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Wyniki wyszukiwania dla: UGT METABOLIC TRANSFORMATIONS
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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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Phase I and phase II metabolism simulation of antitumor-active 2-hydroxyacridinone with electrochemistry coupled on-line with mass spectrometry.
PublikacjaHere, we report the metabolic profile and the results of associated metabolic studies of 2-hydroxyacridinone (2-OH-AC), the reference compound for antitumor-active imidazo- and triazoloacridinones. Electrochemistry coupled with mass spectrometry was applied to simulate the general oxidative metabolism of 2-OH-AC for the first time. The reactivity of 2-OH-AC products to biomolecules was also examined. The usefulness of the electrochemistry...
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Adipokine and cytokine levels in non-functioning adrenal incidentalomas (NFAI)
PublikacjaDue to the fact that overweight or obesity is accompanied by hormonally active adrenal tumors: Cushing Syndrome-(CS) and Subclinical Cushing Syndrome (SCS), it is of high interest the correlation between different adipokines and cytokines secreted by adipose tissue, with metabolic disorders and hormonal activity in this group. Even in non-functioning adrenal incidentalomas (NFAI) elevated risk for cardiovascular disease and metabolic...
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Sweet grass protection against oxidative stress formation in the rat brain
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Mitochondrial DNA levels in Huntington disease leukocytes and dermal fibroblasts
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Erratum to: Activities of genes controlling sphingolipid metabolism in human fibroblasts treated with flavonoids
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Activities of genes controlling sphingolipid metabolism in human fibroblasts treated with flavonoids
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Evidence for interactions between homocysteine and genistein: insights into stroke risk and potential treatment
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The model homologue of the partially defective human 5,10-methylenetetrahydrofolate reductase, considered as a risk factor for stroke due to increased homocysteine level, can be protected and reactivated by heat shock proteins
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Factors and processes modulating phenotypes in neuronopathic lysosomal storage diseases
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Thyroid Peroxidase as an Autoantigen in Hashimoto’s Disease: Structure, Function, and Antigenicity
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Thyroid Peroxidase Revisited – Whatʼs New?
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In vivo imaging of the human eye using a two-photon excited fluorescence scanning laser ophthalmoscope
PublikacjaBACKGROUND. Noninvasive assessment of metabolic processes that sustain regeneration of human retinal visual pigments (visual cycle) is essential to improve ophthalmic diagnostics and to accelerate development of new treatments to counter retinal diseases. Fluorescent vitamin A derivatives, which are the chemical intermediates of these processes, are highly sensitive to UV light; thus, safe analyses of these processes in humans...
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Role of Human UDP-Glucuronosyltransferases in the Biotransformation of the Triazoloacridinone and Imidazoacridinone Antitumor Agents C-1305 and C-1311 : Highly Selective Substrates for UGT1A10
Publikacja5-Diethylaminoethylamino-8-hydroxyimidazoacridinone, C-1311 (NSC-645809), is an antitumor agent shown to be effective against breast cancer in phase II clinical trials. A similar compound, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone, C-1305, shows high activity against experimental tumors and is expected to have even more beneficial pharmacological properties than C-1311. Previously published studies showed that these...
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Electrochemistry meets enzymes: Investigation of the biotransformation pathway of C-1311 based on electrochemical simulation in comparison to in vitro methods.
PublikacjaThe knowledge of the metabolic pathways and the biotransformation of new drugs is one of the major challenges in pharmaceutical research. It is crucial for elucidation of degradation routes of the new biologically active compounds, especially in the area of possible toxicity. Conventional in vitro drug metabolism studies are based on incubating drug candidate with e.g. hepatocytes or, most importantly, liver cell microsomes and...
