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Wyniki wyszukiwania dla: antifungal target
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The Antibacterial and Antifungal Textile Properties Functionalized by Bimetallic Nanoparticles of Ag/Cu with Different Structures
PublikacjaWe reported a preparation and characterization of five kinds of impregnation solutions, containing Ag/Cu in the formof bimetallic nanoparticles (alloy and core-shell) as well as ionic species. The cotton-polyester textiles were successfully impregnated during the washing and ironing process by as-prepared solutions to have antibacterial and antifungal properties against to Escherichia coli, Staphylococcus aureus, and Candida albicans....
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Photosensitive and pH-dependent activity of pyrazine-functionalized carbazole derivative as promising antifungal and imaging agent
PublikacjaCarbazole skeleton plays a significant role as a structural scaffold of many pharmacologically active compounds. Pyrazine-functionalized carbazole derivative was constructed by coupling 2-amino-5-bromo-3-methylaminepyrazine (ABMAP) into 3 and 6 positions of the carbazole ring. Multi-experimental methods were used, e.g., potentiometric, spectroscopic (ATR, UV, XRD powder,1H and13C NMR), electrochemical (cyclic voltammetry), and...
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Synthesis and Characterization of Monometallic (Ag, Cu) and Bimetallic Ag-Cu Particles for Antibacterial and Antifungal Applications
PublikacjaIn this paper, the experimental studies are concerned with the effect of the synthesis parameters on the formation of monometallic Ag and Cu nanoparticles (NPs). We consider the synthesis strategies verification for the bimetallic core-shell and alloy particles preparation. It was successfully obtained by chemical reduction method. The obtained colloidal solution is characterized by the transmission electron microscopy (TEM) with...
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Analytical studies on ascosin, candicidin and levorin multicomponent antifungal antibiotic complexes. The stereostructure of ascosin A2
PublikacjaIn the class of polyene macrolides, there is a subgroup of aromatic heptaenes, which exhibit the highest antifungal activity within this type of antibiotics. Yet, due to their complex nature, aromatic heptaenes were not extensively studied and their potential as drugs is currently underexploited. Moreover, there are many inconsistencies in the literature regarding the composition and the structures of the individual components...
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Bearing errors passive sonar stationary target location
PublikacjaPrzedstawiono metodę wyznaczania współrzędnych nieruchomego celu na podstawie namiarów wykonywanych w sonarze pasywnym. Określono wymagania odnośnie ruchu sonaru, przy których błędy wyznaczania współrzędnych są minimalne. Podano zależności umożliwiające analityczne wyznaczanie błędów współrzędnych. Poprawność wyników analizy potwierdzono eksperymentami numerycznymi.
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Neural Manoeuvre Detection of the Tracked Target in ARPA Systems
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Evolution of Animats Following a Moving Target in an Artificial Ecosystem
PublikacjaMany biological animals, even microscopically small, are able to track moving sources of food. In this paper, we investigate the emergence of such behavior in artificial animals (animats) in a 2-dimensional simulated liquid environment. These "predators" are controlled by evolving artificial gene regulatory networks encoded in linear genomes. The fate of the predators is determined only by their ability to gather food and reproduce—no...
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On a threshold induced bias in fish target strength estimation.
PublikacjaPrzedstawiono statystyczny opis zjawiska wpływu progu rejestracji ech od ryb na estymatę siły celu ryb. Pokazano sposób korekcji wykorzystujący zależności pomiędzy funkcjami rozkładu prawdopodobieństwa poziomu echa i charakterystyki wiązki. Przedstawiono wyniki symulacji.
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Telomerase inhibition - unfulfilled hopes in the perfect molecular target
PublikacjaTelomerase plays a pivotal role in cell proliferation, homeostasis, and neoplastic transformation, making it a promising molecular target for cancer chemotherapy. Of note, although hTERT has been explored thoroughly as a target, none of the promising molecules has been approved as a drug until now. The subject of research conducted as part of my doctoral dissertation is explaining the cellular and molecular mechanism of action...
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Xanthone synthetic derivatives with high anticandidal activity and positive mycostatic selectivity index values
PublikacjaWith the current massive increases in drug-resistant microbial infection as well as the significant role of fungal infections in the death toll of COVID-19, discovering new antifungals is extremely important. Natural and synthetic xanthones are promising derivatives, although only few reports have demonstrated their antifungal mechanism of action in detail. Newly synthetized by us xanthone derivative 44 exhibited strong antifungal...
