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Wyniki wyszukiwania dla: tyrosinase inhibitors
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Metal-Organic Framework (MOF)/Epoxy Coatings: A Review
PublikacjaEpoxy coatings are developing fast in order to meet the requirements of advanced materials and systems. Progress in nanomaterial science and technology has opened a new era of engineering for tailoring the bulk and surface properties of organic coatings, e.g., adhesion to the substrate, anti-corrosion, mechanical, flame-retardant, and self-healing characteristics. Metal-organic frameworks (MOFs), a subclass of coordinative polymers...
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Genetic and Epigenetic Aspects of Atopic Dermatitis
PublikacjaAtopic dermatitis is a heterogeneous disease, in which the pathogenesis is associated with mutations in genes encoding epidermal structural proteins, barrier enzymes, and their inhibitors; the role of genes regulating innate and adaptive immune responses and environmental factors inducing the disease is also noted. Recent studies point to the key role of epigenetic changes in the development of the disease. Epigenetic modifications...
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In vitro and in silico assessment of anti-inflammatory activity of cocoa powders
PublikacjaPlants are considered the major sources of biologically active compounds, which provide unlimited opportunities for their use either as medical treatments or as novel drug formulations. Cocoa powder is frequently used in nutrition and is known to have many benefits thanks to its wide range of biological activities. The presented study was focused on th evaluation of the anti-inflammatory potential of extracts obtained from cocoa...
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Synthesis of disubstituted 1,3,4,9-tetrahydropyrano-[3,4-b]indole-1-acetic acids derivatives
Publikacja1,3,4,9-tetrahydropyrano[3,4-b ]indole-1-acetic acid derivatives are of interest for pharmaceutical research as a core structure for synthesis of biological active substance - Etodolac (selective Cyclooxygenase-2 inhibitor, which belongs to the Non-steroidal Anti-inflammatory Drug, NSAID, that shows a clin-ically effective analgesic and anti-inflammatory activity). Here the way of synthesis of two 1,3,4,9-tetrahydropyrano[3,4-b...
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Factors causing degradation of sulfadimetoxine
PublikacjaSulfadimetoxine is a representative of sulfonamide drugs which presence inhibits growth of activated sludge bacteria, rhat is necessary for the effective mineralization of organic and inorganic contaminants. Therefore factors which con prevent this situation are searched. Aim of this study is selection of conditions causing efficien degradation of the drug- sulfadimetoxine. The impact of such aspects as : the type of oxidizing...
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Synthesis of 5-Substituted 1H-Tetrazoles from Nitriles in the Presence of Heterogeneous Catalyst
PublikacjaTetrazoles are five-membered heterocyclic compounds containing in their rings four nitrogen atoms. They have wide applications as corrosion inhibitors, analytical reagents, high-energy materials and gas generating compositions. Tetrazoles also play important role in coordination chemistry as ligands and in medicinal chemistry as metabolically stable surrogates for carboxylic acids. In recent years, investigation of new method of...
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Molecular targets for antifungals in amino acid and protein biosynthetic pathways
PublikacjaFungi cause death of over 1.5 million people every year, while cutaneous mycoses are among the most common infections in the world. Mycoses vary greatly in severity, there are long-term skin (ringworm), nail or hair infections (tinea capitis), recurrent like vaginal candidiasis or severe, life-threatening systemic, multiorgan infections. In the last few years, increasing importance is attached to the health and economic problems...
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KO-FERMENTACJA METANOWA JAKO ALTERNATYWNA METODA ZAGOSPODAROWANIA ZANIECZYSZCZONEJ BIOMASY
PublikacjaJedną z przyczyn ograniczonego stosowania fitoremediacji jest powstawanie zanieczyszczonej biomasy, dla której wciąż nie opracowano odpowiedniej technologii zagospodarowania lub unieszkodliwiania. W pracy przedstawiono sposób redukcji objętości biomasy, powstającej w wyniku fitoremediacji, metodą fermentacji metanowej. Głównym zagadnieniem jest intensyfikacja produkcji biogazu w procesie ko-fermentacji dwóch lub większej liczby...
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Bioconversion of waste materials to hydrogen via dark fermentation using Enterobacter aerogenes
PublikacjaHydrogen can be obtained via dark fermentation with the use of anaerobic Enterobacter aerogenes. The efficiency of hydrogen production by fermentation techniques is strongly dependent on the con-ditions used i.e. the pH range, temperature, composition of fermentation broths, oxygen content, or even the presence of substances with potentially inhibitory effects on the microbiological culture [1-4]. The paper describes the study...
