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Wyniki wyszukiwania dla: TARGETED DRUG DELIVERY
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Targeting shelterin proteins for cancer therapy.
PublikacjaAs 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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Steroid Sulfatase Inhibitors Based on Phosphate and Thiophosphate Flavone Analogs
PublikacjaA 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
PublikacjaRekombinantowe 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
PublikacjaPharmaceutical 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
PublikacjaIn 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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Kod fontannowy z przyrastającą liczbą symboli źródłowych
PublikacjaKody fontannowe zabezpieczające transmisję przed wymazaniami wyróżnia brak określonej z góry długości i losowy sposób generacji kolejnych pakietów kodowych. W pracy pokazano jak właściwości tych kodów zależą od rozkładu macierzy generującej dla dwóch wariantów dostarczania pakietów do kodera. Szczególnie interesujący jest przypadek, gdy pakiety źródłowe trafiają do kodera stopniowo podczas transmisji. Uzyskane wyniki wskazują na...
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Impact of selected drugs and their binary mixtures on the germination of Sorghum bicolor (sorgo) seeds
PublikacjaThe aim of this study was to assess the toxicological potential of binary drug mixtures and individual drugs under different pH conditions with different inorganic ion additions on the germination of Sorghum bicolor (sorgo) seeds. To assess whether the given drug mixtures were more phytotoxic than the individual compounds, concentration addition (CA) and independent action (IA) approaches were applied to estimate the predicted...
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The project of pull system for storehouse and production line in a company provides electronics
PublikacjaThe chapter below presents how to reduced delivery of the material to production by using a "Kanban schedule board" and related tools from 48 hours and 59 minutes to 41 minutes in a company provides electronics. The solution was found through analysis of the current way of supplying stands and using Just In Time idea, the reduction of ''muda''. To solve the problem was used Kanban card", which has the shape of two triangles joined...
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Wireless Charging Station Design for Electric Scooters: Case Study Analysis
PublikacjaThis study proposes an example of a wireless charging station design for a small-scale vehicle available on the market. The article analyzes basic transmitter inverter topologies and their compensation methods in terms of flexibility of control, tolerance to uncertainty in positioning, and the possibility of decreasing the integration price. Our comprehensive analysis focuses on the battery voltage range, energy capacity, cost,...
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Ancillary services to grids provided with distributed generation
PublikacjaThe paper introduces system for utilization of the customer-side generated energy. Additionally system can secure some ancillary services to grids. Those services include: current active filtering, load voltage stabilization and in case of grid voltage faults - uninterruptible load supplying (possible with energy storage device). Presented experimental results confirm flexibility of this arrangement in processes of power delivery...
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Problem of aggregation in dye-DNA interaction, calorimetry studies
PublikacjaNucleic acids are the biological target for many antimicrobial, antitumor and antiviral drugs. Ligand-DNA interactions can be classified into two major categories: 1. covalent binding, which can provide to intermolecular adducts, 2. physico-chemical interactions, which can be divided into intercalation (e.g. adriamycin) or groove binding (e.g. dystamycin). There are several methods to investigate interactions between drug and DNA....
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Visual Object Tracking System Employing Fixed and PTZ Cameras
PublikacjaThe paper presents a video monitoring system utilizing fixed and PTZ cameras for tracking of moving objects. First type of camera provides image for background modelling, being employed for foreground objects localization. Estimated objects locations are then utilised for steering of PTZ cameras when observing targeted objects with high close-ups. Objects are classified into several classes, then basic event detection is being...
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Considerations of Computational Efficiency in Volunteer and Cluster Computing
PublikacjaIn the paper we focus on analysis of performance and power consumption statistics for two modern environments used for computing – volunteer and cluster based systems. The former integrate computational power donated by volunteers from their own locations, often towards social oriented or targeted initiatives, be it of medical, mathematical or space nature. The latter is meant for high performance computing and is typically installed...
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Closed-loop stimulation of temporal cortex rescues functional networks and improves memory
PublikacjaMemory failures are frustrating and often the result of ineffective encoding. One approach to improving memory outcomes is through direct modulation of brain activity with electrical stimulation. Previous efforts, however, have reported inconsistent effects when using open-loop stimulation and often target the hippocampus and medial temporal lobes. Here we use a closed-loop system to monitor and decode neural activity from direct...
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Nowe substancje psychoaktywne CZ. II. SYNTETYCZNE KANNABINOIDY - CHARAKTERYSTYKA, METODY OZNACZANIA I WYZWANIA ANALITYCZNE
PublikacjaDo nielegalnego obrotu co roku trafiają nowe związki o działaniu psychoaktywnym. Dostęp do takich substancji nie jest trudny, gdyż są one łatwo dostępne w wielu krajach, głównie w sklepach internetowych. Ponadto, organy ścigania i wymiar sprawiedliwości nie nadążają z wprowadzaniem tych substancji na listy substancji zakazanych przez co ich kontrola jest bardzo utrudniona. Syntetyczne kannabinoidy to grupa związków chemicznych,...