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Inhibitory Effect of Eugenol and trans‐Anethole Alone and in Combination with Antifungal Medicines on Candida albicans Clinical Isolates
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A Central Composite Design in increasing the quercetin content in the aqueous onion waste isolates with antifungal and antioxidant properties
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Synthesis of 2-amino-2,6-dideoxy-D-glucitol-6-sulfonic acid as a potential antifungal agent.
PublikacjaGlucosamine-6P (GlcN-6P) synthase catalyzes the first committed step in the biosynthetic pathway leading to the formation of UDP-GlcNAc, a sugar nucleotide precursor providing D-glucosamine for the formation of chitin and manoproteins. 2-Amino-2,6-dideoxy-D-glucitol-6-sulfonic acid is an analog of 2-amino-2-deoxy-D-glucitol 6-phosphate (GlcN-ol-6-P), a known inhibitor of GlcN-6-P synthase, in which the phosphate group of the latter...
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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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Light-Induced Transformation of the Aromatic Heptaene Antifungal Antibiotic Candicidin D into Its All-Trans Isomer
PublikacjaIllumination of the aromatic heptaene macrolide antifungal antibiotic candicicin D with UV light results in an isomerization of the molecule. The product formed after irradiation of the candicidin complex with UV light (λ=365nm), namely, iso-candicidin D, was isolated and subjected to 2D NMR studies, consisting of DQF-COSY, ROESY, TOCSY, HSQC, and HMBC experiments. The obtained spectral data unambiguously evidenced that iso-candicidin...
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Servo tracking of targets at sea
PublikacjaW artykule przedstawiono propozycje systemu sterowania układem śledzącym umieszczonym na okręcie. Przedstawiono dynamikę błędów śledzenia obiektu we współrzędnych LOS (ang., Line - Of - Sight). Zostało wykazane, że regulacja błędów śledzenia LOS jest możliwa przy pomocy sprzężenia feed-forward od prędkości śledzonego obiektu. Ponieważ prędkość ta nie jest mierzalna zastosowano filtr Kalmana w celu jej estymacji. Ponieważ problem...
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Molecular Targets for Anticandidal Chemotherapy
PublikacjaA relatively small number of anticandidal chemotherapeutics used in clinical practice is at least in part consequence of a limited number of their molecular targets: ergosterol in the membrane, lanosterol demethylase, b(1!3) glucan synthase, and DNA/RNA biosynthesis. Much more potential novel targets have been revealed by the comparative genomic studies identifying essential genes unique for Candida albicans or resulted from recognition...
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Phoenixin as a New Target in the Development of Strategies for Endometriosis Diagnosis and Treatment
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CRL4CRBN E3 Ligase Complex as a Therapeutic Target in Multiple Myeloma
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Oxidative Stress as a Possible Target in the Treatment of Toxoplasmosis: Perspectives and Ambiguities
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On Some Aspects of Fish Target Strength Estimation in Shallow Waters
PublikacjaThe theory of acoustic surveys for determining fish abundance are well established in fishery acoustics. The origins of the estimation are related to overcoming the problem of unknown position of target in the beam using statistical inversion. Although recently researchers use more sophisticated echosounders that provides more informative data allowing for direct solution it is known that the results are biased due to not ideally...
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Fish target strength estimation using multiple echo statistics
PublikacjaW pracy przedstawiono sposób określania statystycznych właściwości charakterystyki wiązki systemu hydroakustycznego z uwzględnieniem możliwości pojawienia się echo wielokrotnych od jednej ryby. Przedstawiono modele obejmujące dwa teoretyczne przypadki związane z wzajemnym ruchem statku i pojedynczej ryby i pokazano, że posiadają one zbliżone właściwości statystyczne. Rozważania teoretyczne potwierdzone są analizą przykładowych...
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Receiver of Doppler multistatic system for moving target detection and tracking
PublikacjaThe article presents a method for solving major structural problems that occur in the receiver used in the multistatic Doppler system, aimed at determination of the trajectory and velocity of a moving target. In the system two transmitters emit acoustic continuous sinusoidal waves at different frequencies. The signals, scattered from a moving target are received by four hydrophones. Beside of the echoes, much larger signals coming...
