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Wyniki wyszukiwania dla: anti-cancer agents
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Palindromic carbazole derivatives: unveiling their antiproliferative effect via topoisomerase II catalytic inhibition and apoptosis induction
PublikacjaHuman DNA topoisomerases are essential for crucial cellular processes, including DNA replication, transcription, chromatin condensation, and maintenance of its structure. One of the significant strategies employed in cancer treatment involves the inhibition of a specific type of topoisomerase, known as topoisomerase II (Topo II). Carbazole derivatives, recognised for their varied biological activities, have recently become a significant...
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ANTI-CORROSION METHODS AND MATERIALS
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Novel 2-alkythio-4-chloro-N-[imino(heteroaryl)methyl]benzenesulfonamide Derivatives: Synthesis, Molecular Structure, Anticancer Activity and Metabolic Stability
PublikacjaA series of novel 2-alkythio-4-chloro-N-[imino-(heteroaryl)methyl]benzenesulfonamide derivatives, 8–24, were synthesized in the reaction of the N-(benzenesulfonyl)cyanamide potassium salts 1–7 with the appropriate mercaptoheterocycles. All the synthesized compounds were evaluated for their anticancer activity in HeLa, HCT-116 and MCF-7 cell lines. The most promising compounds, 11–13, molecular hybrids containing benzenesulfonamide...
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Poszukiwanie nowych leków immunosupresyjnych (Quest for new immunosuppressive drugs)
PublikacjaTransplantology is getting more and more important in medicine. Development of surgical techniques and immunosuppressive treatment enabled to establish successful transplantations with various organs and tissues. However, allografts are recognized as foreign tissues and stimulate rejection, i.e. a strong immunological response which, if not stopped, results in complete destruction of the transplanted tissue. In order to prevent...
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Inhibiting activity of HIV-1: protease, reverse transcriptase and integrase all together by novel compounds using computational approaches (flexible and rigid docking)
PublikacjaAcquired immunodeficiency syndrome (AIDS), caused by human immunodeficiency virus type 1 (HIV-1) infection, is one of the most challenging diseases in recent decades. Nevertheless the shortcomings of chemical drugs such as toxicity, lack of curative effects, the search for more potent anti-HIV agents have been focused in our study. In current study, novel scaffold was designed having a benzyl and imidazole in it which are very...
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Anticancer imidazoacridinone C-1311 inhibits hypoxia-inducible factor-1α (HIF-1α), vascular endothelial growth factor (VEGF) and angiogenesis
PublikacjaAntitumor imidazoacridinone C-1311 is a DNA-reactive topoisomerase II and FLT3 receptor tyrosine kinase inhibitor. Here, we demonstrate the mechanism of C-1311 inhibitory action on novel targets: hypoxia-inducible factor-1α (HIF-1α), vascular-endothelial growth factor (VEGF), and angiogenesis. In a cell-free system, C-1311 prevented HIF-1α binding to an oligonucleotide encompassing a canonical hypoxia-responsive element (HRE),...
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Methods for Elucidation of DNA-Anticancer Drug Interactions and Their Applications in the Development of New Drugs
PublikacjaDNA damaging agents including anthracyclines, camptothecins and platinum drugs are among most frequently used drugs in the chemotherapeutic routine. Due to their relatively low selectivity for cancer cells, administration is associated with adverse side effects, whereas the inherent genotoxicity of these drugs is associated with risk of developing secondary cancers. Development of new drugs, which could be spared of these drawbacks...
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Design, synthesis and high antitumor potential of new unsymmetrical bisacridine derivatives towards human solid tumors, specifically pancreatic cancers and their unique ability to stabilize DNA G-quadruplexes
PublikacjaNew promising unsymmetrical bisacridine derivatives (UAs), have been developed. Three groupsincluding 36 compounds were synthesized by the condensation of 4-nitro or 4-methylacridinone, imi-dazoacridinone and triazoloacridinone derivatives with 1-nitroacridine compounds linked with anaminoalkyl chain. Cytotoxicity screening revealed the high potency of these compounds against severaltumor cell lines. Particularly, imidazoacridinone-1-nitroacridine...
