derived from 1,2,3,4-tetrahydro- and 1,2,3,4,7,8,9,10-octahydro-1,10-phenanthroline
PublicationX-ray crystallographic analysis of the title N-nitrosamines revealed that they assume helical conformations in the solid state. Nitrosamines 1b and 2b were resolved by inclusion crystallization with optically active diols (TADDOLs). The absolute configuration of the guest molecules in the complexes 1b·3b and 2b·3b was assigned as M. The optical activity of the resolved compounds is manifested by their solid state CD spectra, which...
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Diver Observations by Means of Acoustic Methods
PublicationSearching for objects, especially small ones, moving under water near its the free surface, is always not an easy task. Designing tools for the detection of such targets is a real challenge when the possibility of a terrorist attack is a real threat. This paper presents some aspects of diver detection by means of acoustics methods, both active (side scan sonar) and passive ones (linear receiving antenna). This approach is quite...
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Development of an emulation platform for synchronous machine power generation system using a nonlinear functional level model
PublicationThe article presents the Power Hardware in the Loop (PHIL) approach for an autonomous power system analysis based on the synchronous generator model incorporating magnetic saturation effects. The model was prepared in the MATLAB/Simulink environment and then compiled into the C language for the PHIL platform implementation. The 150 kVA bidirectional DC/AC commercial-grade converter was used to emulate the synchronous generator....
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Acoustic Hysteresis in Flows with Different Kinds of Relaxation and Attenuation
PublicationGraphs in the thermodynamic plane acoustic pressure versus excess acoustic density representing acoustic hysteresis, are considered as indicators of relaxation processes, equilibrium parameters of a flow, and kinds of wave exciters. Some flows with deviation from adiabaticity are examined: the Newtonian flow of a thermocon- ducting gas, the flow of a gas with vibrational relaxation, the flow of liquid electrolyte with a chemical...
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Nonlinear Excitation of the Non-Wave Perturbations by the Magnetoacoustic Waves in the Non-Isentropic Plasma
PublicationNonlinear excitation of slow modes by the planar magnetosonic perturbations in a plasma is discussed. Plasma is an open system due to radiation and external heating. This may stipulate enhancement of wave perturbations and hence the acoustical activity of plasma. Plasma is assumed to be a homogeneous ideal gas with infinite electrical conductivity. The straight magnetic field is orthogonal to the velocity of fluid’s...
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NANOCRYSTALLINE CATHODES FOR SOLID OXIDE FUEL CELLS MADE OF NOBLE METALS
PublicationCathodes 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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Thermal sequences database of the skin flaps in breast reconstruction and burns
PublicationThis paper presents a database of Active Dynamic Thermography (ADT) thermal sequences gathered throughout 6 year study on ADT application in skin flap blood perfusion monitoring and burn wounds diagnosis. For skin flap monitoring the database comprises of data collected during three different breast reconstruction procedures. The patients were monitored pre, intra and post surgically within 90 days period. The sequences were used...
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Thermal sequences database of the skin flaps in breast reconstruction and burns
PublicationThis paper presents a database of Active Dynamic Thermography (ADT) thermal sequences gathered throughout 6 year study on ADT application in skin flap blood perfusion monitoring and burn wounds diagnosis. For skin flap monitoring the database comprises of data collected during three different breast reconstruction procedures. The patients were monitored pre, intra and post surgically within 90 days period. The sequences were used...
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Speech recognition system for hearing impaired people.
PublicationPraca przedstawia wyniki badań z zakresu rozpoznawania mowy. Tworzony system wykorzystujący dane wizualne i akustyczne będzie ułatwiał trening poprawnego mówienia dla osób po operacji transplantacji ślimaka i innych osób wykazujących poważne uszkodzenia słuchu. Active Shape models zostały wykorzystane do wyznaczania parametrów wizualnych na podstawie analizy kształtu i ruchu ust w nagraniach wideo. Parametry akustyczne bazują na...
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Photoelectrochemical properties of BIMEVOX (ME=Cu, Zn, Mn) electrodes in contact with aqueous electrolyte
PublicationLayered oxide Bi4O2O11 and mixed oxides of bismuth, vanadium and a third metal (ME = Cu, Zn, Mn) were synthesized and characterized using XRD, Raman and SEM. The energy band gap (Eg) of samples determined using UV–VIS reflectance spectra equals to 2.46, 2.34, 2.27 and 2.18 eV for Bi4V2O11, BICUVOX (Bi2V1 − xCuxO5.5 − 3x/2), BIZNVOX (Bi2V1 − xZnxO5.5 − 3x/2) and BIMNVOX (Bi2V1 − xMnxO5.5 − x/2) (x = 0.1), respectively. Open circuit...
