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Metabolic transformation of antitumor acridinone C-1305 but not C-1311 via selective cellular expression of UGT1A10 increases cytotoxic response: implications for clinical use.
PublicationThe acridinone derivates C-1305 and C-1311 are promising antitumor agents with high activity against several experimental cellular and tumor models and which are under evaluation in pre-clinical and early phase clinical trials. Recent evidence from our laboratories has indicated that both compounds were conjugated by several UGT isoforms with the most active being extrahepatic UGT1A10. The present studies were designed to test...
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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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Steroid Sulfatase Inhibitors Based on Phosphate and Thiophosphate Flavone Analogs
PublicationA series of phosphate and thiophosphate flavone derivatives were synthesized and biologically evaluated in vitro for inhibition of steroid sulfatase (STS) activity. The described synthesis includes the straightforward preparation of 7-hydroxy-2-phenyl-4H-chromen-4-one 3a, 2-(4-fluorophenyl)-7-hydroxy-4H-chromen-4-one 3b, 7-hydroxy-2-(4-(trifluoromethyl)phenyl)-4H-chromen-4-one 3c, 7-hydroxy-2-(p-tolyl)-4H-chromen-4-one 3d modified...
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Acridinone antitumor agents: C-1311, C-1330 and C-1305 are metabolized by flavin-containing monooxygenase isoenzymes: FMO1, FMO3 and FMO5 with different rates
PublicationRekombinantowe ludzkie monooksygenazy flawinowe: FMO1, FMO3, FMO5 indukują przemiany metaboliczne wybranych do badań pochodnych akrydonu. Biotransformacja związków C-1311, C-1330 i C-1305 przez FMO prowadzi do jednego produktu o strukturze N-tlenku. Wyniki badań wskazują, że najbardziej podatna na przemiany wobec FMO jest pochodna triazoloakrydonu C-1305. Wydaje się więc, że głównymi enzymami pierwszej fazy przemian metabolicznych...
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Genotoxicity of selected pharmaceuticals, their binary mixtures, and varying environmental conditions – study with human adenocarcinoma cancer HT29 cell line
PublicationPharmaceutical residues are present in the environment in mixtures and their adverse effects may also result from interactions that occur between compounds. Studies presented in this work focus on genotoxicity of pharmaceuticals from different therapeutic groups in mixtures and in individual solutions impacted with different environmental conditions assessed using comet assay (alkaline approach). Binary mixtures of pharmaceuticals...
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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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The role of intestine and liver in glucuronidation of the imidazo- and triazoloacridinone antitumor agents, C-1311 and C-1305: High affinity substrates for UGT1A10
PublicationCelem przeprowadzonych badań było określenie roli poszczególnych izoform UDP-glukuronylotransferazy (UGT)oraz mikrosomów jelita(HIM)i wątroby (HLM) wyizolowanych od różnych pacjentów w metabolizmie pochodnych akrydonu, związków C-1311 i C-1305. Wykazano, że rodziną UGT katalizującą przemiany C-1305 i C-1311 jest UGT1A, z najwyższą aktywnością wykazywaną przez pozawątrobowy izoenzym UGT1A10. Rozkład aktywności frakcji mikrosomalnych...
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Biotransformation of abused synthetic cannabinoids, JWH-018 and JWH-073, by human cytochromes P450 and UDP-glucuronosyltransferases
PublicationZwiązki 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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In silico design of telomerase inhibitors.
PublicationTelomerase is a reverse transcriptase enzyme involved in DNA synthesis at the end of linear chromosomes. Unlike in most other cells, telomerase is reactivated most cancerous cells and, therefore, has become a promising new anticancer target. Despite extensive research, direct telomerase inhibitors have yet not been introduced to the clinics because of the complexity of this enzyme. Structures of this protein from simple organisms...
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Human carnosinases: A brief history, medicinal relevance, and in silico analyses
PublicationCarnosine, an endogenous dipeptide, has been found to have a plethora of medicinal properties, such as antioxidant, antiageing, and chelating effects, but with one downside: a short half-life. Carnosinases and two hydrolytic enzymes, which remain enigmatic, are responsible for these features. Hence, here we emphasize why research is valuable for better understanding crucial concepts like ageing, neurodegradation, and cancerogenesis,...
