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Chiral Pyrazolo[4,3-e][1,2,4]triazine Sulfonamides—Their Biological Activity, Lipophilicity, Protein Affinity, and Metabolic Transformations
PublicationReferring to our previous laboratory results related to the tyrosinase and urease inhibition by pyrazolo[4,3-e][1,2,4]triazine sulfonamides, we examined here in silico the mechanism of action at the molecular level of the investigated pyrazolotriazine sulfonamides by the molecular docking method. The studied compounds being evaluated for their cytotoxic effect against cancer cell lines (MCF-7, K-562) and for recombinant Abl and...
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Budesonide treatment of professional athletes and anti-doping testing- case studies
PublicationAccording to the World Anti-Doping Agency (WADA) Prohibited List, glucocorticosteroids are prohibited in competition and only when administered by oral, intravenous, intramuscular or rectal routes. Up to now, in order to differentiate whether glucocorticosteroids were administered by one of the prohibited routes or not, a specific reporting limit for urinary concentrations of parent compounds and their metabolites was established...
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Online Interactivity – Shift Towards E-textbook-based Medical Education
PublicationTextbooks have played the leading role in academic education for centuries and their form has evolved, adapting to the needs of students, teachers and technological possibilities. Advances in technology have caused educators to look for new sources of knowledge development, which students could use inside and outside the classroom. Today’s sophisticated learning tools range from virtual environments to interactive multimedia resources,...
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Aptamer based tools for environmental and therapeutic monitoring: A review of developments, applications, future perspectives
PublicationNucleic acids in the form of aptamers play a growing and significant role in the targeted and rapid analysis of environmental sample composition and medical analyses. In this paper, the review of both aptamers synthesis methods as well as application of these short chain oligonucleotides (with critical comments on their strong and weak features) are given. The first ones include: systematic evolution of ligands by exponential enrichment...
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Why do G-quadruplexes dimerize through the 5’-ends? Driving forces for G4 DNA dimerization examined in atomic detail
PublicationG-quadruplexes (G4) are secondary structures formed by guanine-rich nucleic acid sequences and shown to exist in living cells where they participate in regulation of gene expression and chromosome maintenance. G-quadruplexes with solvent-exposed guanine tetrads show the tendency to associate together through cofacial stacking, which may be important for packaging of G4-forming sequences and allows for the design of higher-order...
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Receptor for advanced glycation end‐products: Biological significance and imaging applications
PublicationThe receptor for advanced glycation end-products (RAGE or AGER) is a transmembrane, immunoglobulin-like receptor that, due to its multiple isoform structures, binds to a diverse range of endo- and exogenous ligands. RAGE activation caused by the ligand binding initiates a cascade of complex pathways associated with producing free radicals, such as reactive nitric oxide and oxygen species, cell proliferation, and immunoinflammatory...
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Pre-analytical aspects in metabolomics of human biofluids – sample collection, handling, transport, and storage
PublicationMetabolomics is the field of omics research that offers valuable insights into the complex composition of biological samples. It has found wide application in clinical diagnostics, disease investigation, therapy prediction, monitoring of treatment efficiency, drug discovery, or in-depth analysis of sample composition. A suitable study design constitutes the fundamental requirements to ensure robust and reliable results from the...
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Pathogenesis of psoriasis in the “omic” era. Part II. Genetic, genomic and epigenetic changes in psoriasis
PublicationPsoriasis is a multifactorial disease in which genetic, environmental and epigenetic factors regulating gene expression play a key role. In the “genomic era”, genome-wide association studies together with target genotyping platforms performed in different ethnic populations have found more than 50 genetic susceptible markers associated with the risk of psoriasis which have been identified so far. Up till now, the strongest association...
