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Search results for: drug screening platform
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CYP3A4-dependent cellular response does not relate to CYP3A4-catalysed metabolites of C-1748 and C-1305 acridine antitumor agents in HepG2 cells
PublicationHigh CYP3A4 expression sensitizes tumor cells to certain antitumor agents while for others it can lower their therapeutic ef fi cacy. We have elucidated the in fl uence of CYP3A4 overexpression on the cellular response induced by antitumor acridine derivatives, C-1305 and C-1748, in two hepatocellular carcinoma (HepG2) cell lines, Hep3A4 stably transfected with CYP3A4 isoenzyme, and HepC34 expressing empty vector. The compounds...
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Natural Deep Eutectic Solvents as Agents for Improving Solubility, Stability and Delivery of Curcumin
PublicationPurpose Study on curcumin dissolved in natural deep eutectic solvents (NADES) was aimed at exploiting their beneficial properties as drug carriers. Methods The concentration of dissolved curcumin in NADES was measured. Simulated gastrointestinal fluids were used to determine the concentration of curcumin and quantum chemistry computations were performed for clarifying the origin of curcumin solubility enhancement in NADES. Results NADES...
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The Substantial Improvement of Amphotericin B Selective Toxicity Upon Modification of Mycosamine with Bulky Substituents
PublicationAbstract: Background: It is assumed that the unfavorable selective toxicity of an antifungal drug Amphotericin B (AmB) can be improved upon chemical modification of the antibiotic molecule. Objective: The aim of this study was verification of the hypothesis that introduction of bulky substituents at the amino sugar moiety of the antibiotic may result in diminishment of mammalian vitro toxicity of thus prepared AmB derivatives. Methods:...
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Nanoparticles: Taking a Unique Position in Medicine
PublicationThe human nature of curiosity, wonder, and ingenuity date back to the age of humankind. In parallel with our history of civilization, interest in scientific approaches to unravel mechanisms underlying natural phenomena has been developing. Recent years have witnessed unprecedented growth in research in the area of pharmaceuticals and medicine. The optimism that nanotechnology (NT) applied to medicine and drugs is taking serious...
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Antifungal Activity of Capridine β as a Consequence of Its Biotransformation into Metabolite Affecting Yeast Topoisomerase II Activity
PublicationIn the last few years,increasing importance is attached to problems caused by fungal pathogens. Current methods of preventing fungal infections remain unsatisfactory. There are several antifungal compounds whichare highly effective in some cases, however, they have limitations in usage: Nephrotoxicity and other adverse effects. In addition, the frequent use of available fungistatic drugs promotes drug resistance....
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Organic solvents aggregating and shaping structural folding of protein, a case study of the protease enzyme
PublicationLow solubility of reactants or products in aqueous solutions can result in the enzymatic catalytic reactions that can occur in non-aqueous solutions. In current study we investigated aqueous solutions containing different organic solvents / deep eutectic solvents (DESs) that can influence the protease enzyme's activity, structural, and thermal stabilities. Retroviral aspartic protease enzyme is responsible for the cleavage of 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.
PublicationHere, 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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Molecular mechanism of proton-coupled ligand translocation by the bacterial efflux pump EmrE
PublicationThe current surge in bacterial multi-drug resistance (MDR) is one of the largest challenges to public health, threatening to render ineffective many therapies we rely on for treatment of serious infections. Understanding different factors that contribute to MDR is hence crucial from the global “one health” perspective. In this contribution, we focus on the prototypical broad-selectivity proton-coupled antiporter EmrE, one of the...
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Determination of Pesticide Residues in Honeybees using Modified QUEChERS Sample Work-Up and Liquid Chromatography-Tandem Mass Spectrometry
PublicationIncreasing emissions of chemical compounds to the environment, especially of pesticides, is one of factors that may explain present honeybee colony losses. In this work, an analytical method employing liquid chromatography-tandem mass spectrometry (LC-MS/MS) was optimized for the simultaneous screening of 19 pesticides which have not been yet determined in honeybee samples from northern Poland (Pomerania). The sample preparation,...
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A novel chemiluminescent immunoassay based on original acridinium ester labels as better solution for diagnosis of human toxoplasmosis than conventional ELISA test
PublicationToxoplasma gondii infection is one of the most common human zoonosis. Laboratory diagnosis of this disease is mainly based on the results of serological methods detecting specific antibodies in the patient’s sera. In this study we aimed to evaluate the performance of a chemiluminescence immunoassay (CLIA) based on the use of a novel immunochemical reagent in the form of the conjugate of original acridinium label (AL) attached to...