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Targeting shelterin proteins for cancer therapy.
PublicationAs a global health challenge, cancer prompts continuous exploration for innovative therapies that are also based on new targets. One promising avenue is targeting the shelterin protein complex, a safeguard for telomeres crucial in preventing DNA damage. The role of shelterin in modulating ataxia- telangiectasia mutated (ATM) and ataxia-telangiectasia and Rad3-related (ATR) kinases, key players in the DNA damage response (DDR),...
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Information technology assessment using a functional prototype of the agent based system
PublicationIn the paper authors present the progress of works related with the agent-based system serving the purpose of information technology assessment. Currently this is a prototype including agents, the knowledge base and the ontology; the domain incorporated by the assessment-enterprise managing technologies with special attention paid to technologies directed to IT projects. In this paper, besides indication of expected functionalities...
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Big Data from Sensor Network via Internet of Things to Edge Deep Learning for Smart City
PublicationData from a physical world is sampled by sensor networks, and then streams of Big Data are sent to cloud hosts to support decision making by deep learning software. In a smart city, some tasks may be assigned to smart devices of the Internet of Things for performing edge computing. Besides, a part of workload of calculations can be transferred to the cloud hosts. This paper proposes benchmarks for division tasks between an edge...
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Investigation of long-range dependencies in the stochastic part of daily GPS solutions
PublicationThe long-range dependence (LRD) of the stochastic part of GPS-derived topocentric coordinates change (North, East, Up) results with relatively high autocorrelation values with a focus on self-similarity. One of the reasons for such self-similarity in the GPS time series are noises that are commonly recognised to prevail in the form of the flicker noise model. To prove the self-similarity of the stochastic part of GPS time series...
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Algorithms of chemicals detection using raman spectra
PublicationRaman spectrometers are devices which enable fast and non-contact identification of examined chemicals. These devices utilize the Raman phenomenon to identify unknown and often illicit chemicals (e.g. drugs, explosives)without the necessity of their preparation. Now, Raman devices can be portable and therefore can be more widely used to improve security at public places. Unfortunately, Raman spectra measurements is a challenge...
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A novel methodology for the enantiomeric resolution of methamphetamine, its precursors and intermediates by GC-MS
PublicationImpurity profiling and classification of abused drugs using chiral analytical techniques is of particular interest and importance because of the additional information obtained from this approach. When these methods are applied to the synthesis of illicitly used substances, they can supply valuable information about the conditions/chemicals used in the synthesis. In this study, simultaneous chiral separation of methylamphetamine,...
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Specific Binding of Cholesterol to the Amyloid Precursor Protein: Structure of the Complex and Driving Forces Characterized in Molecular Detail
PublicationC99 is the C-terminal membrane-bound fragment of the amyloid precursor protein that is cleaved by γ-secretase to release Aβ peptides, the hallmark of Alzheimer’s disease (AD). Specific interactions of C99 with cholesterol have been proposed to underlie the recognized role of cholesterol in promoting amyloidogenesis. By using molecular dynamics simulations, we studied cholesterol binding to C99 in a lipid bilayer. We determined...
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Meconium analysis as a promising diagnostic tool for monitoring fetal exposure to toxic substances: Recent trends and perspectives
PublicationPrenatal exposure to toxic substances is an important public health problem. Many biological specimens obtained from the fetus or mother are used for biomonitoring. Each material reflects exposure in a specific time period and has different advantages and disadvantages in terms of accuracy, time window of detection and cost/benefit ratio. Recently, meconium has become the matrix of choice in toxicology screening for detecting exposure...
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Amino Acid and Peptide‐Based Antiviral Agents
PublicationA significant number of antiviral agents used in clinical practice are amino acids, short peptides, or peptidomimetics. Among them, several HIV protease inhibitors (e. g. lopinavir, atazanavir), HCV protease inhibitors (e. g. grazoprevir, glecaprevir), and HCV NS5A protein inhibitors have contributed to a significant decrease in mortality from AIDS and hepatitis. However, there is an ongoing need for the discovery of new antiviral...