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Synthesis of Combretastatin A-4 Analogs and their Biological Activities
PublicationCombretastatin A-4 (CA-4) is a natural product, which consists of two phenyl rings, linked by an ethylene bridge. CA-4, inhibitor of polymerization of tubulin to microtubules, possesses a strong antitumor and anti-vascular properties both in vitro and in vivo. Previous studies showed that disodium phosphate salt of CA-4, a water-soluble prodrug is well tolerated at therapeutically useful doses. However, it should be noted that...
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DNA methylation analysis of benign and atypical meningiomas: correlation between RUNX3 methylation and WHO grade
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Novel therapeutic compound acridine–retrotuftsin action on biological forms of melanoma and neuroblastoma
PublicationPURPOSE: As a continuation of our search for anticancer agents, we have synthesized a new acridine-retrotuftsin analog HClx9-[Arg(NO2)-Pro-Lys-Thr-OCH3]-1-nitroacridine (named ART) and have evaluated its activity against melanoma and neuroblastoma lines. Both tumors develop from cells (melanocytes, neurons) of neuroectodermal origin, and both are tumors with high heterogeneity and unsatisfactory susceptibility to chemotherapies....
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ADT in mammography
PublicationWe discuss limitations of the known methods of IR imaging in diagnostics of breast cancer. In conclusion we show that for practical reasons one requires new approaches because the known methods based on simple observation of external temperature distribution are not fully effective. Even advanced pattern recognition could not help too much for static images. We ask the question: may active dynamic thermography, known in nondestructive...
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Isothiocyanates may chemically detoxify mutagenic amines formed in heat processed meat
PublicationMeat consumption represents a dietary risk factor increasing the incidence of common cancers, probably due to carcinogenic amines (HAAs) formed upon meat heating. Interestingly, cancers whose incidence is increased by meat consumption, are decreased in populations consuming brassica vegetables regularly. This inverse correlation is attributed to brassica anticarcinogenic components, especially isothiocyanates (ITCs) that stimulate...
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Genetic predisposition to inflammatory bowel disease
PublicationInflammatory bowel disease (IBD) is a chronic, incurable inflammatory disease of the digestive system. The two main disease entities included in the IBD are ulcerative colitis and Crohn's disease. According to epidemiological studies there are more and more new cases every year. In especially among the youngest patients with symptoms of malnutrition and growth inhibition to land up in hospitalwith cancer suspected. The purpose...
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Explicit solvent repulsive scaling replica exchange molecular dynamics ( RS‐REMD ) in molecular modeling of protein‐glycosaminoglycan complexes
PublicationGlycosaminoglcyans (GAGs), linear anionic periodic polysaccharides, are crucial for many biologically relevant functions in the extracellular matrix. By interacting with proteins GAGs mediate processes such as cancer development, cell proliferation and the onset of neurodegenerative diseases. Despite this eminent importance of GAGs, they still represent a limited focus for the computational community in comparison to other classes...
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Hydroperoxyl radical and formic acid formation from common DNA stabilizers upon low energy electron attachment
Publication2-Amino-2-(hydroxymethyl)-1,3-propanediol (TRIS) and ethylenediaminetetraacetic acid (EDTA) are key components of biological buffers and are frequently used as DNA stabilizers in irradiation studies. Such surface or liquid phase studies are done with the aim to understand the fundamental mechanisms of DNA radiation damage and to improve cancer radiotherapy. When ionizing radiation is used, abundant secondary electrons are formed...
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Triazoloacridone C-1305 impairs XBP1 splicing by acting as a potential IRE1α endoribonuclease inhibitor
PublicationInositol requiring enzyme 1 alpha (IRE1α) is one of three signaling sensors in the unfolding protein response (UPR) that alleviates endoplasmic reticulum (ER) stress in cells and functions to promote cell survival. During conditions of irrevocable stress, proapoptotic gene expression is induced to promote cell death. One of the three signaling stressors, IRE1α is an serine/threonine-protein kinase/endoribonuclease (RNase) that...
