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Wyniki wyszukiwania dla: batracylin analogues
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ortho-Fluorobenzanilides and ortho-fluorothiobenzanilides: Molecular conformations and crystal packing
PublikacjaSeries of 2-fluoro and 2,6-difluorobenzanilides and their thiobenzanilide analogs have been synthesized to investigate the influence of the fluorine atom on their crystal structures and self-assembly in the crystal lattice. The X-ray analysis of the single crystal revealed that the synthesized molecules adopt a geometry being deflected from planarity. The deflection was investigated by analysis of dihedral angles between mean planes...
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The crystal and solution studies of glucosamine-6-phosphate synthase from Candida albicans
PublikacjaOkreślono strukturę krystaliczną domeny izomerazowej syntazy glukozamino-6-fosforanu z Candida albicans w stanie natywnym, oraz w kompleksie z inhibitorem allosterycznym UDP-GlcNAc, fruktozo-6-P, glukozo-6-P oraz analogiem stanu przejściowego reakcji enzymatycznej - 2-amino-2-deoksy-D-mannitolo-6-P (ADMP). Na podstawie wyników badań metodą niskokątowego rozpraszania promieni X (SAXS) wydedukowano przypuszczalną strukturę kompletnej...
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Knowledge base views
PublikacjaThe paper introduces an extension to the NeeK language. In the current shape NeeK allows for selection of fragments of a given ontology. The selected part is automatically mapped to a database schema by Data Views implementation. Experience with a real system using Data Views has shown that the resulting database schema does not necessarily reflect the needs of the business logic of an application that uses a specific Data View....
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A note on the Morse homology for a class of functionals in Banach spaces involving the 2p-area functional
PublikacjaIn this paper we show how to construct Morse homology for an explicit class of functionals involving the 2p-area functional. The natural domain of definition of such functionals is the Banach space W_0^{1,2p}(\Omega), where p > n/2 and \Omega \subet R^n is a bounded domain with sufficiently smooth boundary. As W_0^{1,2p}(\Omega) is not isomorphic to its dual space,critical points of such functionals cannot be non-degenerate...
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Electron-Induced Decomposition of Uracil-5-yl O-(N,N-dimethylsulfamate): Role of Methylation in Molecular Stability
PublikacjaThe incorporation of modified uracil derivatives into DNA leads to the formation of radical species that induce DNA damage. Molecules of this class have been suggested as radiosensitizers and are still under investigation. In this study, we present the results of dissociative electron attachment to uracil-5-yl O-(N,N-dimethylsulfamate) in the gas phase. We observed the formation of 10 fragment anions in the studied range of electron...
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From Knowledge based Vision Systems to Cognitive Vision Systems: A Review
PublikacjaComputer vision research and applications have their origins in 1960s. Limitations in computational resources inherent of that time, among other reasons, caused research to move away from artificial intelligence and generic recognition goals to accomplish simple tasks for constrained scenarios. In the past decades, the development in machine learning techniques has contributed to noteworthy progress in vision systems. However,...
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The effect of nitrogen on the structure and thermal properties of beryllium-containing Na-(Li)-Si-O-N glasses
PublikacjaTwo oxynitride glass series with the composition of 35Na2O-5BeO-(60-x)SiO2-xSi3N4 and 9Li2O- 27Na2O-5BeO-(59-x)SiO2-xSi3N4, were prepared. The glasses' topography and structure were studied by Scanning Electron Microscopy and Raman spectroscopy. The composition was analyzed by Inductively Coupled Plasma Optical Emission Spectrometer, SEM-EDS and nitrogen and oxygen elemental analyzer. Na-(Li)-Be-silicate glasses were found to contain...
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Design Equation for Stirring Fluid by a Stream Pump in a Circulating Tank
PublikacjaA circulating tank is a very useful theoretical scheme for many fluid-flow objects in several branches of engineering. The motion of the fluid in such objects can be induced in different ways. A stream pump provides an especially interesting possibility; however, the quantitative description of such devices shows some shortcomings. Such a device is analogous to a jet pump, thus has similar advantages (simplicity of construction,...
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Quantifying Contextuality
PublikacjaContextuality is central to both the foundations of quantum theory and to the novel information processing tasks. Despite some recent proposals, it still faces a fundamental problem: how to quantify its presence? In this work, we provide a universal framework for quantifying contextuality. We conduct two complementary approaches: (i) the bottom-up approach, where we introduce a communication game, which grasps the phenomenon of...