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A review of applications of ellipsometry in corrosion research
PublikacjaElipsometria jest to nieinwazyjna i bardzo dokładna technika pomiarowa znajdująca coraz więcej zastosowań w badaniach korozyjnych. Poglądowo przedstawiono aktualne zastosowania pomiarów elipsometrycznych. Przeglądu dokonano pod kątem przydatności elipsometrii do wyznaczania grubości oraz charakterystyki optycznej cienkich warstewek pasywnych pokrywających powierzchnię różnych metali. Opisano zastosowanie pomiarów elipsometrycznych...
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Zastosowania pomiarów elipsometrycznych w badaniach korozyjnych
PublikacjaElipsometria jest to nieinwazyjna i bardzo dokładna technika pomiarowa znajdująca coraz więcej zastosowań w badaniach korozyjnych. Poglądowo przedstawiono aktualne zastosowania pomiarów elipsometrycznych. Przeglądu dokonano pod kątem przydatności elipsometrii do wyznaczania grubości oraz charakterystyki optycznej cienkich warstewek pasywnych pokrywających powierzchnię różnych metali. Opisano zastosowanie pomiarów elipsometrycznych...
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Thermostable beta-glucosidase with a broad substrate specifity suitable for processing of lactose-containing products.
PublikacjaHipertermofilny archeon Sulfolobus shibatae wytwarza termostabilną beta glukozydazę przydatną do hydrolizy laktozy w mleku i serwatce przejawiającą największą aktywność w 85 stC przy pH 5,5. Aktywność ekstraktu bezkomórkowego Sulfolobus shibatae wynosi 0.29 U/mg białka i może być 17-krotnie zwiększona poprzez frakcjonowanie siarczanem amonu, chromatografię jonowymienną i filtrację żelową. Badany enzym ma dużą termostabilność i...
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New Analogues of Mycophenolic Acid
PublikacjaMycophenolic acid (MPA) possesses antibacterial, antifungal, antiviral, immunosuppressive and anticancer properties. It is a non-competitive and reversible inhibitor of dehydrogenase inosine-5'-monophosphate (IMPDH). This compound belongs to the immunosuppressive drugs used for the prevention of both acute and chronic transplant rejection. Until now, two derivatives of MPA have been used clinically: mycophenolate mofetil (MMF,...
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Isolation of the GFA1 gene encoding glucosamine-6-phosphate synthase of Sporothrix schenckii and its expression in Saccharomyces cerevisiae
PublikacjaGlucosamine-6-phosphate synthase (GlcN-6-P synthase) is an essential enzyme involved in cell wall biogenesis that has been proposed as a strategic target for antifungal chemotherapy. Here we describe the cloning and functional characterization of Sporothrix schenckii GFA1 gene which was isolated from a genomic library of the fungus. The gene encodes a predicted protein of 708 amino acids that is homologous to GlcN-6-P synthases...
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The Relationship between Gene Activity and Nitrous Oxide Production during Nitrification in Activated Sludge Systems
PublikacjaNitrite is an important factor which inhibits the first stage of the nitrification, the effect is stronger with the decrease of the DO concentrations. NO2- presence at concentration above 15 mg N – NO2 in the aeration tanks stimulates N2O production regardless of the DO concentration. The significant nirS gene induction, observed especially during the experiments with the nitrite addition indicates that N2O production is basically...
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Solid and liquid fractionation of sugarcane and Agave bagasse during ozonolysis and enzymatic hydrolysis: Impact on biohydrogen and biogas production
PublikacjaSustainable and cost-efficient lignocellulosic biomass-to-energy bioprocesses require assessing the main components released during biomass fractionation. This study assessed the mesophilic biochemical potential of biohydrogen (BHP) and methane production (BMP) from sugarcane bagasse (SCB) and cooked (CAB) and uncooked (UAB) Agave bagasse. A systematic comparative analysis was performed for the liquid and solid fractions derived...
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‘Acridines’ as New Horizons in Antifungal Treatment
PublikacjaFrequent fungal infections in immunocompromised patients and mortality due to invasive mycosis are important clinical problems. Opportunistic pathogenic Candida species remain one of the leading causes of systemic mycosis worldwide. The repertoire of antifungal chemotherapeutic agents is very limited. Although new antifungal drugs such as lanosterol 14α-demethylase and β-glucan synthase inhibitors have been introduced into clinical...