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A Novel Multicast Architecture of Programmable Networks
PublikacjaIn the paper a multicast architecture for programmable networks based on separation of group management and network control tasks is proposed. Thanks to this separation, services which want to make use of multicast communications no longer have to implement low-level network functionalities and their operation is greatly simplified. Abstracting service’s view of the network into a fully connected cloud enables us to transparently...
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Ipertrofan Revisited—The Proposal of the Complete Stereochemistry of Mepartricin A and B
PublikacjaBeing 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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Nowe substancje psychoaktywne. Cz. I. Współczesna sytuacja narkotykowa
PublikacjaGwałtowny wzrost liczby substancji wprowadzanych na rynek narkotykowy został zaobserwowany już pod koniec lat dziewięćdziesiątych XX wieku. Każdego roku syntezowane są nowe substancje jako analogi już istniejących, a ich ilość systematycznie rośnie. Niejednokrotnie wprowadzenie niewielkiej zmiany w strukturze związku może spowodować znaczne zmiany ich właściwości fizykochemicznych oraz psychoaktywnych. Nowe substancje psychoaktywne...
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Wpływ produkcji butelek z tworzyw sztucznych na środowisko naturalne. Cz. I. Zastosowanie metody oceny ReCiPe 2016 w celu identyfikacji problemów środowiskowych
PublikacjaDokonano oceny wpływu opakowań na środowisko naturalne. Głównym celem było przeprowadzenie analizy cyklu życia (LCA) butelki do napojów wykonanej z poli(tereftalanu etylenu) (PET). Za jednostkę funkcjonalną przyjęto łącznie 1000 szt. butelek PET o pojemności 1 L. Granica przyjętego systemu obejmowała kroki od momentu dostarczenia preform do zakładu produkcyjnego aż do ich prawidłowego ukształtowania w procesie produkcyjnym. Z systemu...
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Metabolism of antitumour agent 1-nitroacridine derivative, C-1748 in pancreatic cancer cell lines
PublikacjaPancreatic cancer has the highest mortality rate of all major cancers because of limited treatment options. Surgical removal of the tumour is possible only in its early stage, nevertheless the asymptomatic development very often makes unable an accurate diagnose. In the case of metastatic pancreatic cancer only chemotherapy, mainly with gemcitabine, can be offered to patients. However, common resistance towards gemcitabine imposes...
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Impact of inorganic ions and pH variations on toxicity and endocrine potential of selected environmentally relevant pharmaceuticals
PublikacjaAssessment of the impact of pharmaceutical residues on living organisms is a very complex subject. Apart from taking into account the toxicity of individual compounds, environmental factors should also be taken into account. In this paper, attempts were made to assess the impact of coexisting inorganic ions and changes in pH on the toxicity of ten selected pharmaceuticals. Two bioassays were used to measure the estrogenic and androgenic...
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Improving the production planning and control process
PublikacjaFocusing the activities of a production business on the strategy based on quality entails orientation on meeting the expectations of the customers with respect to the product itself, and the terms of its delivery. The article notes the role of the production planning and control process in improving the quality of the business offer. It identifies the objectives set for the process from the perspective of meeting the expectations...
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PROJECT IMPLEMENTATION IN ORGANISATIONS OF REPETITIVE ACTIVITIES
PublikacjaThe study presents the implementation of projects in organisations that achieve business objec-tives through the implementation of repetitive actions. Projects in these organisations are, on the one hand, treated as marginal activities, while the results of these projects have significant impact on the delivery of main processes, e.g. through the introduction of new products. Human capital and solutions in this field bear impact...
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Voltage control in a power system with renewable sources of energy
PublikacjaIntensive development of distributed generation in power systems, caused by the European Union energy policy, gives possibility for improving safety in power delivery as well as optimizing the costs of the systems functioning. In this context, distributed generation can be used for voltage control in power systems – it can be performed by the control of reactive power of each source of energy or a group of energy sources. This...
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Detection of propofol concentrations in blood by Raman spectroscopy
PublikacjaIn this paper we present a proof-of-concept of a Raman spectroscopy-based approach for measuring the content of propofol, a common anesthesia drug, in whole human blood, and plasma, which is intended for use during clinical procedures. This method utilizes the Raman spectroscopy as a chemically–sensitive method for qualitative detection of the presence of a drug and a quantitative determination of its concentration. A number of...