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Time variable gain for long range sonar with chirp sounding signal
PublicationThe main purpose of applaying Time Variable Gain (TVG) in active sonars with digital signal processing is to reduce dynamic range of echo signal and adapt it to the dynamic range of the analogue to digital conversion. With high transmission losses level, the dynamic range of the input signal in long range sonars can be very high and even exceed 200dB. When chirp sounding signals with matched filtration are used, sonars can raech...
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Biobójcze wykończenie tkanin
PublicationThe problem of nosocomial infections is nothing new. In places, where people, whose immune system is weakened, are gathered and subjected to various kinds of treatments, the risk of infection increases considerably. The use of textiles with biocidal finishing, which contains nanoAg and nanoCu, may give an additional protection against nosocominal infections. This article presents the latest information regarding various methods...
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Impact of R/X ratio of distribution network on selection and control of energy storage units
PublicationThe interest in energy storage is still increasing. Energy storage units are installed in high voltage networks, medium voltage networks and low voltage distribution networks as well. These units are often used to improve power quality. One of the criteria for improving power quality is reducing voltage deviations. Depending on the type of network and specifying its R/X ratio, this criterion can be fulfilled by control of active...
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Hysteresis curves and loops for harmonic and impulse perturbations in some non-equilibrium gases
PublicationEvolution of sound in a relaxing gas whose properties vary in the course of wave propagation, is studied. A relaxing medium may reveal normal acoustic properties or be acoustically active. In the first case, losses in acoustic energy lead to an increase in internal energy of a gas similarly as it happens in Newtonian fluids. In the second case, acoustic energy increases in the course of sound propagation, and the internal energy...
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Miniaturization of ESPAR Antenna Using Low-Cost 3D Printing Process
PublicationIn this paper, the miniaturized electronically steerable parasitic array radiator (ESPAR) antenna is presented. The size reduction was obtained by embedding its active and passive elements in polylactic acid (PLA) plastic material commonly used in low-cost 3D printing. The influence of 3D printing process imperfections on the ESPAR antenna design is investigated and a simple yet effective method to compensate them has been proposed....
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Tetrahedrally modified MnMe0.1Co1.9O4 (Me = Zn, Mg, Li) spinels for non-enzymatic glucose sensing
PublicationIn this work, tetrahedrally modified MnMe0.1Co1.9O4 (Me = Zn, Mg, Li) spinels were prepared via the sol–gel synthesis method with subsequent ball-milling fragmentation. The prepared samples were evaluated as glucose–sensing catalyst. The reference MnCo2O4 spinel exhibited a sensitivity of 49 µA mM−1 cm−2 and a nonlinearity error of 5.2% in the response range from 0.02 to 1 mM. The partial substitution of cobalt in the reference...
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Experimental study of the multi-disc negative brake for a hydraulic motor
PublicationThis paper describes the methodology for experimental testing of a multi-disc brake. The construction of this brake was also present. The brake is dedicated to hydraulic motors with a small working volume. Experimental tests were carried out on a brake with plates immersed in oil and, for comparison, tests were carried out on a dry brake. As a result of the tests, the permissible torque (load) that is able to transfer the brake...
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Approaches Towards Better Immunosuppressive Agents
PublicationSeveral classes of compounds are applied in clinics due to their immunosuppressive properties in transplantology and the treatment of autoimmune diseases. Derivatives of mycophe-nolic acid, corticosteroids and chemotherapeutics bearing heterocyclic moieties like methotrexate, azathioprine, mizoribine, and ruxolitinib are active substances with investigated mechanisms of action. However, improved synthetic approaches of known drugs...
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Influence of Dielectric Overlay Permittivity on Size and Performance of Miniaturized ESPAR Antenna
PublicationIn this paper, influence of dielectric overlay permittivity on miniaturized ESPAR antenna parameters is presented. ESPAR antenna is a low-cost and energy-efficient way to implement beam steering capability to a node and improve network performance. The antenna size reduction is obtained by embedding its active and passive elements in ABS based materials of relative permittivity equal to 4, 5.5 and 7.5 in order to achieve network...
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Influence of the jitter buffer on the quality of service VoIP.
PublicationVoIP (Voice over IP) is a modern service with enormous potential for yet further growth. It uses the already available and universally implemented IP transport platform. One significant problem, however, is ensuring the Quality of Service, abbreviated QoS. This paper addresses exactly that issue. In an extensive investigation the influence of jitter buffers on QoS is being examined in depth. Two implementations, namely a passive...