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Effect of microstructure on mechanical properties and corrosion resistance of 2205 duplex stainless steel
PublikacjaThis 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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Revealing dynamic changes of the volatile profile of food samples using PTR–MS
PublikacjaVolatile compounds carry valuable information regarding the properties of foodstuffs. Volatiles emitted from food can be used as, for example, indicators of quality, shelf-life, or authenticity. A better understanding of the multitude of transformations which occur during food processing could facilitate the optimisation of production, increase the desirability of food products, and also their wholesomeness. However, as some of...
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Urine headspace analysis in medical diagnostics
PublikacjaThe analysis of the volatile organic compounds in the bodily fluids such as urine may provide useful information on the patients’ general health. The potential application of urine headspace analysis could facilitate the diagnostics of various diseases such as metabolic disorders, urinary tract diseases and gastrointestinal conditions. Described in this paper are the currently available techniques of urine sample analysis as well...
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Influence of geotechnical conditions on damage states of Gdansk Bay Coast cliff formations
PublikacjaA geotechnical aspect of destruction processes of seashores was identified based on the case of erosion of Gdansk Bay Coast cliff formations. Causative factors of landslide were described in the context of natural phenomena, land development and its anthropogenic transformations. Possible directions of theoretical analysis of changes in groundwater relations were indicated.
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Applications of Alkanethiols in Organic Synthesis
PublikacjaThis manuscript is an update to the earlier Science of Synthesis contribution describing methods for the synthesis of alkanethiols. Thiols can be converted into sulfonic, sulfinic, sulfenic acid and their derivatives, sulfides, disulfides, polysulfides, sulfonium salts, and thiiranes, etc. These transformations are accomplished by nucleophilic displacement or addition, oxidation, condensation, or coupling reactions involving thiol...
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System of breath collection and analysis for diseases detection
PublikacjaCollection and study of composition of the exhaled air is now intensively investigated to develop non-invasive medical diagnostics based on presence of metabolic compounds in the exhaled air. The process of collecting and processing of the exhaled air must fulfill relevant conditions to achieve satisfactory results. The paper presents the system of collecting samples of exhaled breath and the proposed methods of its analysis, using...
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The role and scope of architectural and conservation research procedures in the process of restoring the splendour of an architectural monument created after 1945 on the example of the Suburban Railway Station in Gdynia
PublikacjaModern Movement buildings, despite their relatively recent construction, are sometimes affected by radical transformations of layout and form. The railway stations being one of the most important public buildings in the city are a special group of them. Due to long-term and intensive use they may bear the signs of exploitation of parts of its substance and have secondary transformations disharmony with the building. The subject...
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Acyl Meldrum's acid derivatives: application in organic synthesis
PublikacjaThis review is focused on one of the most important classes of Meldrum's acid derivatives commonly known as acyl Meldrum's acids. The preparation methods of these compounds are considered including the recently proposed and rather rarely used ones. The chemical properties of acyl Meldrum's acids are described in detail, including thermal stability and reactions with various nucleiophiles. The possible mechanisms of these transformations...
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Application, design and operation of constructed wetland systems: case studies of systems in the Gdańsk region, Poland
PublikacjaDifferences in operation result from physical, chemical and biological conditions, which directly influence transformations in the whole aquatic-matrix-plants environment. Depending on the quantity of inflowing organic matter load and the rate of biochemical processes, the contaminations could be removed or/and retuned in the system. From this point of view the facility should be designed and operated in such way that the highest...
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Instrumental techniques used in the analysis of exhaled air
PublikacjaExhaled air composition changes depending on the health status of the patient, making it possible to use breath analysis for diagnosis and monitoring purposes. Despite the fact that it is not yet used in every day medical practice, it potential application could facilitate the diagnostics of various diseases such as metabolic disorders, respiratory tract and gastrointestinal diseases. Described in this paper are different application...
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Transforming the Gdansk Bay Area
PublikacjaThe political transformation of Poland in the early nineties from a centrally steered economy to a free market economy entailed changes of the spatial planning system. The impact of these changes on the spatial transformations and current shape of urban structures in the Gdansk Bay Metropolitan Area is apparent and significant. The paper concentrates on the present spatial phenomena of Gdansk Agglomeration resulting from the main...