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Multi-mode vibronic interactions in the five lowest electronic states of the fluorobenzene radical cation
PublikacjaThe multi-mode vibronic interactions between the five lowest electronic states of the fluorobenzene radical cation are investigated theoretically, based on ab initio electronic structure data, and employing the linear vibronic coupling model. Low-energy conical intersections, and strong vibronic couplings are found to prevail within the set of X-A and B-C-D cationic states, while the interactions between these two sets of states...
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The Multiplatform Environment for Simulation and Features Estimation of Mixed-Signal Devices
PublikacjaThe use of simulation laboratories is gaining popularity in thedomains of engineering programs. However, the experience in teaching showsthat the simulation itself is not very effective in didactic processes. Teachingprocesses in thefield of specialist subjects, designed for students of technicaluniversities, should be based on direct operations performed by the student onreal devices. At the same time, at the later stages of didactic...
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Artificial Intelligence Aided Architectural Design
PublikacjaTools and methods used by architects always had an impact on the way building were designed. With the change in design methods and new approaches towards creation process, they became more than ever before crucial elements of the creation process. The automation of architects work has started with computational functions that were introduced to traditional computer-aided design tools. Nowadays architects tend to use specified tools...
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Exploring the cocrystallization potential of urea and benzamide
PublikacjaThe cocrystallization landscape of benzamide and urea interacting with aliphatic and aromatic carboxylic acids was studied both experimentally and theoretically. Ten new cocrystals of benzamide were synthesized using an oriented samples approach via a fast dropped evaporation technique. Information about types of known bi-component cocrystals augmented with knowledge of simple binary eutectic mixtures was used for the analysis...
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Anticancer Properties of Amino Acid and Peptide Derivatives of Mycophenolic Acid
PublikacjaBackground: Although Mycophenolic Acid (MPA) is applied as prodrugs in clinic as an immunosuppressant, it also possesses anticancer activity. MPA acts as Inosine-5’-Monophosphate Dehydrogenase (IMPDH) inhibitor, where the carboxylic group at the end of the side chain interacts with Ser 276 of the enzyme via hydrogen bonds. Therefore, MPA derivatives with other polar groups indicated high inhibition too. On the other hand, potent...
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Characterization of recombinant homocitrate synthase from Candida albicans
PublikacjaLYS21 and LYS22 genes from Candida albicans encoding isoforms of homocitrate synthase (HCS), an enzyme catalyzing the first committed step in the L-lysine biosynthetic pathway, were cloned and expressed as NoligoHistagged fusion proteins in Escherichia coli. The purified gene products revealed HCS activity, i.e. catalyzed the condensation of α-ketoglutarate with acetyl-coenzyme A to yield homocitrate. The recombinant enzymes were purified...
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Molecular basis for the DNA damage induction and anticancer activity of asymmetrically substituted anthrapyridazone PDZ-7
Publikacjanthrapyridazones, imino analogues of anthraquinone, constitute a family of compounds with remarkable anti-cancer activity. To date, over 20 derivatives were studied, of which most displayed nanomolar cytotoxicity towards broad spectrum of cancer cells, including breast, prostate and leukemic ones. BS-154, the most potent derivative, had IC50 values close to 1 nM, however, it was toxic in animal studies. Here, we characterize another...
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Comparison of the coordination geometries of Zn(II) and Cd(II) ions in complexes with water, methanol and bulky aryloxysilanethiolate ligands
PublikacjaZinc and cadmium complexes containing silanethiolate anions and methanol or water were synthesized and characterized by X-ray diffraction, FT-IR and NMR spectroscopy, and DFT calculations. Contrary to zinc, the cadmium ion utilizes very weak donors to complete its coordination sphere; it forms contacts to phenyl rings of the silanethiolate ligand. Two zinc analogs of the general formula [Zn{SSi(OAr)3}2(L)2] where L = CH3OH (2)...
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Two-spinors, oscillator algebras, and qubits: aspects of manifestly covariant approach to relativistic quantum information
PublikacjaThe first part of the paper reviews applications of 2-spinor methods to relativistic qubits (analogies between tetrads in Minkowski space and 2-qubit states, qubits defined by means of null directions and their role for elimination of the Peres-Scudo-Terno phenomenon, advantages and disadvantages of relativistic polarization operators defined by the Pauli-Lubanski vector, manifestly covariant approach to unitary representations...