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Molecular Imaging and Nanotechnology—Emerging Tools in Diagnostics and Therapy
PublicationPersonalized medicine is emerging as a new goal in the diagnosis and treatment of diseases. This approach aims to establish differences between patients suffering from the same disease, which allows to choose the most effective treatment. Molecular imaging (MI) enables advanced insight into molecule interactions and disease pathology, improving the process of diagnosis and therapy and, for that reason, plays a crucial role in personalized...
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Methods of Network Resource Provisioning for the Future Internet IIP Initiative
PublicationIn this paper, we present specification, design and implementation aspects of a network resource provisioning module introduced for the Polish Initiative of Future Internet called System IIP. In particular, we propose a set of novel LP optimization models of network resource provisioning designed to minimize the network resource consumption, either bandwidth or node’s computational power, as well as to maximize the residual capacity....
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Vapor correction of FTIR spectra – A simple automatic least squares approach
PublicationFTIR spectroscopy is one of the best techniques to study intermolecular interactions. However, such an application requires high quality spectra with as little noise as possible, which are often difficult to obtain. One of the main sources of unwanted interference is water vapor. Here a robust method is proposed for automatic, fast and reliable vapor correction of FTIR spectra. The presented least squares approach of vapor subtraction...
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A method of earth fault loop impedance measurement without unwanted tripping of RCDs
PublicationIn low-voltage networks, earth fault loop impedance (EFLI) measurement is the basis for assessing the effectiveness of automatic disconnection of supply. Such a measurement is performed during initial and periodical verification, especially in a TN low-voltage network. Nowadays, due to widespread application of residual current devices (RCDs), such test is difficult in many circuits because RCDs operate during the test. In this...
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One-step recovery of REE oxalates in electro-leaching of spent NdFeB magnets
PublicationRecovery of rare-earth elements (REEs) from spent NdFeB magnets is receiving great attention because of high amount of neodymium and potential risk of environmental pollution. In this study, a novel environment-friendly hydrometallurgical route is proposed for efficient recovery of REEs during electrochemical leaching with sulfuric and oxalic acids. With proper adjustment of the electrolyte composition and operating conditions,...
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The biological role of prolyl oligopeptidase and the procognitive potential of its peptidic inhibitors from food proteins
PublicationProlyl oligopeptidase (POP) is a conserved serine protease belonging to proline-specific peptidases. It has both enzymatic and non-enzymatic activity and is involved in numerous biological processes in the human body, playing a role in e.g., cellular growth and differentiation, inflammation, as well as the development of some neurodegenerative and neuropsychiatric disorders. This article describes the physiological and pathological...
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Sondowanie statyczne : Metody i zastosowanie w geoinżynierii.
PublicationKsiążka stanowi pierwsze polskie kompendium nt. sondowań statycznych metodą CPTU. Przedstawiono w niej problematykę sondowania w dwóch częściach: numerycznej i praktycznej. W części pierwszej autor zwraca uwagę na złożoność obliczeniową omawianych zagadnień, porusza kwestie zaawansowanej mechaniki obliczeniowej. Druga część zawiera wiele praktycznych wskazówek jak korzystać z metody CPTU i jak interpretować jej wyniki w celu określenia...
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Instytucjonalny kontekst intencji rozwojowych przedsiębiorstw na Pomorzu
PublicationLiteratura dotycząca wzrostu małych firm podkreśla wagę kontekstu instytucjonalnego w tworzeniu warunków ich wzrostu. Mówiąc o instytucjach należy odróżniać zarówno aspekt obiektywny jak i subiektywny. Artykuł porusza oba aspekty: jakość instytucji jak i ich postrzeganie przez przedsiębiorców. Ten drugi aspekt został opisany w oparciu o wyniki badań Pomorskiego Obserwatorium Gospodarczego. W konkluzji zawarto wniosek iż postrzeganie...