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Effect of long term service at elevated temperatures on mechanical properties of Manaurite XM reformer tubes
PublikacjaMicrostructure transformations occur in the Manaurite XM cast steel tubes during long-term operation in the reformer furnace were revealed and described. The rela tionship between mechanical properties, an increase of internal diameter of the tube and microstructure degradation is discussed. Static tensile test was performed on two types of samples with different shapes. It has been shown differences in the results of tests...
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Cardinal regenerative features of the MRL mouse
PublikacjaIn this review, we discuss recent studies relating to major features of adult MRL mouse biology that contribute to the regenerative responses seen. These include an increased inflammatory cell profile, a unique glycolytic metabolic state typically found during embryogenesis, and a cell cycle phenotype of DNA damage and G2/M arrest. These traits have been found in other mammalian and non-mammalian regenerative systems. How these...
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A method of self-testing of an analog circuit terminated by an ADC in electronic embedded systems controlled by microcontrollers
PublikacjaA new self-testing method of analog parts terminated by an ADC in electronic embedded systems controlled by microcontrollers is presented. It is based on a new fault diagnosis method based on on-line (i.e. during measurement), transformations of voltage samples of the time response of a tested part to a square pulse - onto localization curves placed in the measurement space. The method can be used for fault detection and single...
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The Effect of Long Term Service at Elevated Temperatures on Microstructure Degradation of Austenitic Reformer Tubes
PublikacjaThe paper analyses the relationship between an increase of the inner diameter of tubes made of Manaurite XM cast steel and transformations occurring in their microstructure due to long-lasting operation in methane reformer. Examinations included metallographic analysis with light microscope (LM), scanning electron microscope (SEM) and microanalysis of the chemical composition of precipitates (EDX). It was indicated that there is...
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Biotransformation of abused synthetic cannabinoids, JWH-018 and JWH-073, by human cytochromes P450 and UDP-glucuronosyltransferases
PublikacjaZwiązki oznaczone symbolami JWH-018 i JWH-073 są syntetycznymi pochodnymi kanabinoidów, obecnymi w preparatach o działaniu psychoaktywnym (K2/Spice). Wcześniejsze badań wykazały, że u osób przyjmujących tzw. ''legalną marihuanę'', głównymi produktami biotransformacji obecnymi w moczu były hydroksylowe pochodne obu związków, jak również ich glukuronidy. W związku z tym celem prowadzonych badań było określenie roli poszczególnych...
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The Imidazoacridinone Antitumor Drug, C-1311, Is Metabolized by Flavin Monooxygenases but Not by Cytochrome P450s.
PublikacjaPrezentowane w publikacji wyniki badań mają na celu wyjaśnienie roli enzymów wątrobowych w metabolizmie przeciwnowotworowych pochodnych C-1311 oraz C-1330. Oba związki inkubowane były z frakcją mikrosomalną oraz enzymami rekombinantowymi należącymi do grypy cytochromu P450, FMO oraz UGT. Badania wykazały, że oba związki są metabolizowane przez enzymy frakcji mikrosomalnej, ale nie przez enzymy cytochromu P450. Aktywność enzymatyczna...
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Alkanethiolates of Group 1,2, and 13-15 Metals
PublikacjaThis manuscript is an update to the earlier Science of Synthesis contribution describing methods for the synthesis of alkanethiolates of group 1, 2, and 13-15 metals. Alkanethiolates can be converted into S-alkyl thiocarboxylic acid esters, 1-thioglycosides, S-alkyl thiosulfinates, tetrahydro-1,4-thiazine-3-ones, sulfides, disulfides, sulfonium salts, dithioacetals and dithioketals, etc. These transformations are accomplished by...