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Non-Gaussian Resistance Fluctuations in Gold-Nanoparticle-Based Gas Sensors: An Appraisal of Different Evaluation Techniques
PublikacjaVolatile organic compounds, such as formaldehyde, can be used as biomarkers in human exhaled breath in order to non-invasively detect various diseases, and the same compounds are of much interest also in the context of environmental monitoring and protection. Here, we report on a recently-developed gas sensor, based on surface-functionalized gold nanoparticles, which is able to generate voltage noise with a distinctly non-Gaussian...
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Corrosion fatigue crack propagation rate characteristics for weldable ship and offshore steels with regard to the influence of loading frequency and seawater temperature
PublikacjaAfter Vosikovsky (1975), the corrosion fatigue crack growth rate (CFCGR) characteristics have been divided into three regions. The region-III rates are very close to mechanical fatigue crack growth rates. CFCGR formulae, including the long-crack length effect (in region I only), the loading frequency effect (in region II only), and the saltwater temperature effect, have been proposed. It has been assumed that CFCGR is proportional...
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New insights on lithium storage in silicon oxycarbide/carbon composites: Impact of microstructure on electrochemical properties
PublikacjaIn this work, we study the impact of the preceramic precursor vinyltriethoxysilane (VTES) on the electrochemical performance of silicon oxycarbide (SiOC) glass/graphite composites. We apply an innovative approach based on high-power ultrasounds in order to obtain highly homogenous composites with a uniform distribution of small graphitic flakes. This procedure enhances gelation and drying of VTES-based preceramic polymer/graphite...
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Superconductivity in the Cu(Ir1-xPtx)2Se4 spinel
PublikacjaWe report the observation of superconductivity in the CuIr2Se4 spinel induced by partial substitution of Pt for Ir. The optimal doping level for superconductivity in Cu(Ir1-xPtx )2Se4 is x = 0.2, where Tc is 1.76 K. A superconducting Tc vs composition dome is established between the metallic, normal conductor CuIr2Se4 and semiconducting CuIrPtSe4. Electronic structure calculations show that the optimal Tc occurs near the electron count...
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PTD4 Peptide Increases Neural Viability in an In Vitro Model of Acute Ischemic Stroke
PublikacjaIschemic stroke is a disturbance in cerebral blood flow caused by brain tissue ischemia and hypoxia. We optimized a multifactorial in vitro model of acute ischemic stroke using rat primary neural cultures. This model was exploited to investigate the pro-viable activity of cell-penetrating peptides: arginine-rich Tat(49–57)-NH2 (R49KKRRQRRR57-amide) and its less basic analogue, PTD4 (Y47ARAAARQARA57-amide). Our model included glucose...
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A New Rehabilitation Device for Balance Impaired Individuals
PublikacjaIn the paper authors present a device designed to improve the rehabilitation process of people with balance impairment. The discussed device (JStep) utilizes a commercially available static standing frame (stander) modified in order to fit force sensing units under the feet and in the pillows around the hips of a patient. While executing rehabilitation tasks, the patient may compensate his balance deficiency by leaning on the pillows...
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Preparation and characterization of dummy-template molecularly imprinted polymers as potential sorbents for the recognition of selected polybrominated diphenyl ethers
PublikacjaThe main aim of this work was to conduct the preliminary/basic research concerning the preparation process of a new dummy molecularly imprinted polymer (DMIP) materials. Developed DMIPs were proposed as a sorption material in solid-phase extraction (SPE) technique for recognition of selected low mass polybrominated diphenyl ethers (PBDEs) e PBDE-47 and PBDE-99. Four new DMIPs were synthesized employing bulky polymerization technique...
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Experimental and Machine-Learning-Assisted Design of Pharmaceutically Acceptable Deep Eutectic Solvents for the Solubility Improvement of Non-Selective COX Inhibitors Ibuprofen and Ketoprofen
PublikacjaDeep eutectic solvents (DESs) are commonly used in pharmaceutical applications as excellent solubilizers of active substances. This study investigated the tuning of ibuprofen and ketoprofen solubility utilizing DESs containing choline chloride or betaine as hydrogen bond acceptors and various polyols (ethylene glycol, diethylene glycol, triethylene glycol, glycerol, 1,2-propanediol, 1,3-butanediol) as hydrogen bond donors. Experimental...