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Inactivation of glucosamine-6-phosphate synthase by N3-oxoacyl derivatives of L-2,3-diaminopropanoic acid
PublikacjaN3-oksoacylowe pochodne kwasu l-2,3-diaminopropanowego zawierające ugrupowanie epoksydowe lub układ sprzężonych wiązań podwójnych inaktywują syntaze glukozamino-6-fosforanu (GlcN-6-P) z S. cerevisiae. Wyniki badań kinetycznych inaktywacji enzymu wskazują na dwuetapowy przebieg tej reakcji, przy czym tworzenie kompleksu enzym:ligand poprzedza nieodwracalną modyfikację enzymu. Badane związki różniły się powinowactwem do centrum aktywnego...
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From DNA damage to G2 arrest: the many roles of topoisomerase II. W: Prog-ress in Cell Cycle Research. Ed. Meijer L., Jezequel A., Roberge M. London: Plenum Publ. Comp. Ltd**2003 vol. 5 chapt. 30 s. 295-300 Od uszkodzeń DNA do bloku w G2: wiele ról dla topoizomerazy II.
PublikacjaInhibitory DNA topoizomerazy II sa jednymi z najbardziej szeroko stosowanymi lekami przeciwnowotworowymi. Związki te indukuja pekniecia nici DNA i bloku progresji cyklu komorkowego w fazie G2. Jednak topoizomeraza II jest nie tylko celem molekularnym dla lekow przeciwnowtworowych ale enzym ten pelniwazna role w odpowiedzi komorkowej na dzialanie wielu lekow uszkadzajacych DNA. Topoizomeraza tworzy kompleksy molekularne z bialkami...
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Peptide-Based Rapid and Selective Detection of Mercury in Aqueous Samples with Micro-Volume Glass Capillary Fluorometer
PublikacjaMercury, a toxic heavy metal produced through both natural and anthropogenic processes, is found in all of Earth’s major systems. Mercury’s bioaccumulation characteristics in the human body have a significant impact on the liver, kidneys, brain, and muscles. In order to detect Hg2+ ions, a highly sensitive and specific fluorescent biosensor has been developed using a novel, modified seven amino acid peptide, FY7. The tyrosine ring...
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Modyfikacje polimeraz DNA jako rozwiązania problemów w reakcjach PCR
PublikacjaReakcja PCR już od wielu lat jest podstawowym narzędziem stosowanym w biotechnologii molekularnej. Nadal napotykamy jednak liczne problemy podczas jej przeprowadzania związane z trudnymi matrycami, obecnością inhibitorów itp. Optymalizacja reakcji PCR jest więc niezbędna w celu poprawy wyników. Jednym z rozwiązań tych problemów może być modyfikowanie polimeraz DNA. W powyższym artykule opisano problemy i rozwiązania zależne polimerazy...
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The psychrotrophic yeast Sporobolomyces roseus LOCK 1119 as a source of a highly active aspartic protease for the in vitro production of antioxidant peptides
PublikacjaA psychrotrophic yeast strain producing a cold-adapted protease at low temperature was classified as Sporobolomyces roseus. In standard YPG medium, S. roseus LOCK 1119 synthesized an extracellular protease with an activity of approximately 560 U/L. Optimization of medium composition and process temperature considerably enhanced enzyme biosynthesis; an approximate 70% increase in activity (2060 U/L). The native enzyme was purified...
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Zużyty płyn wiertniczy - odpad czy ściek?
PublikacjaPłuczka wiertnicza wywiera znaczący wpływ na wszystkie operacje podczas procesu technologicznego jakim jest wiercenie górotworu. Odpowiedni skład płuczki wpływa na ilość jak i jakość pozyskiwania ropy naftowej i gazu ziemnego, dlatego powinien spełniać zadania mające związek z jego określonymi właściwościami. Jednym z najważniejszych zadań płuczki jest oczyszczanie dna otworu ze zwiercin, a następnie ich transport na powierzchnie...
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Mass spectrometric identification of 13C-Labeled metaboloites during anaerobic propanoic acid oxidation
PublikacjaBiowaste digestion is a possibility to gain biogas as a renewable fuel source. However, the anaerobic food chain may be disrupted by, e.g., substrate overload or by inhibitors, leading to the accumulation of volatile fatty acids (VFAs), predominantly of propanoic acid (PA). VFA Accumulation may cause a rapid pH decrease, less biogas production, or even a total inhibition. To maintain high biogas productivity or to prevent a collapse...