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Chemical composition and antifungal activity of Chelidonium majus extracts – antagonistic action of chelerythrine and sanguinarine against Botrytis cinerea
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Molecular organization of antifungal antibiotic amphotericin B in lipid monolayers studied by means of Fluorescence Lifetime Imaging Microscopy
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Virulence, antifungal susceptibility and molecular mechanisms of echinocandin resistance among Candida isolates recovered from clinical specimens
PublikacjaFungi of the genus Candida belong to the natural microflora of healthy individuals. However, they can also be a cause of opportunistic infections especially among patients with an impaired immune system. The first line therapy of Candida infections is based on triazoles. However, in recent years there an increase of azole resistant Candida spp., in particular C. glabrata and C. krusei, has been observed. For this reason, echinocandin...
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Quest for the Molecular Basis of Improved Selective Toxicity of All-Trans Isomers of Aromatic Heptaene Macrolide Antifungal Antibiotics
PublikacjaThree aromatic heptaene macrolide antifungal antibiotics, Candicidin D, Partricin A (Gedamycin) and Partricin B (Vacidin) were subjected to controlled cis-trans to all trans photochemical isomerization. The obtained all-trans isomers demonstrated substantially improved in vitro selective toxicity in the Candida albicans cells: human erythrocytes model. This effect was mainly due to the diminished hemotoxicity. The molecular modeling...
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Indirect Methods of Fish Target Strenght Estimation in Absolute and Logarithmic Domain
PublikacjaW artykule przedstawiono wyniki estymacji zasobów ryb realizowane w dziedzinie absolutnej (jako estymacja rozproszenia wstecznego) oraz w dziedzinie logarytmicznej (estymacja siły celu).
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Principles of target DNA cleavage and the role of Mg2+ in the catalysis of CRISPR–Cas9
PublikacjaAt the core of the CRISPR–Cas9 genome-editing technology, the endonuclease Cas9 introduces site-specific breaks in DNA. However, precise mechanistic information to ameliorate Cas9 function is still missing. Here, multimicrosecond molecular dynamics, free energy and multiscale simulations are combined with solution NMR and DNA cleavage experiments to resolve the catalytic mechanism of target DNA cleavage. We show that the conformation...
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Probabilistic Analysis of Structure Models using Target Random Sampling (TRS)
PublikacjaThe work presents testing methods of sensitivity and reliability of mechanical or structural systems. All computations concerned the case of Zigler column, a simple model of a compressed column involving two random variables only. A conclusion was drawn that the standard Monte Carlo method, its reduction variants and the response surface method allow to assess the sensitivity of structural response to the variation of random structural...
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Experimental guinea pig model of dermatophytosis: a simple and useful tool for the evaluation of new diagnostics and antifungals
PublikacjaCelem badań było opracowanie prostego modelu zwierzęcego (świnki morskie) odpowiedniego do sprawdzania systemów diagnostycznych oraz terapii infekcji dermatofitów. Następujące zmienne były analizowane: przygotowanie skóry przez golenie versus użycie taśmy, testowy szczep Microsporum canis czy Trichophyton mentagrophytes jako czynnik etiologiczny, sposób inokulacji. Przebieg infekcji był oceniany poprzez ocenę zaczerwienienia i...
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Genome Mining Revealed a High Biosynthetic Potential for Antifungal Streptomyces sp. S-2 Isolated from Black Soot
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Novel Nystatin A1 derivatives exhibiting low host cell toxicity and antifungal activity in an in vitro model of oral candidosis
PublikacjaOpportunistic oral infections caused by Candida albicans are frequent problems in immunocompromised patients. Management of such infections is limited due to the low number of antifungal drugs available, their relatively high toxicity and the emergence of antifungal resistance. Given these issues, our investigations have focused on novel derivatives of the antifungal antibiotic Nystatin A1, generated by modifications at the amino...
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Intramolecular transformation of an antifungal antibiotic nystatin A1 into its isomer, iso-nystatin A1 - structural and molecular modeling studies
PublikacjaNystatin A1, a polyene macrolide antifungal antibiotic, in a slightly basic or acidic solution undergoes an intramolecular transformation, yielding a structural isomer, the translactonization product, iso-nystatin A1 with lactone ring diminished by two carbon atoms. Structural evidence is provided by advanced NMR and Mass Spectrometry (MS) studies. Molecular dynamics simulations and quantum mechanics calculations gave the insight...
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Human Female Hair Follicles Are a Direct, Nonclassical Target for Thyroid-Stimulating Hormone
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On the possibility of estimating fish length distribution from its target strength statistics.
PublikacjaArtykuł przedstawia koncepcję odtwarzania rozkładu długości ryb na podstawie danych z przeszukiwań akustycznych. Wykorzystując metody odwrotne w statystycznym przetwarzaniu rozkładu siły celu ryb pokazano, że przy pewnych założeniach co do rozkładu położenia ryb w wiązce, możliwa jest estymacja szukanego rozkładu długości ryb.