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Conjugates of Ciprofloxacin and Levofloxacin with Cell-Penetrating Peptide Exhibit Antifungal Activity and Mammalian Cytotoxicity
PublikacjaSeven conjugates composed of well-known fluoroquinolone antibacterial agents, ciprofloxacin (CIP) or levofloxacin (LVX), and a cell-penetrating peptide transportan 10 (TP10-NH2) were synthesised. The drugs were covalently bound to the peptide via an amide bond, methylenecarbonyl moiety, or a disulfide bridge. Conjugation of fluoroquinolones to TP10-NH2 resulted in congeners demonstrating antifungal in vitro activity against human...
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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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Cancer immune escape: the role of antigen presentation machinery
PublikacjaThe mechanisms of antigen processing and presentation play a crucial role in the recognition and targeting of cancer cells by the immune system. Cancer cells can evade the immune system by downregulating or losing the expression of the proteins recognized by the immune cells as antigens, creating an immunosuppressive microenvironment, and altering their ability to process and present antigens. This review focuses on the mechanisms...
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Experimental and Theoretical Insights into the Intermolecular Interactions in Saturated Systems of Dapsone in Conventional and Deep Eutectic Solvents
PublikacjaSolubility is not only a crucial physicochemical property for laboratory practice but also provides valuable insight into the mechanism of saturated system organization, as a measure of the interplay between various intermolecular interactions. The importance of these data cannot be overstated, particularly when dealing with active pharmaceutical ingredients (APIs), such as dapsone. It is a commonly used anti-inflammatory and...
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Amino Acid and Peptide‐Based Antiviral Agents
PublikacjaA 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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Leader election for anonymous asynchronous agents in arbitrary networks
PublikacjaWe consider the problem of leader election among mobile agents operating in an arbitrary network modeled as an undirected graph. Nodes of the network are unlabeled and all agents are identical. Hence the only way to elect a leader among agents is by exploiting asymmetries in their initial positions in the graph. Agents do not know the graph or their positions in it, hence they must gain this knowledge by navigating in the graph...
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Comparison of antimicrobial activity of selected, commercially available wound dressing materials
PublikacjaOBJECTIVE: The aim of our study was to examine the antimicrobial potential of eight selected, commercially available wound dressings containing different antimicrobial agents: silver, chlorhexidine acetate, povidone-iodine, and manuka honey. METHOD: The materials were tested against four reference strains of bacteria: Staphylococcus aureus (PCM 2051), Staphylococcus epidermidis (PCM 2118), Pseudomonas aeruginosa (ATCC 27853),...
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Clearing directed subgraphs by mobile agents
PublikacjaWe study several problems of clearing subgraphs by mobile agents in digraphs. The agents can move only along directed walks of a digraph and, depending on the variant, their initial positions may be pre-specified. In general, for a given subset S of vertices of a digraph D and a positive integer k, the objective is to determine whether there is a subgraph H=(V,A) of D such that (a) S is a subset of V, (b) H is the union of k directed...
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ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
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Gold nanoparticles for cancer radiotherapy: a review
PublikacjaRadiotherapy is currently used in around 50% of cancer treatments and relies on the deposition of energy directly into tumour tissue. Although it is generally effective, some of the deposited energy can adversely affect healthy tissue outside the tumour volume, especially in the case of photon radiation (gamma and X-rays). Improved radiotherapy outcomes can be achieved by employing ion beams due to the characteristic energy deposition...
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Decontaminating Arbitrary Graphs by Mobile Agents: a Survey
PublikacjaA team of mobile agents starting from homebases need to visit and clean all nodes of the network. The goal is to find a strategy, which would be optimal in the sense of the number of needed entities, the number of moves performed by them or the completion time of the strategy. Currently, the field of distributed graph searching by a team of mobile agents is rapidly expanding and many new approaches and models are being presented...