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Train the trainer course
PublikacjaThis 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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Comparative Analysis of Two Polish Hyperbolic Systems AEGIR and JEMIOLUSZKA
PublikacjaGlobal Navigation Satellite System (GNSS) is seen by terrorists or hostile countries as a high value target. Volpe Center report contains the following statement: “During the course of its development for military use and more recent extension to many civilian uses, vulnerabilities of Global Navigation Satellite Systems (GNSS) – in the United States the Global Positioning System (GPS) – have become apparent. The vulnerabilities...
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What Is Troubling IT Analysts? A Survey Report from Poland on Requirements-Related Problems
PublikacjaRequirements engineering and business analysis are activities considered to be important to software project success but also difficult and challenging. This paper reports on a survey conducted in Polish IT industry, aimed at identifying most widespread problems/challenges related to requirements. The survey was targeted at people performing role of analyst in commercial IT projects. The questionnaire included 64 pre-defined problems...
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Alkohol-społeczny problem XXI wieku. Zastosowanie biowskaźników spożywania alkoholu w diagnostyce medycznej.
PublikacjaAlkohol etylowy jest legalną i ogólnodostępną substancją o działaniu psychoaktywnym. Spożywany w niewielkich ilościach może pozytywnie wpływać na zdrowie, ale jego nadmierna konsumpcja powoduje silne uzależnienie. Może być to przyczyną agresywnych zachowań, przemocy w rodzinie, problemów w kontaktach z ludźmi, problemów z prawem, samobójstw, wypadków samochodowych oraz problemów finansowych. Dlatego też, szybka i jednoznaczna diagnostyka...
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Factors causing degradation of sulfadimetoxine
PublikacjaSulfadimetoxine is a representative of sulfonamide drugs which presence inhibits growth of activated sludge bacteria, rhat is necessary for the effective mineralization of organic and inorganic contaminants. Therefore factors which con prevent this situation are searched. Aim of this study is selection of conditions causing efficien degradation of the drug- sulfadimetoxine. The impact of such aspects as : the type of oxidizing...
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Mechanism-based inactivation of human cytochrome P450 1A2 and 3A4 isoenzymes by antitumor triazoloacridinone C-1305.
Publikacja5-Dimethylaminopropylamino-8-hydroxytriazoloacridinone, C-1305, is a promising antitumor therapeutic agent with high activity against several experimental tumors. It was determined to be a potent and selective inhibitor of liver microsomal and human recombinant cytochrome P450 (CYP) 1A2 and 3A4 isoenzymes. Therefore, C-1305 might modulate the effectiveness of other drugs used in multidrug therapy. The objective of this study was...
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Thermodynamics and kinetics of amphotericin B self-association in aqueous solution characterized in molecular detail
PublikacjaAmphotericin B (AmB) is a potent but toxic drug commonly used to treat systemic mycoses. Its efficiency as a therapeutic agent depends on its ability to discriminate between mammalian and fungal cell membranes. The association of AmB monomers in an aqueous environment plays an important role in drug selectivity, as oligomers formed prior to membrane insertion – presumably dimers – are believed to act differently on fungal (ergosterol-rich)...
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Visualizing Carotid Bodies With Doppler Ultrasound Versus CT Angiography: Preliminary Study
PublikacjaOBJECTIVE. The purpose of this article is to evaluate the utility of ultrasound in identifying carotid bodies (CBs) in patients with drug-resistant arterial hypertension. SUBJECTS AND METHODS. We enrolled 13 patients with drug-resistant hypertension into a trial for surgical CB excision. CT angiography (CTA) and Doppler ultrasound (DUS) of the cervical arteries were performed before surgery. CBs were identified in a blind manner...
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Evaluation of the efficiency of the duty cycle of refuse collection vehicle based on real-world data
PublikacjaIn this paper a method of the efficiency evaluation of the duty cycle of Refuse Collection Vehicle is presented. Using real world data, two representative duty cycles were analysed. Total cycle efficiency was calculated, as well as the efficiency of particular cycle phases. Then, energy needed to collect and compact the waste and energy from fuel were compared. Measured and calculated values were shown on the diagrams illustrating...
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Molecular detection of Candida krusei
PublikacjaThe species identification of fungi belonging to genus Candida is an important issue as this genus becomes the emerging problem of nosocomial infections. As Candida krusei presents intrinsicresistance to the fluconazole that is the drug of the first choice in case of invasive candidiasis the PCR identifying the DNA of C. krusei was elaborated. The analytical sensitivity of the assay on spiked blood samples was estimated at 3-5...
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Pathological brain network activity: memory impairment in epilepsy
PublikacjaOur thinking, memory and cognition in general, relies upon precisely timed interactions among neurons forming brain networks that support cognitive processes. The surgical evaluation of drug-resistant epilepsy using intracranial electrodes provides a unique opportunity to record directly from human brain and to investigate the coordinated activity of cognitive networks. In this issue of Neurology®, Kleen and colleagues1 implicate...