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Optical method supported by machine learning for dynamics of C‐reactive protein concentrations changes detection in biological matrix samples
PublicationIn this article we present the novel spectroscopy method supported with machine learning for real-time detection of infectious agents in wastewater. In the case of infectious diseases, wastewater monitoring can be used to detect the presence of inflammation biomarkers, such as the proposed C-reactive protein, for monitoring inflammatory conditions and mass screening during epidemics for early detection in communities of concern,...
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Folding‐upon‐repair DNA nanoswitches for monitoring DNA repair enzymes activity
PublicationWe demonstrate here a new class of DNA‐based nanoswitches that, upon enzymatic repair, could undergo a conformational change mechanism leading to a change in fluorescent signal. Such folding‐upon‐repair DNA nanoswitches are synthetic DNA sequences containing O6‐methyl‐guanine (O6‐MeG) nucleobases and labelled with a fluorophore/quencher optical pair. The nanoswitches are rationally designed so that only upon enzymatic demethylation...
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Detection of gaseous compounds with different techniques
PublicationSensing technology has been developed for detection of gases in some environmental, industrial, medical, and scientific applications. The main tasks of these works is to enhance performance of gas sensors taking into account their different applicability and scenarios of operation. This paper presents the descriptions, comparison and recent progress in some existing gas sensing technologies. Detailed introduction to optical sensing...
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LEGAL ASPECTS OF ELECTRIC ENERGY GENERATION IN A FLOATING POWER PLANT
PublicationThis paper discusses the characteristics of pollution and legal regulations governing investment projects affecting the environment. It describes a combined system of a compression ignition engine and a steam turbine, whose aim, when placed on a floating platform, is to produce electric energy in a so-called distributed generation system. Such a system involves a reciprocating internal combustion engine and a connected steam turbine...
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Game with a Purpose for Verification of Mappings Between Wikipedia and WordNet
PublicationThe paper presents a Game with a Purpose for verification of automatically generated mappings focusing on mappings between WordNet synsets and Wikipedia articles. General description of idea standing behind the games with the purpose is given. Description of TGame system, a 2D platform mobile game with verification process included in the game-play, is provided. Additional mechanisms for anti-cheating, increasing player’s motivation...
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Measurement of Latency in the Android Audio Path
PublicationThis paper provides a description of experimental investigations concerning comparison between the audio path characteristics of various Android versions. First, information about the changes in each system version in the context of latency caused by them is presented. Then, a measurement procedure employing available applications to measure latency is described comparing to results contained in the Internet. Finally, a comparison...
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Comparison of active proximity radars for the wearable devices
PublicationTwo methods of object position and movement estimation in relation to the user of smart glasses were investigated. An active infrared and ultrasonic methods of the obstacle detection were presented and compared. Application of these methods depend on active transducers type (physical medium used), geometry and surface properties of detected objects and their movement direction and speed. In the article properties of both detectors...
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Celebrating 50 years of SWIMs (Salt Water Intrusion Meetings)
PublicationThe Salt Water Intrusion Meetings, or SWIMs, are a series of meetings that focus on seawater intrusion in coastal aquifers and other salinisation processes. 2018 marks the 50th year of the SWIM and the 25th biennial meeting. The SWIM proceedings record half a century of research progress on site characterisation, geophysical and geochemical techniques, variable-density flow, modelling, and water management. The SWIM is positioning...
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Electrochemical simulation of enzymatic transformations studied for the selected antitumor acridine derivatives
PublicationThe elucidation of the metabolic pathways and the biotransformation mechanisms of potential drugs is a crucial point in drug development. It allows to know the activation routes of the new biologically active compounds, especially in respect to their possible toxicity. Generally, in vivo or in vitro experiments with liver microsomes or hepatocytes are performed. However, these testing schemes are tedious, time consuming and of...
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Tailoring the electrochemical degradation of iron protected with polypyrrole films for biodegradable cardiovascular stents
PublicationThe degradation of polypyrrole (PPy) coated iron is studied in phosphate buffer saline solution at 37 °C by odd random phase multisine electrochemical impedance spectroscopy (ORP-EIS). PPy is electropolymerized with anti-inflammatory salicylates incorporated in the film, as a drug release system. The modelling of EIS over time provides the quantitative description of the corrosion behaviour of the material. Thus, the reliable...
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MPSs Marine port surveillance and observation system using mobile unmanned research units
ProjectsProject realized in Department of Geoinformatics according to NOR/POLNOR/MPSS/0037/2019-00 agreement from 2021-02-01
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A Human Behaviour Model Agent for Testing of Voluntary Computing Systems
PublicationPaper presents a design and performance of a voluntary-based distributed computing system testing agent, implementing a human behaviour model. The agent, nicknamed iRobot, was designed and implemented to enable controlled, large scale testing of core algorithms of Comcute - a new voluntary distributed computing platform complementary to BOINC. The main agent design goals were: emulation of human behaviour when browsing web pages,...