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Mass Spectrometric Identification of 13C-Labeled Metabolites DuringAnaerobic Propanoic Acid Oxidation
PublikacjaBiowaste digestion is a possibility to gain biogas as a renewable fuel source. However, the anaerobic food chain may be disrupted by, e.g., substrate overload or by inhibitors, leading to the accumulation of volatile fatty acids (VFAs), predominantly of propanoic acid (PA). VFA Accumulation may cause a rapid pH decrease, less biogas production, or even a total inhibition. To maintain high biogas productivity or to prevent a collapse...
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Antimicrobial resistance of Pseudomonas spp. isolated from wastewater and wastewater-impacted marine coastal zone
PublikacjaIn this study, species distribution and antimicrobial susceptibility of cultivated Pseudomonas spp. were studied in influent (INF), effluent (EFF), and marine outfall (MOut) of wastewater treatment plant (WWTP). The susceptibility was tested against 8 antimicrobial classes, active against Pseudomonas spp.: aminoglycosides, carbapenems, broad-spectrum cephalosporins from the 3rd and 4th generation, extended-spectrum penicillins,...
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Resistance of Escherichia coli and Enterococcus spp. to selected antimicrobial agents present in municipal
PublikacjaIn this study, the susceptibility to erythromycin (E) and to trimethoprim/sulfamethoxazole (SXT) among isolates of Enterococcus spp. and Escherichia coli was tested, respectively. Both fecal indicators were detected and isolated from raw(RW) and treated wastewater (TW) as well as from samples of activated sludge (AS) collected in a local wastewater treatment plant (WWTP). Biodiversity of bacterial community in AS was also monitored...
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Synthesis and Biological Evaluation of Acridine/Acridone Analogs as Potential Anticancer Agents
PublikacjaAcridine and acridone analogues were prepared by Ullmann condensation and then cyclization reaction. As a result of nucleophilic substitution reaction 1-nitro-9-phenoxyacridine or 1-chloro-4-nitro-9(10H)-acridone with the corresponding peptides, the planned acridine derivatives (10a-c, 12, 17-a-d, 19) have been obtained. The cytotoxic activity of the newly obtained analogs were evaluated against melanotic (Ma) and amelanotic (Ab)...
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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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The influence of G2 arrest abrogation on the long-term cytotoxicity of different genotoxic lesions
PublikacjaJak się uważa, zdolność komórek nowotworowych z uszkodzeniami DNA do zatrzymywania progresji w cyklu komórkowym w fazie G2 wydłuża czas na reperację tych uszkodzeń i zwiększa zdolność do przeżycia tych komórek. W pracy badaliśmy wpływ skrócenia bloku w fazie G2 w komórkach dwóch typów białaczek, poddanych działaniu związków przeciwnowotworowych indukujących różne typy uszkodzeń DNA, na efekt cytotoksyczny tych związków. Zwiększenie...
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Synthesis of Combretastatin A-4 Analogs and their Biological Activities
PublikacjaCombretastatin 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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Cancer-selective, single agent chemoradiosensitising gold nanoparticles
PublikacjaTwo nanometre gold nanoparticles (AuNPs), bearing sugar moieties and/or thiol-polyethylene glycol-amine (PEG-amine), were synthesised and evaluated for their in vitro toxicity and ability to radiosensitise cells with 220 kV and 6 MV X-rays, using four cell lines representing normal and cancerous skin and breast tissues. Acute 3 h exposure of cells to AuNPs, bearing PEG-amine only or a 50:50 ratio of alpha-galactose derivative and...
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Targeting yeast topoisomerase II by imidazo and triazoloacridinone derivatives resulting in their antifungal activity
PublikacjaFungal pathogens are considered as serious factors for deadly diseases and are a case of medical concern. Invasive fungal infections also complicate the clinical course of COVID-19, leading to a significant increase in mortality. Furthermore, fungal strains' multidrug resistance has increased the demand for antifungals with a different mechanism of action. The present study aimed to identify antifungal compounds targeting yeast...