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Parallel processing of multimedia streams
PublicationW artykule zaprezentowana jest nowa biblioteka wspierającą tworzenie zadań obliczeniowych, część platformy KASKADA.Przedstawiony został projekt biblioteki, uwzględniający diagram głównych klas oraz diagram sekwencji. Drugi z diagramów ukazuje współpracę głównych klas w procesie przetwarzania strumieni multimedialnych. W dalszej częsci omówione zostały szczegły mechanizmu komunikacji międzyzadawniowej oraz przedstawiony został graf...
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Przewidywanie poziomu zaburzeń elektromagnetycznych w przekształtnikach energoelektroncznych
PublicationArtykuł opisuje dwie metody przewidywania zaburzeń elektromagnetycznych przewodzonych generowanych w przekształtnikach energoelektronicznych. W pierwszej metodzie zastosowano symulacje komputerową wykorzystując dokładne modele wszystkich elementów układu tj. urządzeń półprzewodnikowych, elementów pasywnych i pomiarowych oraz ścieżek przewodzących. Jako drugą metodę, zastosowano filtracje Wienera opartą na cyfrowym przetwarzaniu...
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Działalność w obszarze grantów realizowana przez Katedrę Sieci Teleinformacyjnych
PublicationPrzedstawiono działalność Katedry Sieci Teleinformacyjnych PG WETI w obszarze grantów finansowanych przez instytucje centralne, przy czym główny nacisk położono na scharakteryzowanie aktualnie realizowanych projektów. Opisano dwa projekty finansowane przez NCBiR. Pierwszy dotyczy koncepcji oraz implementacji integracji informacji w rozproszonych elementach systemu wymiany danych Straży Granicznej, natomiast drugi strumieniowej...
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Wzmacnianie gruntu in situ metodą wgłębnego mieszania i wykorzystanie cemento gruntu
PublicationOpisano zasady wykonywania mieszania wgłębnego gruntu przy zastosowaniu suchych spoiw oraz zaczynu cementowego. Pierwszy sposób, określany jako metoda mieszania na sucho, zastosowano w Polsce m.in. do posadowienia nasypów drogowych w ramach budowy przeprawy mostowej przez Regalicę. Drugi sposób, określany jako mieszanie na mokro, zastosowano m.in. do wzmocnienia gruntów pod Trasą Zieloną w Lublinie oraz do wykonania uszczelnień...
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Zakres stabilnej pracy silnika indukcyjnego z obserwatorem prędkości kątowej wału wyznaczony za pomocą drugioej metody Lapunowa.
PublicationZamieszczono analizę stabilności układu regulacji silnika indukcyjnego z obserwatorem prędkości kątowej wału w oparciu o drugą metodę Lapunowa. Na podstawie modelu matematycznego układu silnika z obserwatorem wyznaczono funkcję Lapunowa oraz udowodniono warunki jej poprawności. Dokonano analizy lokalnej dla małych prędkości oraz częściowej analizy globalnej rozważanego układu. Wyniki potwierdzono w symulacji komputerowej z zastosowaniem...
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ASIC Design Example of Complex SoC with FPGA Prototyping
PublicationThe paper presents an example of the System on a Chip design, where the FPGA prototyping has been used. Two FPGA prototypes have been realized. The first FPGA prototype uses AVNET board containing Xilinx Virtex4 device accompanied by custom board with required devices. The second FPGA prototype has been built using the custom PCB with Xilinx Virtex-4 XC4VLX60 FPGA accompanied by all needed external components. The final system...
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Implementation of Non-Probabilistic Methods for Stability Analysis of Nonlocal Beam with Structural Uncertainties
PublicationIn this study, a non-probabilistic approach based Navier’s Method (NM) and Galerkin Weighted Residual Method (GWRM) in term of double parametric form has been proposed to investigate the buckling behavior of Euler-Bernoulli nonlocal beam under the framework of the Eringen's nonlocal elasticity theory, considering the structural parameters as imprecise or uncertain. The uncertainties in Young’s modulus and diameter of the beam are...