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Quadratic Cohen representations in spectral analysis of serration process in Al–Mg alloys
PublikacjaImportant from mechanical point of view the Portevin–Le Chatelier serration phenomenon is being characterized by a complicated spectral profile. As a typical example of nonstationary processes it demands a special treatment allowing to follow the evolution of energy of stress fluctuations as a function of strain. The authors suggest the utilization of a compact system of quadratic transformations, known as Cohen class, as a technique...
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On Dynamic Extension of a Local Material Symmetry Group for Micropolar Media
PublikacjaFor micropolar media we present a new definition of the local material symmetry group considering invariant properties of the both kinetic energy and strain energy density under changes of a reference placement. Unlike simple (Cauchy) materials, micropolar media can be characterized through two kinematically independent fields, that are translation vector and orthogonal microrotation tensor. In other words, in micropolar continua...
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Effect of crystallization process at cryogenic conditions on the functional properties of the SUPERSTON alloy used in production the ship's propellers
PublikacjaThe purpose of this paper is to show results of laser treatment at cryogenic conditions of the SUPERSTON alloy used for ship's propellers. That modification process ought to bring beneficial changes of microstructure and residual stresses in the surface layer. During the laser remelting at cryogenic conditions the microstructure changes significantly. This is related to synergistic effects of the solidification rate, phase transformations...
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Spike patterns and chaos in a map-based neuron model
PublikacjaThe work studies the well-known map-based model of neuronal dynamics introduced in 2007 by Courbage, Nekorkin and Vdovin, important due to various medical applications. We also review and extend some of the existing results concerning β-transformations and (expanding) Lorenz mappings. Then we apply them for deducing important properties of spike-trains generated by the CNV model and explain their implications for neuron behaviour....
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Landscape as a Potential Key Concept in Urban Environmental Planning: The Case of Poland
PublikacjaRapid urban development increases the consumption of materials, energy, and water, resulting in an overproduction of waste and emissions. These cause many environmental threats, such as ozone layer depletion and rain acidification, leading to climate change. Therefore, the question arises on how to improve the effectiveness of tools that strengthen environmental protection. This discursive article presents an approach stressing...
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Multiscalar Model Based Control Systems for AC Machines
PublikacjaContents of the Chapter: Nonlinear transformations and feedback linearization. Models of the squirrel cage induction machine: Vector model of the squirrel cage induction machine. Multiscalar models of the squirrel cage induction machine.Feedback linearization of multiscalar models of the induction motor.Models of the double fed induction machine: Vector model of the double fed induction machine. Multiscalar model of the...
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Superconducting properties of vn-sio 2 sol-gel derived thin films
Publikacjain this work studies of structure and superconducting properties of vnsio2 films are reported. the films were obtained through thermal nitridation (ammonolysis) of solgel derived v2o3sio2 coatings (in a proper v2o3/sio2 ratio) at 1200 ◦c. this process leads to the formation of disordered structure with vn metallic grains dispersed in the insulating sio2 matrix. the structural transformations occurring in the lms as a result...
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Invariant Measures for Uncountable Random Interval Homeomorphisms
PublikacjaA necessary and sufficient condition for the iterated function system { f (·, ω) | ω ∈ } with probability P to have exactly one invariant measure μ∗ with μ∗((0, 1)) = 1 is given. The main novelty lies in the fact that we only require the transformations f (·, ω) to be increasing homeomorphims, without any smoothness condition, nei- ther we impose conditions on the cardinality of . In particular, positive Lyapunov exponents conditions...
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Design, synthesis, and molecular docking of new 5-HT reuptake inhibitors based on modified 1,2-dihydrocyclopenta[b] indol-3(4H)-one scaffold
PublikacjaA new group of serotonin reuptake inhibitors containing 1,2-dihydrocyclopenta[b]indol-3(4H)-one scaffoldwas synthesized, starting from indole 5-((1H-indol-3-yl)(1,3-dioxane-4,6-diones as a key intermediates. Following three transformations including intramolecular cyclization and formation of imines, a series of new ligand for human serotonin transporter was obtained. The ability of these ligands to inhibit human TS3 serotonin transporter...