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Rendezvous of Heterogeneous Mobile Agents in Edge-Weighted Networks
PublikacjaWe introduce a variant of the deterministic rendezvous problem for a pair of heterogeneous agents operating in an undirected graph, which differ in the time they require to traverse particular edges of the graph. Each agent knows the complete topology of the graph and the initial positions of both agents. The agent also knows its own traversal times for all of the edges of the graph, but is unaware of the corresponding traversal...
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Rendezvous of heterogeneous mobile agents in edge-weighted networks
PublikacjaWe introduce a variant of the deterministic rendezvous problem for a pair of heterogeneous agents operating in an undirected graph, which differ in the time they require to traverse particular edges of the graph. Each agent knows the complete topology of the graph and the initial positions of both agents. The agent also knows its own traversal times for all of the edges of the graph, but is unaware of the corresponding traversal...
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Rendezvous of Distance-Aware Mobile Agents in Unknown Graphs
PublikacjaWe study the problem of rendezvous of two mobile agents starting at distinct locations in an unknown graph. The agents have distinct labels and walk in synchronous steps. However the graph is unlabelled and the agents have no means of marking the nodes of the graph and cannot communicate with or see each other until they meet at a node. When the graph is very large we want the time to rendezvous to be independent of the graph size...
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Gossiping by energy-constrained mobile agents in tree networks
PublikacjaEvery node of an edge-weighted tree network contains a data packet. At some nodes are placed mobile agents, each one possessing an amount of energy (not necessarily the same for all agents). While walking along the network, the agents spend the energy proportionally to the distance traveled and collect copies of the data packets present at the visited network nodes. An agent visiting a node deposits there copies of all currently...
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Document Agents with the Intelligent Negotiations Capability
PublikacjaThe paper focus is on augmenting proactive document-agents with built -in intelligence to enable them to recognize execution context provided by devices visited durning the business process, and to reach collaboration agreement despite of their conflicting requirements. We propose a solution based on neural networks to improve simple multi-issue negotiation between the document and the device, practically with no excessive cost...
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Human UDP-Glucuronosyltransferases: Effects of altered expression in breast and pancreatic cancer cell lines.
PublikacjaIncreased aerobic glycolysis and de novo lipid biosynthesis are common characteristics of invasive cancers. UDP-glucuronosyltransferases (UGTs) are phase II drug metabolizing enzymes that in normal cells possess the ability to glucuronidate these lipids and speed their excretion; however, de-regulation of these enzymes in cancer cells can lead to an accumulation of bioactive lipids, which further fuels cancer progression. We hypothesize...
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TRF1 and TRF2: pioneering targets in telomere-based cancer therapy
PublikacjaThis article presents an in-depth exploration of the roles of Telomere Repeat-binding Factors 1 and 2 (TRF1 and TRF2), and the shelterin complex, in the context of cancer biology. It emphasizes their emerging significance as potential biomarkers and targets for therapeutic intervention. Central to the shelterin complex, TRF1 and TRF2 are crucial in maintaining telomere integrity and genomic stability, their dysregulation often...
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Neural network agents trained by declarative programming tutors
PublikacjaThis paper presents an experimental study on the development of a neural network-based agent, trained using data generated using declarative programming. The focus of the study is the application of various agents to solve the classic logic task – The Wumpus World. The paper evaluates the effectiveness of neural-based agents across different map configurations, offering a comparative analysis to underline the strengths and limitations...
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Big Data Processing by Volunteer Computing Supported by Intelligent Agents
PublikacjaIn this paper, volunteer computing systems have been proposed for big data processing. Moreover, intelligent agents have been developed to efficiency improvement of a grid middleware layer. In consequence, an intelligent volunteer grid has been equipped with agents that belong to five sets. The first one consists of some user tasks. Furthermore, two kinds of semi-intelligent tasks have been introduced to implement a middleware...
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Mobile chromatographs and spectrometers for the analysis of chemical warfare agents
PublikacjaThis article describes the technological state of readiness regarding mobile chromatographs and spectrometers and their appiicability for the analysis of chemical warfare agents (CWAs), degradation products, simulants, and precursors.