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TECHNOLOGIA RADIA PROGRAMOWALNEGO – SPRZĘT I OPROGRAMOWANIE
PublicationTechnologia radia programowalnego (ang. Software Defined Radio) jest nowoczesnym rozwiązaniem umożliwiającym realizację urządzeń pracujących w różnego rodzaju systemach łączności radiowej. W pracy zaprezentowano zagadnienia dotyczące koncepcji realizacji radia programowalnego. Zaprezentowano budowę dwóch przykładowych platform sprzętowych do realizacji radia programowalnego. Przedstawiono również architekturę oprogramowania stosowaną...
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Android OS: A Review
PublicationDue to the technological development, mobile terminals have evolved into functionally sophisticated devices such as smartphones and tablets. The Android platform has become one of the most popular operating system with millions of new users each year. Despite many studies, none have provided a comprehensive description of this operating system. In this paper we present a review of the Android OS. We describe the platforms history...
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Moduł gier miejskich dla elektronicznego przewodnika multimedialnego EGIT
PublicationW artykule przedstawiono charakterystykę dostępnych rozwiązań i platform gier miejskich oraz dokonano ich porównania. Przedstawiono koncepcję definiowania funkcjonalności modułu gier miejskich stanowiącego rozszerzenie przewodnika eGIT. Opisano architekturę komponentową elektonicznego, bezprzewodowego, multimedialnego przewodnika eGIT wraz z modułem gier miejskich. Przedstawiono proces integracji modułu z aplikacją bazową eGIT,...
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Some Optimization Methods for Simulations in Volunteer and Grid Systems
PublicationIn this chapter, some optimization methods have been presented for improving performance of simulations in the volunteer and grid computing system called Comcute. Some issues related to the cloud computing can be solved by presented approaches as well as the Comcute platform can be used to simulate execution of expensive and energy consuming long-term tasks in the cloud environment. In particular, evolutionary algorithms as well...
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Systemy pomiarowe stosowane na platformach powietrznych
PublicationPoszukiwanie na ogromnych obszarach złóż bogactw naturalnych Ziemi przeprowadza się z zastosowaniem platform powietrznych (samolot, helikopter). Jest to stosunkowo szybka i tania metoda poszukiwań. W badaniach geologicznych stosuje się metodę magnetometryczną, elektromagnetyczną i grawimetryczną. W pracy przedstawiono systemy pomiarowe na platformach powietrznych wykorzystujące metodę elektromagnetyczną i magnetometryczną. W pracy...
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Joanna Kabrońska dr inż. arch.
PeoplePhD with honours: Forma architektoniczna jako droga realizacji idei biblioteki przyszłości (Form of Architectural Solutions as a Means of Implementing the idea of Libraries of the Future), 1994 IV International Biennale of Architecture in Cracow Prize winner, 1991 DAAD post-doctoral scholarship, Berlin, 2002 Author of publications on architecture, art and memory, including the monograph Architektura jako forma pamięci. Rola architektury...
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Accuracy of a low-cost autonomous hexacopter platforms navigation module for a photogrammetric and environmental measurements
PublicationA photogrammetry and environmental measurements from an unmanned aerial vehicle (UAV) are a low-cost alternative for a traditional aerial photogrammetry. A commercial off-the-shelf products (COTS) offers a variety of cheap components that a suitable to be used on board a UAV. In this paper a low-cost navigation module based on Ublox NEO-M8N GPS and Pixhawk flight controller have been described, as a main extrinsic parameters source...
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Impact of SDN Controller’s Performance on Quality of Service
PublicationSoftware Defined Networking is a paradigm in network architecture; that is quickly becoming commonplace in modern telecommunication systems. It facilitates network customization for the requirements of different applications and simplifies the implementation of new services. Since its proposal, a significant evolution in its functionality has occurred. However, this development brought along problems of efficiency and performance,...
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Effects of an immunosuppressive treatment on the rat prostate
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Synthesis and biological evaluation of N-acylated tyramine sulfamates containing C-F bonds as steroid sulfatase inhibitors
PublicationSteroid sulfatase (STS) is responsible for the hydrolysis of biologically inactive sulfated steroids into their active un-sulfated forms and promotes the growth of various hormone-dependent cancers (e.g., breast cancer). Therefore, the STS enzyme is a promising therapeutic target for the treatment of steroid-sensitive cancers. Herein, we report the synthesis and biological evaluation of sulfamate analogs as potential STS inhibitors...