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What is the future of digital education in the higher education sector? An overview of trends with example applications at Gdańsk Tech, Poland
PublikacjaUniversities worldwide recognise the need to adapt to changes in society, the economy and the way young people prefer to learn. Additionally, the impetus to improve the digital approach in higher education intensifies as educational institutions have to remain competitive with commercial providers of education. Following the latest technological trends and implementing strategies to develop new digital solutions helps to improve...
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Development of chromatographic and mass spectrometry conditions for untargeted lipidomic analysis of human breast milk
PublikacjaHuman breast milk (HBM) is a complex biofluid containing components which are essential for the proper growth of the newborn (for example nutrients such as carbohydrates, proteins, lipids) and also bioactive substances. According to the literature, most of studies involving HBM nutrients investigations focused essentially on the determination of proteins. The molecular composition of lipids in HBM is not well known as the protein...
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A Mesh Deformation Technique Based on Solid Mechanics for Parametric Analysis of High-Frequency Devices With 3-D FEM
PublikacjaIn this paper, a versatile technique for mesh defor- mation is discussed, targeted at the electromagnetic (EM) field simulation of high-frequency devices using the 3-D finite element method (FEM). The approach proposed applies a linear elasticity model to compute the displacements of the internal mesh nodes in 3-D when the structure geometry is changed. The technique is compared with an alternative approach...
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Analytical Strategies and Applications in Lipidomics
PublikacjaLipidomics is a field of study aiming at a comprehensive analysis of a set of lipids in biological systems. This includes both quantitative and qualitative characterization of lipid profiles, comparative studies of lipidomes, and analysis of lipid-protein interactions. Lipids are structurally diversified that make their analysis a challenging task. The constant advances in analytical technologies, especially in the field of high-performance...
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Direct brain stimulation modulates encoding states and memory performance in humans
PublikacjaPeople often forget information because they fail to effectively encode it. Here, we test the hypothesis that targeted electrical stimulation can modulate neural encoding states and subsequent memory outcomes. Using recordings from neurosurgical epilepsy patients with intracranially implanted electrodes, we trained multivariate classifiers to discriminate spectral activity during learning that predicted remembering from forgetting,...
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Nanotubular oxide layers and hydroxyapatite coatings on porous titanium alloy Ti13Nb13Zr
PublikacjaThe surface condition of an implant has a significant impact on response occurring at the implant-biosystem border. The knowledge of physical-chemical and biological processes allows for targeted modification of biomaterials to induce a specified response of a tissue. The present research was aimed at development of technology composing of obtaining the nanotube oxide layers on a porous titanium alloy Ti13Nb13Zr, followed by the...
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Threat intelligence platform for the energy sector
PublikacjaIn recent years, critical infrastructures and power systems in particular have been subjected to sophisticated cyberthreats, including targeted attacks and advanced persistent threats. A promising response to this challenging situation is building up enhanced threat intelligence that interlinks information sharing and fine-grained situation awareness. In this paper a framework which integrates all levels of threat intelligence...
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Information-driven network resilience: Research challenges and perspectives
PublikacjaInternet designed over 40 years ago was originally focused on host-to-host message delivery in a best-effort manner. However, introduction of new applications over the years have brought about new requirements related with throughput, scalability, mobility, security, connectivity, and availability among others. Additionally, convergence of telecommunications, media, and information technology was responsible for transformation...
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Evaluation of possibilities in identification and susceptibility testing for Candida glabrata clinical isolates with the Integral System Yeast Plus (ISYP)
PublikacjaThe aim of this study was to evaluate possibilities of correct identification and susceptibility testing of C. glabrata clinical isolates with Integral System Yeast Plus (ISYP). For species identification, as the reference method, API Candida test and species-specific PCR reactions were used. The potential of antifungal susceptibility testing by the ISYP test was compared with the Sensititre Yeast One. Whilst the reference methods...
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Molecular mechanism of proton-coupled ligand translocation by the bacterial efflux pump EmrE
PublikacjaThe 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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Organic solvents aggregating and shaping structural folding of protein, a case study of the protease enzyme
PublikacjaLow 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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Antifungal Activity of Capridine β as a Consequence of Its Biotransformation into Metabolite Affecting Yeast Topoisomerase II Activity
PublikacjaIn 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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Imidazoacridinone-dependent lysosomal photodestruction: a pharmacological Trojan horse approach to eradicate multidrug-resistant cancers
PublikacjaMultidrug resistance (MDR) remains a primary hindrance to curative cancer therapy. Thus, introduction of novel strategies to overcome MDR is of paramount therapeutic significance. Sequestration of chemotherapeutics in lysosomes is an established mechanism of drug resistance. Here, we show that MDR cells display a marked increase in lysosome number. We further demonstrate that imidazoacridinones (IAs), which are cytotoxic fluorochromes,...
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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
PublikacjaHigh 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...