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Release of Encapsulated Bioactive Compounds from Active Packaging/Coating Materials and Its Modeling: A Systematic Review
PublicationThe issue of achieving controlled or targeted release of bioactive compounds with specific functional properties is a complex task that requires addressing several factors, including the type of bioactive, the nature of the delivery system, and the environmental conditions during transportation and storage. This paper deals with extensive reporting for the identification of original articles using Scopus and Google Scholar based...
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eFRADIR: An Enhanced FRAmework for DIsaster Resilience
PublicationThis paper focuses on how to increase the availability of a backbone network with minimal cost. In particular, the new framework focuses on resilience against natural disasters and is an evolution of the FRADIR/FRADIR-II framework. It targets three different directions, namely: network planning, failure modeling, and survivable routing. The steady state network planning is tackled by upgrading a sub-network (a set of links termed...
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Recent advancements in molecularly imprinted polymers for the removal of heavy metal ions and dyes
PublicationContamination set off by highly toxic metal ions and dyes is a big threat to the environment and living beings. Various industries like metal plating, mining, pesticides, battery manufacturing, and dyeing release metal ions and toxic dyes directly into the water. It is necessary to remove these toxic substances from the environment. Molecular imprinting technology (MIT) got a lot of attention in the last two decades because of...
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Parallelization of large vector similarity computations in a hybrid CPU+GPU environment
PublicationThe paper presents design, implementation and tuning of a hybrid parallel OpenMP+CUDA code for computation of similarity between pairs of a large number of multidimensional vectors. The problem has a wide range of applications, and consequently its optimization is of high importance, especially on currently widespread hybrid CPU+GPU systems targeted in the paper. The following are presented and tested for computation of all vector...
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Impact evaluation of a cycling promotion campaign using daily bicycle counters data: The case of Cycling May in Poland
PublicationThe promotion of active and sustainable transport modes as an alternative to motorised individual transport has become a key policy priority in Europe, to reduce air pollution, road congestion, noise, traffic injuries, and the adverse health outcomes of sedentary lifestyles. Policymakers are implementing a wide range of measures to encourage this shift in attitudes and behaviours. These interventions are most valuable when targeting...
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Exergy and Energy Analyses of Microwave Dryer for Cantaloupe Slice and Prediction of Thermodynamic Parameters Using ANN and ANFIS Algorithms
PublicationThe study targeted towards drying of cantaloupe slices with various thicknesses in a microwave dryer. The experiments were carried out at three microwave powers of 180, 360, and 540 W and three thicknesses of 2, 4, and 6 mm for cantaloupe drying, and the weight variations were determined. Artificial neural networks (ANN) and adaptive neuro-fuzzy inference systems (ANFIS) were exploited to investigate energy and exergy indices of...
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Antimicrobial resistance of fecal indicators in disinfected wastewater
PublicationThe main objective of the study was to assess the potential of three systems (UV irradiation, ozonation, and micro/ultrafiltration) operated in a pilot scale in removal of antimicrobial-resistant fecal bacteria from secondary effluent of the local wastewater treatment plant (700,000 population equivalent). The effectiveness of the processes was analysed using the removal ratio of fecal indicators (Escherichia coli and Enterococcus...
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The Usefulness of Cyclic Diamidines with Different Core-substituents as Antitumor Agents
PublicationA series of related polycationic compds. has been screened for potential antitumor activity by the NCI's in vitro testing (one dose primary anticancer assay and the NCI-60 full panel screening). The GI50 values of triazines 3 and 4 are on av. 1.9 μM and 2.4 μM, resp. Furan 8 deserves mention too (1.9 μM). The biol. test results showed that carbazole 10 possessed cytotoxic activity in the nanomolar range, much better than...
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Metal nanoparticles-assisted early diagnosis of diseases
PublicationEarly diagnosis is essential for the effective illness treatment, but traditional diagnostic approaches inevitably have major downsides. Recent advancements in nanoparticle-based biosensors have created new opportunities for accelerating diagnosis. High surface area, exceptional sensitivity, high specificity, and optical characteristics of metal and metal oxide nanoparticles have made it possible to detect a variety of health conditions...