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Novel 1,2,3-Triazole Derivatives as Mimics of Steroidal System—Synthesis, Crystal Structures Determination, Hirshfeld Surfaces Analysis and Molecular Docking
PublicationHerein, we present the synthesis and crystal structures determination of five 4-(1-phenyl-1H-1,2,3-triazol-4-yl)phenol derivatives containing halogen atoms, 6a–e, which may be used as an excellent mimic of steroids in the drug development process. Good quality crystals obtained for all of the synthesized compounds allowed the analysis of their molecular structures. Subsequently, the determined crystal structures were used to calculate...
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New methodology for determination cationic surfactants in liquid environmental samples
PublicationBecause of their specific physical and chemical properties (e.g. amphiphilicity, solubility in polar and nonpolar liquids, ability to form micelles, adsorption at phase boundaries, low toxicity) surfactants (surface-active compounds) are widely applied in industry and in the household. As their applications are on a very large scale, it has become necessary to acquire a more detailed understanding of their environmental fate. Mainly,...
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A new cold-adapted beta-D-galactosidase from the Antarctic Arthrobacter sp. 32c - gene cloning, overexpression, purification and properties
PublicationThe development of a new cold-active β-D-galactosidases and microorganisms that efficiently ferment lactose is of high biotechnological interest, particularly for lactose removal in milk and dairy products at low temperatures and for cheese whey bioremediation processes with simultaneous bio-ethanol production. In this article, we present a new β-D-galactosidase as a candidate to be applied in the above mentioned biotechnological...
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The role of aluminium in metal–organic frameworks derived carbon doped with cobalt in electrocatalytic oxygen evolution reaction
PublicationWater electrolysis is one of the most crucial processes in the development of new energy sources, where ultra-clean fuel is produced - hydrogen. Oxygen evolution reaction (OER) is the sluggish process of overall water splitting. Therefore, this study presents the design, characterization and electrochemical study of cobalt-based electrocatalysts embedded into porous carbons derived from an Al-metal–organic...
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Imidazoacridinone antitumor agent C-1311 as a selective mechanism- based inactivator of human cytochrome P450 1A2 and 3A4 isoenzymes.
Publication5-Diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311), a promising antitumor agent that is also active against autoimmune diseases, was determined to be a selective inhibitor of the cytochrome P450 (CYP) 1A2 and 3A4 isoenzymes. Therefore, C-1311 might modulate the effectiveness of other drugs used in multidrug therapy. The present work aimed to identify the mechanism of the observed C-1311-mediated inactivation of CYP1A2...
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Recombinant !ermostable AP Exonuclease from Thermoanaerobacter tengcongensis: Cloning, Expression, Purification, Properties and PCR Application
PublicationApurinic/apyrimidinic (AP) sites in DNA are considered to be highly mutagenic and must be corrected to preserve genetic integrity, especially at high temperatures. !e gene encoding a homologue of AP exonuclease was cloned from the thermophilic anaerobic bacterium Thermoanaerobacter tengcongensis and transformed into Escherichia coli. The protein product showed high identity (80%) to human Ape1 nuclease, whereas to E. coli exonuclease...
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Knowledge‐Intensive Business Services (KIBS) and Their Role in the Knowledge‐Based Economy
PublicationThe importance of the knowledge‐intensive business services sector for the development of the economy is growing. In the 80s and 90s this sector became the fastest growing sector in the OECD countries (OECD, 2001). Many publications stress its close relationship to the levels of innovation and performance of the whole economy (e.g. Hipp, 1999; Tomlinson, 1999; Aslesen and Isaksen, 2007). It is an increasingly common belief that...
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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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Train the trainer course
PublicationThis chapter presents the concept, evaluation and evaluation results for the train the trainer. This concept of train the trainers is prepared within Workpackage 5 of EU-funded project: MASTER BSR (Erasmus+ Strategic Partnership Programme). Due to the nature of adult learning the content is designed for the use of participatory methods (involved, active). This method uses various techniques of active learning e.g. group work,...
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Anticancer Properties of Amino Acid and Peptide Derivatives of Mycophenolic Acid
PublicationBackground: Although Mycophenolic Acid (MPA) is applied as prodrugs in clinic as an immunosuppressant, it also possesses anticancer activity. MPA acts as Inosine-5’-Monophosphate Dehydrogenase (IMPDH) inhibitor, where the carboxylic group at the end of the side chain interacts with Ser 276 of the enzyme via hydrogen bonds. Therefore, MPA derivatives with other polar groups indicated high inhibition too. On the other hand, potent...