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Membrane separation processes for the extraction and purification of steviol glycosides: an overview
PublicationSteviol glycosides (SGs), as natural sweeteners from Stevia rebaudiana, are currently employed for replacing sugar and its derivatives in several food products and formulations. Such compounds play an essential role in human health. Their usage provides a positive effect on preventing diseases related to sugar consumption, including diabetes mellitus, cancer, and lipid metabolism disorders. The traditional extraction of SGs is...
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Fast method for IEEE 802.16-2004 standard-based networks coverage measuring
PublicationThis paper presents the time and cost efficient method for measuring effective coverage of IEEE 802.16-2004 standard-based networks. This is done by performing a series of continuous measurements on the grid basis. Due to this kind of signal quality surveying, estimationof the probable coverage area can be made. It is significant that themethod is fast and is uses a standard customer equipment which makes it more accessible for...
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On constitutive modeling for technical woven fabric
PublicationW pracy przestawiono kilka modeli konstytutywnych przyjmowanych do opisu zachowania się tkanin technicznych. Oprócz modeli zaczerpniętych z literatury autorzy prezentują własną koncepcje modelu stanowiąca rozszerzenie modelu sieci gęstej.This paper describes several types of the constitutive models used for the technical woven fabric description. Besides of the literatures examples of the constitutive models, the authors presented...
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Data regarding a new, vector-enzymatic DNA fragment amplification-expression technology for the construction of artificial, concatemeric DNA, RNA and proteins, as well as biological effects of selected polypeptides obtained using this method
PublicationApplications of bioactive peptides and polypeptides are emerging in areas such as drug development and drug delivery systems. These compounds are bioactive, biocompatible and represent a wide range of chemical properties, enabling further adjustments of obtained biomaterials. However, delivering large quantities of peptide derivatives is still challenging. Several methods have been developed for the production of concatemers –...
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Ipertrofan Revisited—The Proposal of the Complete Stereochemistry of Mepartricin A and B
PublicationBeing a methyl ester of partricin, the mepartricin complex is the active substance of a drug called Ipertrofan (Tricandil), which was proven to be useful in treatment of benign prostatic hyperplasia and chronic nonbacterial prostatitis/chronic pelvic pain syndrome. Nevertheless, no direct structural evidence on the stereochemistry of its components has been presented to date. In this contribution, we have conducted detailed, NMR-driven...
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Waterborne polyesters partially based on renewable resources
PublicationA new experimental approach for preparing biobased, water-soluble polyesters via titanium(IV) n-butoxide-catalyzed bulk polycondensation is presented. In the described method polymers were obtained from isosorbide, maleic anhydride and poly(ethylene glycol). The chemical structure of the synthesized polyesters was confirmed using 2D NMR spectroscopy and by titration methods. Careful analysis of 2D NMR spectra viz. Correlation Spectra...
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Review of the determination of modern used pesticides in water samples
PublicationThe increasingly widespread application of pesticides causes that larger amounts of them are entering the environment. Their presence in sources of drinking water, essential to life, is a particular danger. For these reasons it is important to monitor and analyse pesticide residues in the environment. The analysis of environmental samples for the presence of pesticides is very difficult. Firstly, the processes involved in sample...
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Key issues in modeling and optimization of lignocellulosic biomass fermentative conversion to gaseous biofuels
PublicationThe industrial-scale production of lignocellulosic-based biofuels from biomass is expected to benefit society and the environment. The main pathways of residues processing include advanced hydrolysis and fermentation, pyrolysis, gasification, chemical synthesis and biological processes. The products of such treatment are second generation biofuels. The degree of fermentation of organic substances depends primarily on their composition...
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A Data Driven Model for Predicting RNA-Protein Interactions based on Gradient Boosting Machine
PublicationRNA protein interactions (RPI) play a pivotal role in the regulation of various biological processes. Experimental validation of RPI has been time-consuming, paving the way for computational prediction methods. The major limiting factor of these methods has been the accuracy and confidence of the predictions, and our in-house experiments show that they fail to accurately predict RPI involving short RNA sequences such as TERRA RNA....