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Poloxamer: A versatile tri-block copolymer for biomedical applications
PublicationPoloxamers, also called Pluronic, belong to a unique class of synthetic tri-block copolymers containing central hydrophobic chains of poly(propylene oxide) sandwiched between two hydrophilic chains of poly(ethylene oxide). Some chemical characteristics of poloxamers such as temperature-dependent self-assembly and thermo-reversible behavior along with biocompatibility and physiochemical properties make poloxamer-based biomaterials...
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Antipsychotic drug prescription sequence analysis in relation to death occurrence and cardiometabolic drug usage: A retrospective longitudinal study
PublicationThe potential role of antipsychotics in increasing cardiovascular risk of mortality is still debated. The aim of this study was to assess the death risk associated with sequences of first-generation antipsychotic (FGA) and second-generation antipsychotic (SGA) prescriptions, including clozapine and lithium, and drugs for cardiometabolic diseases. We conducted a retrospective longitudinal analysis involving 84,881 patients who received...
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Antimicrobial Activity of Honey
PublicationHoney has had a valued place in traditional medicine for centuries. It was used to overcome liver, cardiovascular and gastrointestinal problems and for treatment of some types of infectious disease. Particularly, good results were achieved in the case of application of this product for therapy of infected, difficult to heal wounds. The high health-promoting properties of honey have been recently confirmed in many research investigations....
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Daily diet containing canned products significantly increases serum concentrations of endocrine disruptor bisphenol A in young women
PublicationNowadays, exposure to environmental factors is considered to be one of the possible causes of several lifestyle diseases, such as obesity, type 2 diabetes, cardiovascular disease, and cancer. Particularly noteworthy are endocrine‑disrupting chemicals (EDCs), which affect the metabolism of hormones and interact with their receptors, thus exerting adverse health effects. One of the most ubiquitous EDC in daily life is bisphenol A...
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Diagnostyka eksploatacyjna okrętowych silników spalinowych - tłokowych i turbinowych
PublicationW monografii przedstawiono wybrane zagadnienia diagnostyki technicznej silników spalinowych dużej mocy, zarówno tłokowych, jak i turbinowych, ukierunkowane na eksploatację okrętowych (i nie tylko) systemów energetycznych, w których występują tego typu silniki. W początkowej części opracowania zaproponowano koncepcję systemowego ujęcia diagnostyki eksploatacyjnej silników okrętowych w aspekcie obowiązujących standardów światowych...
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The compositional space of exhaled breath condensate and its link to the human breath volatilome
PublicationBreath analysis is commonly understood to target gaseous or volatile organic compounds (VOCs) for the characterization of different pathologies. Targeted analysis is most effective if a working hypothesis can be based on a plethora of data. The recently published volatilome builds an optimal basis for organizing powerful target sets. However, the origin and pathways of biosynthesis of many VOCs are not known, which complicates...
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Interspecies distances between propionic acid degraders and methanogens in syntrophic consortia for optimal hydrogen transfer
PublicationA mixed culture from an anaerobic biowaste digester was enriched on propionate and used to investigate interspecies hydrogen transfer in dependence of spatial distances between propionate degraders and methanogens. From 20.3 mM propionate, 20.8 mM acetate and 15.5 mM methane were formed. Maximum specific propionate oxidation and methane formation rates were 49 and 23 mmol mg−1day−1, respectively. Propionate oxidation was inhibited by...
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Phenotypic consequences of the LYS4 gene disruption in Candida albicans
PublicationThe main scientific purpose of our studies was to verify the hypothesis that homoaconitase (HA) from Candida albicans, an enzyme catalyzing a second step of the α-aminoadipate pathway (AAP) of L-Lys biosynthesis may become a new target for antifungal chemotherapy. Previous studies indicated that the A. fumigatus mutant lacking the functional lysF gene, encoding HA, exhibited attenuated virulence in a low-dose mouse infection model...