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Selection of derivatisation agents for chlorophenols determination with multicriteria decision analysis
PublikacjaThe paper shows very systematic method of selection of derivatisation agents for a given group of analytes. In this study 8 derivatisation agents are assessed for their capability to derivatise 8 chlorophenols. Multicriteria decision analysis is used to combine many objectives of derivatisation agents selection into single, easy to be interpreted numerical value. Three basic analyses were performed to obtain rankings with the aims...
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Exploring the Prevalence of Anti-patterns in the Application of Scrum in Software Development Organizations
PublikacjaThe paper presents a survey-based study that aimed to determine the prevalence of anti-patterns in the Scrum software development methodology. A total of 35 anti-patterns were selected from the literature review, and 42 respondents indicated whether they had encountered each anti-pattern in their organizations. The study found that``Unfinished Tasks'' was the most prevalent anti-pattern, highlighting the importance of proper planning...
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Deterministic rendezvous of asynchronous bounded-memory agents in polygonal terrains
PublikacjaTwo mobile agents, modeled as points starting at differentlocations of an unknown terrain, have to meet. The terrain is a polygon with polygonal holes. We consider two versions of this rendezvous problem: exact RV, when the points representing the agents have to coincide at some time, and epsilon-RV, when these points have to get at distance less than epsilon in the terrain. In any terrain, each agent chooses its trajectory, but...
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The Anti-Staphylococcal Potential of Ethanolic Polish Propolis Extracts
PublikacjaAbstract: The principal objective of this study was to determine the anti-staphylococcal potential of ethanol extracts of propolis (EEPs). A total of 20 samples of propolis collected from apiaries located in different regions of Poland were used in the study. The two-fold broth microdilution method revealed some important differences in the antimicrobial activity of investigated EEPs. Up to the concentration of 4096 µg/mL no activity...
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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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Justyna Płotka-Wasylka dr hab. inż.
OsobyUrodziła się w Słupsku (24.03.1986).W 2005 roku ukończyła I Liceum Ogólnokształcące im. Jana II Sobieskiego w Wejherowie i rozpoczęła studia na Wydziale Chemicznym Politechniki Gdańskiej. Po ich ukończeniu w 2010 rozpoczęła pracę naukową na tej uczelni, uzyskując w 2014 roku stopień doktora nauk chemicznych. Tematem jej rozprawy doktorskiej, wykonywanej pod kierunkiem prof. Marka Biziuka oraz dr Caluma Morrisona (Uniwersytet w...
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Cancer immunosurveillance by ILC2s
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Solubility of dapsone in deep eutectic solvents: Experimental analysis, molecular insights and machine learning predictions
PublikacjaBackground. Dapsone (DAP) is an anti-inflammatory and antimicrobial active pharmaceutical ingredient used to treat, e.g., AIDS-related diseases. However, low solubility is a feature hampering its efficient use. Objectives. First, deep eutectic solvents...
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Anti-plane waves in an elastic thin strip with surface energy
PublikacjaWe consider anti-plane motions of an elastic plate taking into account surface energy within the linear Gurtin–Murdoch surface elasticity. Two boundary-value problems are considered that describe complete shear dynamics of a plate with free faces or with free and clamped faces, respectively. These problems correspond to anti-plane dynamics of an elastic film perfectly or non-perfectly attached to a rigid substrate. Detailed analysis...
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Investigating beliefs in anti-vax conspiracy theories among medical students
PublikacjaAbstract: While the doctors’ role in immunization is essential, their lack of knowledge or vaccine hesitancy may affect their ability to communicate effectively and educate patients about vaccination, vaccine hesitancy, and vaccine conspiracy theories. This, in turn, may hinder health policy aimed at fighting infectious diseases. Vaccine hesitancy is prevalent not only among the general population but also among healthcare...