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Influence of S-Oxidation on Cytotoxic Activity of Oxathiole-Fused Chalcones
PublicationSynthesis, in vitro cytotoxic activity, and interaction with tubulin of oxidized, isomeric 1-(5-alkoxybenzo[d] [1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-ones and 1-(6- alkoxybenzo[d][1,3]oxathiol-5-yl)-3-phenylprop-2-en-1- ones are described. Most of the compounds demonstrated cytotoxic activity at submicromolar concentrations. It was found that oxidation of sulfur atom of the oxathiole-fused chalcones strongly influenced activity...
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Novel anticancer strategy aimed at targeting shelterin complexes by the induction of structural changes in telomeric DNA: hitting two birds with one stone.
PublicationThe ends of chromosomes in mammals are composed of telomeric DNA containing TTAGGG repeats, which bind specific proteins called shelterins. This telomeric DNA together with shelterins form a cap that protects the ends of chromosomes from being recognized as sites of DNA damage and from chromosomal fusions. Many very successful antitumor drugs used in the treatment of cancer patients bind to DNA, some of them with a prominent sequence...
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Structural Factors Affecting Cytotoxic Activity of (E)-1-(Benzo[d ][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one Derivatives
PublicationDerivatives of (E)-1-(5-alkoxybenzo[d][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one (1) demonstrated exceptionally high in vitro cytotoxic activity, with IC50 values of the most active derivatives in the nanomolar range. To identify structural fragments necessary for the activity, several analogs deprived of selected fragments were prepared, and their cytotoxic activity was tested. It was found that the activity depends on combined effects...
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Solubility advantage of sulfanilamide and sulfacetamide in natural deep eutectic systems: experimental and theoretical investigations
PublicationObjective: The aim of this study was to explore the possibility of using natural deep eutectic solvents (NADES) as solvation media for enhancement of solubility of sulfonamides, as well as gaining some thermodynamic characteristics of the analyzed systems. Significance: Low solubility of many active pharmaceutical ingredients is a well-recognized difficulty in pharmaceutical industry, hence the need for different strategies addressing...
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Highly Potent Antidiuretic Antagonists: Conformational Studies of Vasopressin Analogues Modified with 1-Naphthylalanine Enantiomers at Position 2
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Structure–activity relationships study on biological activity of peptides as dipeptidyl peptidase IV inhibitors by chemometric modeling
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Design and characteristics of gellan gum beads for modified release of meloxicam
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Synthesis and biological evaluation of fluorinated 3-phenylcoumarin-7-O-sulfamate derivatives as steroid sulfatase inhibitors
PublicationIn the present work, we report the initial results of our study on a series of 3-phenylcoumarin sulfamate-based compounds containing C-F bonds as a novel inhibitors of steroid sulfatase (STS). The new compounds are potent STS inhibitors, possessing more than 10 times higher inhibitory potency than coumarin-7-O-sulfamate. In the course of our investigation, compounds 2b and 2c demonstrated the highest inhibitory effect in the enzymatic...
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Simplified, serine‐rich theta‐defensin analogues as antitumour peptides
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Conformational Preferences of Proline Derivatives Incorporated into Vasopressin Analogues: NMR and Molecular Modelling Studies
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Aryl- and heteroaryl-substituted phenylalanines as AMPA receptor ligands
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Short Term Monitor of Photodegradation Processes in Ranitidine Hydrochloride Observed by FTIR and ATR FTIR
PublicationThe effects of degradation of ranitidine hydrochloride exposed to UVB radiation (l = 310 nm) and oxygen in a weathering chamber were studied by Fourier Transform Infrared spectroscopy (FTIR) and Attenuated Total Reflectance Fourier Transform Infrared spectroscopy (ATR-FTIR). ATR-FTIR profile indicated that the degradation was spatially heterogeneous. Significant amounts of photoproducts were detected only in a directly...
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CDK9: Therapeutic Perspective in HCC Therapy
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Current Challenges in Targeting Tumor Desmoplasia to Improve the Efficacy of Immunotherapy
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Investigating the disease‐modifying properties of sclerotiorin in Alzheimer's therapy using acetylcholinesterase inhibition
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Current state of a dual behaviour of antimicrobial peptides-Therapeutic agents and promising delivery vectors
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Preliminary antifungal activity assay of selected chlorine-containing derivatives of xanthone and phenoxyethyl amines
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The Chemometric Evaluation of Antitumor Activity of Novel Benzensulfonamide Derivatives Based on their Physiochemical Properties
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