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The impact of training and neurotrophins on functional recovery after spinal cord transection: cellular and molecular mechanisms contributing to motor improvement
PublicationBeneficial effects of locomotor training on the functional recovery after complete transection of the spinal cord indicate that in chronic spinal animals spontaneous recovery processes are enhanced and shaped by the training. The mechanisms of that use-dependent improvement are still not fully understood. This review tackles three aspects of this issue: (1) neurochemical attributes of functional improvement...
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Online Volatile Compound Emissions Analysis Using a Microchamber/Thermal Extractor Coupled to Proton Transfer Reaction-Mass Spectrometry
PublicationIndoor air is a complex and dynamic mixture comprising manifold volatile organic compounds (VOCs) that may cause physiological and/or psychological discomfort, depending on the nature of exposure. This technical note presents a novel approach to analyze VOC emissions by coupling a microchamber/thermal extractor (μ-CTE) system to a proton transfer reaction-mass spectrometer (PTR-MS). This configuration provides an alternative to...
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Recent advancements in LC‐MS based analysis of biotoxins: Present and future challenges
PublicationThere has been a rising concern regarding the harmful impact of biotoxins, source of origin, and the determination of the specific type of toxin. With numerous reports on their extensive spread, biotoxins pose a critical challenge to figure out their parent groups, metabolites, and concentration. In that aspect, liquid chromatography‐mass spectrometry (LC‐MS) based analysis paves the way for its accurate identification and quantification....
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Broadband/Dual-band Metal-Mountable UHF RFID Tag Antennas: A Systematic Review. Taxonomy Analysis, Standards of Seamless RFID System Operation, Supporting IoT implementations, Recommendations and Future Directions
PublicationThe employment of broadband/dual-band ultra-high frequency (UHF) radio frequency identification (RFID) tag antennas contributes to the growth of RFID technology, with many potential implications, such as the increase of international trade, and reducing costs thereof. This study presents all reported articles on RFID tags for metal objects that can work seamlessly across different countries. Moreover, it addresses all available...
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The effects of the IM1-12Br ionic liquid and the oxytetracycline mixture on selected marine and brackish microorganisms
PublicationThe number of applications and commercialized processes utilizing ionic liquids has been increasing, and it is anticipated that this trend will persist and even intensify in the future. Ionic liquids possess desirable characteristics, such as low vapor pressure, good water solubility, amphiphilicity, and stability. Nevertheless, these properties can influence their environmental behavior, resulting in resistance to biotic and abiotic...
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Electrically Conductive Carbon‐based (Bio)‐nanomaterials for Cardiac Tissue Engineering
PublicationA proper self-regenerating capability is lacking in human cardiac tissue which along with the alarming rate of deaths associated with cardiovascular disorders makes tissue engineering critical. Novel approaches are now being investigated in order to speedily overcome the challenges in this path. Tissue engineering has been revolutionized by the advent of nanomaterials, and later by the application of carbon-based nanomaterials...
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Probabilistyczna ocena wrażliwości stanów granicznych konstrukcji inżynierskich na imperfekcje geometryczne i materiałowe
PublicationTematem pracy jest analiza probabilistyczna wrażliwości mechanicznej odpowiedzi konstrukcji inżynierskich na imperfekcje geometryczne oraz zmianę własności materiałów. Z tematem tym ściśle związany jest problem estymacji niezawodności konstrukcji, również szeroko opisany w rozprawie. W pracy dokonano przeglądu metod wykorzystywanych w analizie probabilistycznej oraz zaproponowano procedury wykorzystujące te metody w analizie wrażliwości...
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Progress in targeting tumor cells by using drug-magnetic nanoparticles conjugate.