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Occurrence of Surface Active Agents in the Environment
PublikacjaDue to the specific structure of surfactants molecules they are applied in different areas of human activity (industry, household). After using and discharging from wastewater treatment plants as effluent stream, surface active agents (SAAs) are emitted to various elements of the environment (atmosphere, waters, and solid phases), where they can undergo numerous physic-chemical processes (e.g., sorption, degradation) and freely...
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Quantum strategies for rendezvous and domination tasks on graphs with mobile agents
PublikacjaThis paper explores the application of quantum nonlocality, a renowned and unique phenomenon acknowledged as a valuable resource. Focusing on an alternative application, we demonstrate its quantum advantage for mobile agents engaged in specific distributed tasks without communication. The research addresses the significant challenge of rendezvous on graphs and introduces a distributed task for mobile agents grounded in the graph...
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UK travel agents’ evaluation of eLearning courses offered by destinations: an exploratory study.
PublikacjaThis study aims to develop an understanding of the use of e-learning courses created for travel agents by Destination Management Organizations (DMOs). It explores agents’ perceptions of such courses. The research examines the views of 304 UK-based travel agents using online survey and investigates whether age, sex, type of agency, work experience, and educational level have influence on e-learning uptake. The satisfaction of travel...
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Anti‐corrosion protection of chimneys and flue gas ducts
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The concept of anti-collision system of autonomous surface vehicle
PublikacjaThe use of unmanned vehicles in various fields of science and the economy is becoming more common. An extremely important aspect of creating this type of solution is to provide autonomous vehicle navigation, which does not require interference of the human factor or in which it is limited to a minimum. This article discusses the concept of autonomous anti-collision system of unmanned surface vehicle. It proposed a sensor system...
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Surface and interfacial anti-plane waves in micropolar solids with surface energy
PublikacjaIn this work, the propagation behaviour of a surface wave in a micropolar elastic half-space with surface strain and kinetic energies localized at the surface and the propagation behaviour of an interfacial anti-plane wave between two micropolar elastic half-spaces with interfacial strain and kinetic energies localized at the interface have been studied. The Gurtin–Murdoch model has been adopted for surface and interfacial elasticity....
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Arsenic-Based Warfare Agents: Production, Use, and Destruction
PublikacjaSince the beginning of time, civilizations have looked for more creative ways to dominate and defeat their enemies. The rapid development of the chemical industry just before the Second World War started the era of modern chemical weapon production based on poisons, including toxic arsenic compounds. This paper provides a detailed overview of the production, usage and destruction of this dangerous chemical weapon. Milestones include:...
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A Review of Traffic Analysis Attacks and Countermeasures in Mobile Agents' Networks
PublikacjaFor traditional, message-based communication, traffic analysis has been already studied for over three decades and during that time various attacks have been recognised. As far as mobile agents’ networks are concerned only a few, specific-scope studies have been conducted. This leaves a gap that needs to be addressed as nowadays, in the era of Big Data, the Internet of Things, Smart Infrastructures and growing concerns for privacy,...
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Anti-Microbiological, Anti-Hyperglycemic and Anti-Obesity Potency of Natural Antioxidants in Fruit Fractions of Saskatoon Berry
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Entangled rendezvous: a possible application of Bell non-locality for mobile agents on networks
PublikacjaRendezvous is an old problem of assuring that two or more parties, initially separated, not knowing the position of each other, and not allowed to communicate, are striving to meet without pre-agreement on the meeting point. This problem has been extensively studied in classical computer science and has vivid importance to modern and future applications. Quantum non-locality, like Bell inequality violation, has shown that in many...
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OPERATION OF TWO-SHAFT GAS TURBINE IN THE RANGE OF OPEN ANTI-SURGE VALVE
PublikacjaThis paper presents experimental tests of full-scale two-shaft gas turbine in the range of open anti-surge valve (ASV). The tests were carried out in a laboratory gas- turbine test stand belonging to Department of Automation and Power Engineering , Faculty of Ocean Engineering and Ship Technology , Gdańsk University of Technology. The tests covered the start-up and low load operation of the turbine set in the range of open...