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Quinoline-based thiazolyl-hydrazones target cancer cells through autophagy inhibition
PublikacjaHeterocyclic pharmacophores such as thiazole and quinoline rings have a significant role in medicinal chemistry. They are considered privileged structures since they constitute several Food and Drug Administration (FDA)-approved drugs for cancer treatment. Herein, we report the synthesis, in silico evaluation of the ADMET profiles, and in vitro investigation of the anticancer activity of a series of novel thiazolyl-hydrazones based...
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How acidic amino acid residues facilitate DNA target site selection
PublikacjaDespite the negative charge of the DNA backbone, acidic residues (Asp/Glu) commonly participate in the base readout, with a strong preference for cytosine. In fact, in the solved DNA/protein structures, cytosine is recognized almost exclusively by Asp/Glu through a direct hydrogen bond, while at the same time, adenine, regardless of its amino group, shows no propensity for Asp/Glu. Here, we analyzed the contribution of Asp/Glu...
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A Target Information Display for Visualising Collision Avoidance Manoeuvres in Various Visibility Conditions
PublikacjaThe paper introduces a new approach to displaying information on targets. The proposed display visualises three types of information: targets’ motion parameters (typical for target tracking), combinations of own course and speed which collide with those targets (typical for Collision Threat Parameters Area display by Lenart (1983)) and combinations of own course and speed which are not compliant with COLREGS in this case (based...
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Homocitrate synthase gene as a new molecular target in diagnostics of Candida spp. infections
PublikacjaNew potential molecular target which will be investigated during this research (homocitrate synthase gen) is the innovative target other than ribosomal DNA. This gene encodes enzyme present only in fungi and some Archaea what significantly increases specificity. It also reduces risk of contamination or influence of other factors (reaction with other DNA present in sample derived from bacteria or host cells) what excludes false...
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Lipophilicity Determination of Antifungal Isoxazolo[3,4-b]pyridin-3(1H)-ones and Their N1-Substituted Derivatives with Chromatographic and Computational Methods
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Amphotericin B derivatives: novel strategy for the development of non-toxic, broad spectrum, fungicidal and overcoming multidrug resistance antifungal agents.
PublikacjaZaprezentowano porównawczą charakterystykę działania amfoterycyny B (AmB) oraz jej pochodnych o różnym stopniu selektywnej toksyczności na szczepy grzybów reperezentujących różne mechanizmy oporności. Były to mutanty C. albicans posiadające defekt w szlaku biosyntezy ergosterolu oraz wielolekooporne szczepy S. cerevisiae wyposażone w pompy eksportujące typu ABC i MFS. Badania obejmowały: 1)porównanie aktywności przeciwgrzybowej...
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New possible pharmacological targets for statins and ezetimibe
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Mechanism of Binding of Antifungal Antibiotic Amphotericin B to Lipid Membranes: An Insight from Combined Single-Membrane Imaging, Microspectroscopy, and Molecular Dynamics
PublikacjaAmphotericin B is a lifesaving polyene antibiotic used in the treatment of systemic mycoses. Unfortunately, the pharmacological applicability of this drug is limited because of its severe toxic side effects. At the same time, the lack of a well-defined mechanism of selectivity hampers the efforts to rationally design safer derivatives. As the drug primarily targets the biomembranes of both fungi and humans, new insights into the...
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A novel in vitro assay for assessing efficacy and toxicity of antifungals using human leukaemic cells infected with Candida albicans
PublikacjaAims: This study describes a novel in vitro assay that simultaneously determines antifungal efficiency and host cell toxicity using suspensions of human leukaemic cells (HL-60) infected with Candida albicans. Methods and Results: The effect of Candida infection on host cell viability was evaluated by the microscopy of trypan blue-stained cells and lactate dehydrogenase (LDH) activity. The in vitro ‘drug potency assay’ utilized...
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CEACAM6 as a Novel Therapeutic Target to Boost HO-1—mediated Antioxidant Defense in COPD
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A comparison of the target tracking in marine navigational radars by means of GRNN filter and numerical filter
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Potential pitfalls of propofol target controlled infusion delivery related to its pharmacokinetics and pharmacodynamics
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Adoptive Cell Therapy—Harnessing Antigen-Specific T Cells to Target Solid Tumours
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Role of Myeloid-derived suppressor cell (MDSC) in autoimmunity and its potential as a therapeutic target
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