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Experimental and Machine-Learning-Assisted Design of Pharmaceutically Acceptable Deep Eutectic Solvents for the Solubility Improvement of Non-Selective COX Inhibitors Ibuprofen and Ketoprofen
PublikacjaDeep eutectic solvents (DESs) are commonly used in pharmaceutical applications as excellent solubilizers of active substances. This study investigated the tuning of ibuprofen and ketoprofen solubility utilizing DESs containing choline chloride or betaine as hydrogen bond acceptors and various polyols (ethylene glycol, diethylene glycol, triethylene glycol, glycerol, 1,2-propanediol, 1,3-butanediol) as hydrogen bond donors. Experimental...
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Stan graniczny nośności dźwigara żelbetowego mostu na zginanie według norm PN-EN 1992-2 oraz PN-S-10042:1991
PublikacjaPraca włącza się w bogaty w ostatnich latach w krajowym piśmiennictwie nurt porównań dwóch generacji norm projektowania mostów z betonu: polskiej - wycofanej, aczkolwiek powszechnie stosowanej oraz europejskiej – wciąż jeszcze wdrażanej do praktyki projektowej. Nowością w stosunku do dotychczasowych publikacji polskich jest szersze ujęcie różnic pomiędzy obydwiema generacjami norm. Poza rozpatrywanymi przez wielu autorów różnicami...
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Identification of novel halogenated naturally occurring compounds in marine biota by high-resolution mass spectrometry and combined screening approaches
PublikacjaMarine animals, plants or bacteria are a source of bioactive naturally-occurring halogenated compounds (NHCs) such as bromophenols (BPs), bromoanisoles (BAs) and hydroxylated or methoxylated analogues of polybrominated diphenyl ethers (HO-PBDEs, MeO-PBDEs) and bromobiphenyls (HO-BBs, MeO-BBs). This study applied a comprehensive screening approach using liquid chromatography high-resolution mass spectrometry and combining target,...
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Theory versus experiment for vacuum Rabi oscillations in lossy cavities
PublikacjaThe 1996 experiment by Brune et al. [Phys. Rev. Lett. 76, 1800 (1996)] on vacuum Rabi oscillation is analyzed by means of alternative models of atom-reservoir interaction. Agreement with experimental Rabi oscillation data can be obtained if one defines jump operators in the dressed-state basis and takes into account thermal fluctuations between dressed states belonging to the same manifold. Such low-frequency transitions could...
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Modelling tunnelling-induced deformation in stiff soils with a hyperelastic–plastic anisotropic model
PublikacjaIn this paper, the tunnelling-induced deformation in anisotropic stiff soils is analysed using FE modelling. The influence of material description is investigated rather than an advanced simulation of the tunnelling method. A new hyperelastic– plastic model is proposed to describe the anisotropic mechanical behaviour of stiff highly overconsolidated soil. This model can reproduce the superposition of variable stress-induced anisotropy...
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Hidden Tensor Structures
PublikacjaAny single system whose space of states is given by a separable Hilbert space is automatically equipped with infinitely many hidden tensor-like structures. This includes all quantum mechanical systems as well as classical field theories and classical signal analysis. Accordingly, systems as simple as a single one-dimensional harmonic oscillator, an infinite potential well, or a classical finite-amplitude signal of finite duration...
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The influence of the type of halogen substituent and its position on the molecular conformation, intermolecular interactions and crystal packing for a series of 1-benzoyl-3-(halogenophenyl)thioureas
PublikacjaBy the reaction of benzoyl chloride, potassium isothiocyanate and the appropriate halogenoaniline, i.e. 2/3/4-(bromo/iodo)aniline, we have obtained five new 1-benzoyl-3-(halogenophenyl)thioureas, namely, 1-benzoyl-3-(2-bromophenyl)- thiourea and 1-benzoyl-3-(3-bromophenyl)thiourea, C14H11BrN2OS, and 1-benzoyl-3-(2-iodophenyl)thiourea, 1-benzoyl-3-(3-iodophenyl)thiourea and 1-benzoyl-3-(4-iodophenyl)thiourea, C14H11IN2OS. Structural...
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Reinforcement Learning Algorithm and FDTD-based Simulation Applied to Schroeder Diffuser Design Optimization
PublikacjaThe aim of this paper is to propose a novel approach to the algorithmic design of Schroeder acoustic diffusers employing a deep learning optimization algorithm and a fitness function based on a computer simulation of the propagation of acoustic waves. The deep learning method employed for the research is a deep policy gradient algorithm. It is used as a tool for carrying out a sequential optimization process the goal of which is...