PublicationTo limit the cytotoxicity of anticancer drugs against healthy cells, an appropriate carrier should be synthesized to deliver the drug to the tumor tissue only. A good solution is to anchor a magnetic nanoparticle to the molecule of the drug and to use a properly directed external magnetic field. We have shown that the improved by us synthesis of the conjugate of doxorubicin with iron-oxide magnetic nanoparticles allows a substantial...
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Gentiana asclepiadea exerts antioxidant activity and enhances DNA repair of hydrogen peroxide- and silver nanoparticles-induced DNA damage
PublicationExposure to high levels of different environmental pollutants is known to be associated with induction of DNA damage in humans. Thus DNA repair is of great importance in preventing mutations and contributes crucially to the prevention of cancer. In our study we have focused on quantitative analysis of Gentiana asclepiadea aqueous or methanolic extracts obtained from flower and haulm, their antioxidant potency in ABTS post-column...
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Biomechanical properties of 3D-printed bone models
PublicationBone lesions resulting from large traumas or cancer resections can be successfully treated by directly using synthetic materials or in combination with tissue engineering methods (hybrid). Synthetic or hybrid materials combined with bone tissue’s natural ability for regeneration and biological adaptation to the directions of loading, allow for full recovery of its biological functions. Increasing interest in new production methods...
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Effective Drug Concentration and Selectivity Depends on Fraction of Primitive Cells
PublicationPoor efficiency of chemotherapeutics in the eradication of Cancer Stem Cells (CSCs) has been driving the search for more active and specific compounds. In this work, we show how cell density-dependent stage culture profiles can be used in drug development workflows to achieve more robust drug activity (IC50 and EC50) results. Using flow cytometry and light microscopy, we characterized the cytological stage profiles of the HL-60-,...
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Utilizing Genome-Wide mRNA Profiling to Identify the Cytotoxic Chemotherapeutic Mechanism of Triazoloacridone C-1305 as Direct Microtubule Stabilization
PublicationRational drug design and in vitro pharmacology profiling constitute the gold standard in drug development pipelines. Problems arise, however, because this process is often dicult due to limited information regarding the complete identification of a molecule’s biological activities. The increasing aordability of genome-wide next-generation technologies now provides an excellent opportunity to understand a compound’s diverse eects...
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Peptidoglycan hydrolases - potential weapons against Staphylococcus aureus
PublicationBacteria of the genus Staphylococcus are common pathogens responsible for a broad spectrum of human and animal infections and belong to most important etiological factors causing food poisoning. Because of rapid increase in prevalence of isolation of staphylococci resistant to many antibiotics, there is an urgent need for development of new alternative chemotherapeutics. A number of studies have recently demonstrated the strong...
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Wykorzystanie kamery termowizyjnej nowej generacji do oceny wpływu sił ortodontycznych na dziąsło = The application of a new-generation thermal imaging camera for the assessment of hemodynamic changes in gingiva during orthodontic treatment
PublicationIntroduction. One ot the most interesting modern methods of assessing microcirculation is thermovisiual examination. Thermovision cameras are commonly used in general medicine. As the periodontium is one of the most vascularized tissues in the human body, the application of high-sensitivity thermovision cameras may allow tor noninvasive asses- sment and early detection ot pathological changes in the gingiva by giving a complete...
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A novel in vitro assay for assessing efficacy and toxicity of antifungals using human leukaemic cells infected with Candida albicans
PublicationAims: 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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Long range molecular dynamics study of interactions of the eukaryotic glucosamine-6-phosphate synthase with fructose-6-phosphate and UDP-GlcNAc
PublicationGlucosamine-6-phosphate synthase (EC 2.6.1.16) is responsible for catalysis of the first and practically irreversible step in hexosamine metabolism. The final product of this pathway, uridine 5 diphospho Nacetyl- d-glucosamine (UDP-GlcNAc), is an essential substrate for assembly of bacterial and fungal cell walls. Moreover, the enzyme is involved in phenomenon of hexosamine induced insulin resistance in type II diabetes, which...