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Novel, Fully Biobased Semicrystalline Polyamides
PublicationNovel, semicrystalline polyamides and co(polyamides) were synthesized from biobased sebacic acid (SA), 2,5-diamino-2,5-dideoxy-1,4;3,6-dianhydroiditol (diaminoisoidide, DAII) as well as from 1,4-diaminobutane (DAB), also known as putrescine in nature. Low molecular weight polyamides were obtained by melt polycondensation of the salts based on these monomers or by interfacial polycondensation. In order to increase their molecular...
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Modifications to the anaerobic digestion model no. 1 (ADM1) for enhanced understanding and application of the anaerobic treatment processes – A comprehensive review
PublicationAnaerobic digestion (AD) is a promising method for the recovery of resources and energy from organic wastes. Correspondingly, AD modelling has also been developed in recent years. The International Water Association (IWA) Anaerobic Digestion Model No. 1 (ADM1) is currently the most commonly used structured AD model. However, as substrates become more complex and our understanding of the AD mechanism grows, both systematic and specific...
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Wielopoziomowy system diagnostyki konstrukcji. Badania eksperymentalne na płycie stalowej
PublicationCelem pracy jest zweryfikowanie przydatności systemu wykrywania uszkodzeń bazującego na sieciach neuronowych i testach dynamicznych. Analizowanie są dwa poziomy dynamicznego badania konstrukcji. Pierwszy poziom zakłada wykorzystanie drgań środowiskowych, zaś drugi wykorzystuje drgania wywołane siłami o znanych amplitudach i ma na celu szczegółową ocenę stalowej płyty. Uszkodzenie symulowano przez umieszczenie dodatkowej masy w...
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Antena mikropaskowa o poszerzonym paśmie pracy
PublicationW pracy przedstawiono wyniki badań dotyczące anteny mikropaskowej o poszerzonym paśmie pracy. Poprzez zastosowanie układu dwóch szczelin sprzęgających we wspólnej warstwie masy uzyskano 29% pasmo pracy (0.96GHz -1.25 GHz) mierzone przy poziomie WFS < 1.5. Ze względu na obserwowane w charakterystyce promieniowania minima, wykonano drugą wersję anteny ze zmodyfikowanymi wymiarami warstwy masy. Efektemtego zabiegu było uzyskanie anteny...
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Podatki w Polsce : zarys wykładu
PublicationMonografia zawiera X rozdziałów Pierwsza częśc zawiera charakterystykę i ocenę polskiego systemu podatkowego, zagadnienia rejestracji i ewidencji podatkowych, wybrane problemy wspólpracy podatkowej z krajami UE, oraz elementy kształtujące odpowiedzialność karną skarbową. Druga cześć poświęcona jest przedstawieniu zródeł prawa podatkowego w Polsce omówieniu istoty i konstrukcji zobowiązań podatkowych, zasad postepowania podatkowego...
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Experimental study on earthquake-induced pounding between structural elements made of different building materials
PublicationCelem artykułu jest pokazanie wyników dwóch eksperymentów dotyczących zderzeń pomiędzy elementami wykonanymi z różnych materiałów budowlanych, takich jak: stal, beton, drewno i ceramika. Pierwszy z nich polegał na zrzucaniu kul na płaską powierzchnię, drugi dotyczył zderzeń modeli konstrukcji poddanych wymuszeniom sejsmicznym na stole wstrząsowym. Wyniki testów pokazują, iż wpływ materiału elementów kolidujących ze sobą na zachowanie...
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Modele i metody kolorowania grafów. Część II
PublicationNiniejszy artykuł jest drugą częścią 2-odcinkowego cyklu przeglądowego na temat modeli i metod kolorowania grafów. Przedstawiono w nim najważniejsze, z punktu widzenia zastosowań, modele kolorowania grafów. W szczególności pokazano różne kryteria i ograniczenia modyfikujące kolorowanie klasyczne. Ponieważ kolorowanie we wszystkich tych odmianach i wariantach jest NP-trudne, podano oszacowania na liczbę chromatyczną (indeks chromatyczny)...