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Rola przekształceń styku lądu i wody w procesach rewitalizacji
PublikacjaArtykuł poświęcony jest zweryfikowaniu roli, jaką pełnią przekształcenia granic miedzy lądem i wodą w procesach rewitalizacji. Analizując szereg tego typu działań, w szczególności dotyczących transformacji obszarów poprzemysłowych, można zauważyć, że w ostatnim czasie charakterystyczne dla nich stają się modyfikacje planów obszarów wodnych i form ich granic. Jak okazuje się, działania takie mają nie tylko znaczenie kompozycyjne...
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Bioactive Ingredients with Health-Promoting Properties of Strawberry Fruit (Fragaria x ananassa Duchesne)
PublikacjaStrawberries (Fragaria x ananassa Duchesne) belong to the berry group and are characterized primarily by delightful sensory properties. Due to their chemical composition, these fruits are a rich source of bioactive compounds that can modify the metabolic and physiological functions of the body. The aim of this work is to present the current state of research on bioactive ingredients found in these fruits in the context of their...
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Retained features of embryonic metabolism in the adult MRL mouse
PublikacjaThe MRL mouse is an inbred laboratory strain that was derived by selective breeding in 1960 from the rapidly growing LG/J (Large) strain. MRL mice grow to nearly twice the size of other commonly used mouse strains, display uncommonly robust healing and regeneration properties, and express later onset autoimmune traits similar to Systemic Lupus Erythematosis. The regeneration trait (heal) in the MRL mouse maps to 14-20 quantitative...
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Adipokine and cytokine levels in patients with adrenocortical cancer, subclinical Cushing's syndrome and healthy controls
PublikacjaIntroduction In recent years researchers have focused at hormonal activity in Cushing’s syndrome (CS) in connection with metabolic disorders and the role of adipokines and cytokines secreted by the adipose tissue. The aim of the study was to investigate levels of adipokines and cytokines in patients with: subclinical CS (SCS) – in relation to hormonal parameters of hypercortisolemia, and, adrenocortical cancer (ACC). Materials...
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Endoscopy video analysis algorithms and their independence of rotation , brightness , contrast , color and blur
PublikacjaThe article presents selected image analysis algorithms for endoscopy videos. Mathematical methods that are part of these algorithms are described, and authors’ claims about the characteristics of these algorithms, such as the independence of rotation, brightness, contrast, etc. are mentioned. Using the common test on the real endoscopic image database and a set of image transformations, the validity of these claims was checked...
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Company versus consumer performance: does brand community identification foster brand loyalty and the consumer’s personal brand?
PublikacjaThis study investigates the effect of community identification in building brand loyalty (attitudinal and behavioural) and a personal brand via social networks. The proposed model explained the main community identification antecedents and how identification can lead to enhanced company and consumer performance. This study adopts the theoretical lens of uses and gratifications theory and identifies three motivational drivers of...
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Investigation of the Combustion Processes in the Gas Turbine Module of an FPSO Operating on Associated Gas Conversion Products
PublikacjaIn this paper, we consider the issue of thermo-chemical heat recovery of waste heat from gas turbine engines for the steam conversion of associated gas for offshore vessels. Current trends in the development of offshore infrastructure are identified, and the composition of power plants for mobile offshore drilling units and FPSO vessels is analyzed. We present the results of a comparison of power-to-volume ratio, power-to-weight...
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RE-SHAPING THE LAND AND WATER CONNECTIONS AND ITS ROLE IN ACHIEVING LANDSCAPE AND ECOLOGICAL SYSTEMS’ CONTINUITY ON THE POST-INDUSTRIAL TERRITORIES
PublikacjaThis paper delves into recently applied strategies of creating new water areas and modifying the existing ones as a part of the transformation processes of post-industrial territories. It proves that while the pursuit for unique architectural and urban space values remains an important factor contributing to such modifications, they may also play an important role in reclaiming ecological systems continuity. On the basis of theoretical...