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Fast GC as a useful tool for authenticity assessment of kiwifruit
PublikacjaKiwifruit is one of the healthiest fruits due to its high content of biologically active substances and nutrients. The most popular species of Actinidia (kiwifruit) are the Actinidia deliciosa fruits called kiwi and Actinidia chinensis commonly called golden kiwi, while the lesser known species is Actinidia arguta known as mini kiwi. Bioactivities and nutrients of Actinidia are influenced by species and cultivars. It is very important...
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Application of Electronic Nose Based on Fast GC for Authenticity Assessment of Polish Homemade Liqueurs Called Nalewka
PublikacjaThe possibility of application of electronic nose based on fast GC for differentiation of three types of cherry liqueurs, namely Polish homemade liqueurs called nalewka, commercially available liqueurs labeled as nalewka, and commercial liqueurs, was investigated. This device was equipped with two parallel connected columns with different stationary phases coupled to two ultrasensitive flame ionization detectors (μ-FIDs). Four...
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Evaluation of the suitability of electronic nose based on fast GC for distinguishing between the plum spirits of different geographical origins
PublikacjaPlum spirits are obtained exclusively via the alcoholic fermentation and distillation of meaty plums or must composed of plums, with or without stones. The European countries such as Poland, the Slovak Republic, the Czech Republic, Bulgaria and Romania are the leading producers of this alcoholic beverage. Information about the authentication of plum spirits produced in different countries can be found in the published literature....
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Synthesis of bicoumarin thiophosphate derivatives as steroid sulfatase inhibitors
PublikacjaBased on the frameworks of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy- 7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c] chromen-6-one, a series of bicoumarin thiophosphate analogs have been synthesized and biologically evaluated. Additionally, their binding modes have been modeled using docking techniques. The inhibitory properties of the synthesized compounds...
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Synthesis and steroid sulfatase inhibitory activities of N-alkanoyl tyramine phosphates and thiophosphates
PublikacjaA series of phosphate and thiophosphate analogs based on the frameworks of N-alkanoyl tyramines have been synthesized and biologically evaluated. Their binding modes have been modeled using docking techniques. The inhibitory effects of the synthesized compounds were tested on STS isolated from the human placenta as well as the MCF-7, MDA-MB-231 and SkBr3 cancer cell lines. Most of the new STS inhibitors possessed potent activity...
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Exploring the Antitumor Efficacy of N-Heterocyclic Nitrilotriacetate Oxidovanadium(IV) Salts on Prostate and Breast Cancer Cells
PublikacjaThe crystal structures of two newly synthesized nitrilotriacetate oxidovanadium(IV) salts, namely [QH][VO(nta)(H2O)](H2O)2 (I) and [(acr)H][VO(nta)(H2O)](H2O)2 (II), were determined. Additionally, the cytotoxic effects of four N-heterocyclic nitrilotriacetate oxidovanadium(IV) salts— 1,10-phenanthrolinium, [(phen)H][VO(nta)(H2O)](H2O)0.5 (III), 2,2′-bipyridinium [(bpy)H][VO(nta)(H2O)](H2O) (IV), and two newly synthesized compounds...
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Comparative analysis of mRNA transcripts of HT-29 cell line expressed in identical quantities for pathogenic E. coli strains UM146 and UM147 with control Escherichia coli Nissle 1917
PublikacjaAim of study was comparative analysis of mRNA transcripts of HT-29 cell line, expressed in identical quantities for the combination of pathogenic and non-pathogenic Escherichia coli strains. HT-29 confluent monolayers infection with two pathogenic E. coli strains UM146 and UM147 resulted in two sets of mRNA transcripts that were identical with RNA transcripts obtained for non-pathogenic one strain E. coli Nissle 1917. In this study...
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Dimeric structure of the N-terminal domain of PriB protein from Thermoanaerobacter tengcongensis solved ab initio
PublikacjaPriB is one of the components of the bacterial primosome, which catalyzes the reactivation of stalled replication forks at sites of DNA damage. The N-terminal domain of the PriB protein from the thermophilic bacterium Thermoanaerobacter tengcongensis (TtePriB) was expressed and its crystal structure was solved at the atomic resolution of 1.09 Å by direct methods. The protein chain, which encompasses the first 104 residues of the...
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Low-Barrier Hydrogen Bond Determines Target-Binding Affinity and Specificity of the Antitubercular Drug Bedaquiline
PublikacjaThe role of short strong hydrogen bonds (SSHB) in ligand-target binding remains largely unexplored, thereby hin- dering a potentially important avenue in the rational drug de- sign. Here, we investigate the interaction between bedaquiline (Bq), a potent anti-tuberculosis drug, and the mycobacterial ATP synthase, to unravel the role of a specific hydrogen bond to a conserved acidic residue in the target affinity and specificity....
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The Quantum Efficiency Roll-Off Effect in Near-Infrared Organic Electroluminescent Devices with Iridium Complexes Emitters
PublikacjaThe electroluminescence quantum efficiency roll-off in iridium(III)-based complexes, namely Ir(iqbt)2(dpm) and Ir(iqbt)3(iqbt=1 (benzo[b]thiophen-2-yl)-isoquinolinate, dpm=2,2,6,6-tetramethyl-3,5-heptanedionate) utilized as near-infrared emitters in organic light emitting diodes with remarkable external quantum efficiencies, up to circa 3%, 1.5% and 1%, are measured and analyzed. With a 5–6 weight % of emitters embedded...
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Superconductivity in the Nb-Ru-Ge σ phase
PublikacjaWe show that the previously unreported ternary σ-phase material Nb20.4Ru5.7Ge3.9 (Nb0.68Ru0.19Ge0.13) is a superconductor with a critical temperature of 2.2 K. Temperature-dependent magnetic susceptibility, resistance, and specific-heat measurements were used to characterize the superconducting transition. The Sommerfeld constant γ for Nb20.4Ru5.7Ge3.9 is 91 mJ mol f.u. −1K−2 (∼3 mJ mol atom−1 K−2) and the specific-heat anomaly at...
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GNSS INVENTORY OF HISTORIC NARROW-GAUGE RAILWAY LINE IN KOSZALIN UNDER EXTREMELY UNFAVORABLE MEASUREMENTS CONDITIONS FROM THE POINT OF VIEW OF SATELLITE SIGNALS AVAILABILITY
PublikacjaA team of academic researchers from the Gdańsk University of Technology, Gdynia Maritime University and the Polish Naval Academy have been working since 2009 on the methodology of using active GNSS geodetic networks for geodetic inventory of railways and on adapting this measurement technique for designing geometric layouts of railway and tram lines. Over the years, the team tested a variety of configurations of receivers and settings...
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Fluconazole resistant Candida auris clinical isolates have increased levels of cell wall chitin and increased susceptibility to a glucosamine-6-phosphate synthase inhibitor
PublikacjaIn 2009 Candida auris was first isolated as fungal pathogen of human disease from ear canal of a patient in Japan. In less than a decade, this pathogen has rapidly spread around the world and has now become a major health challenge that is of particular concern because many strains are resistant to multiple class of antifungal drugs. The lack of available antifungals and rapid increase of this fungal pathogen provides an incentive...
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Reactions of (Ph)tBuP-P(SiMe3)Li·3THF with [(PNP)TiCl2] and [MeNacNacTiCl2·THF]. Synthesis of first PNP titanium(IV) complex with phosphanylphosphinidene ligand [(PNP)Ti(Cl){η2-P-P(Ph)tBu}]
PublikacjaLithium derivative of diphosphane (Ph)tBuP-P(SiMe3)Li (1) was isolated for the first time and investigated in reactions with β-diketiminate (MeNacnac− = [Ar]NC(Me)CHC(Me)N[Ar]; Ar = 2,6-iPr2C6H3) and PNP-pincer (PNP = N[2-PiPr2-4-methylphenyl]2) Ti(III) complexes. The β-diketiminate titanium(III) complex containing phosphanylphosphido ligand [MeNacNacTi(Cl){η2-P(SiMe3)-P(Ph)tBu}] (2) was prepared in reaction of [MeNacNacTiCl2·THF]...
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Antibiotic-Based Conjugates Containing Antimicrobial HLopt2 Peptide: Design, Synthesis, Antimicrobial and Cytotoxic Activities
PublikacjaRecent studies have shown that modified human lactoferrin 20−31 fragment, named HLopt2, possesses antibacterial and antifungal activity. Thus, we decided to synthesize and evaluate the biological activity of a series of conjugates based on this peptide and one of the antimicrobials with proven antibacterial (ciprofloxacin, CIP, and levofloxacin, LVX) or antifungal (fluconazole, FLC) activity. The drugs were covalently connected...
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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...