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Mass Spectrometric Identification of 13C-labeled Metabolites During anaerobic Propanoic Acid Oxidation
PublikacjaBiowaste digestion is a possibility to gain biogas as a renewable fuel source. However, the anaerobic food chain may be disrupted by, e.g., substrate overload or by inhibitors, leading to the accumulation of volatile fatty acids (VFAs), predominantly of propanoic acid (PA). VFA Accumulation may cause a rapid pH decrease, less biogas production, or even a total inhibition. To maintain high biogas productivity or to prevent a collapse...
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Enhanced Activity of P4503A4 and UGT1A10 Induced by Acridinone Derivatives C-1305 and C-1311 in MCF-7 and HCT116 Cancer Cells: Consequences for the Drugs’ Cytotoxicity, Metabolism and Cellular Response
PublikacjaActivity modulation of drug metabolism enzymes can change the biotransformation of chemotherapeutics and cellular responses induced by them. As a result, drug-drug interactions can be modified. Acridinone derivatives, represented here by C-1305 and C-1311, are potent anticancer drugs. Previous studies in non-cellular systems showed that they are mechanism-based inhibitors of cytochrome P4503A4 and undergo glucuronidation via UDP-glucuronosyltranspherase...
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Dual inhibition of PI3K/Akt signaling and the DNA damage checkpoint in p53-deficient cells with strong survival signaling: implications for cancer therapy
PublikacjaOporność komórek nowotworowych na leki uszkadzjące DNA związana jest ściśle ze zdolnością do utrzymywania blok z fazie G2 cyklu komórkowego. Blok ten regulowany jest przez mechanizmy punktu kontrolnego G2/M oraz szlaki przeżycia komórkowego. W pracy badaliśmy rolę szlaku kinazy PI3K/Akt w funkcjonowaniu punktu kontrolnego cyklu komórkowego i wpływ na przeżycie komórek traktowanych lekiem przeciwnowotworowym - cisplatyną. Nasze...
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Utilizing Genome-Wide mRNA Profiling to Identify the Cytotoxic Chemotherapeutic Mechanism of Triazoloacridone C-1305 as Direct Microtubule Stabilization
PublikacjaRational 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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Mechanism of reaction of RNA-dependent RNA polymerase from SARS-CoV-2
PublikacjaWe combine molecular dynamics, statistical mechanics, and hybrid quantum mechanics/molecular mechanics simulations to describe mechanistically the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) RNA-dependent RNA polymerase (RdRp). Our study analyzes the binding mode of both natural triphosphate substrates as well as remdesivir triphosphate (the active form of drug), which is bound preferentially over ATP by RdRp while...
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Sporothrix schenckii: purification and partial biochemical characterisation of glucosamine-6-phosphate synthase, a potential antifungal target
PublikacjaW artykule opisano izolację i charakterystykę właściwości natywnego enzymu, syntazy GlcN-6-P z komórek dimorficznego grzyba patogennego Sporothrix schenckii. Masę cząsteczkową enzymu natywnego określono na 350 kDa, a enzymu zdenaturowanego na około 79 kDa, co sugeruje homotetrameryczną strukturę białka. Wartość punktu izoelektrycznego wyniosła 6,26; wyznaczono także parametry kinetyczne katalizowanej reakcji. Aktywność enzymu była...
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KONSTRUKCJA AUKSOTROFICZNEGO WZGLĘDEM L-LIZYNY SZCZEPU CANDIDA ALBICANS
PublikacjaEnzymy szlaku kwasu L-α-aminoadypinowego biosyntezy L-lizyny z Candida albicans są potencjalnymi celami molekularnymi w terapii przeciwgrzybowej. Niektóre grupy badawcze wykazały, że auksotrofia wobec L-lizyny u pewnych gatunków grzybów powoduje zmniejszenie ich zjadliwości i może mieć wpływ na wzrost in vivo [Liebmann i in. 2004]. Oznacza to, że można się spodziewać zahamowania wzrostu komórek grzybowych w wyniku działania selektywnych...
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Functional domains of Candida albicans glucosamine-6-phosphate synthase.
PublikacjaSkonstruowano oddzielnie dwie domeny syntazy GlcN-6-P z Candida albicans jako białka fuzyjne, tj. domenę glutaminazową oraz domenę izomerazową, zawierające sekwencje poliHis, odpowiednio na C- i N-końcu. Zoptymalizowano warunki nadekspresji domen w komórkach Escherichia coli. Oba białka oczyszczono do homogenności przy zastosowaniu chromatografii metalopowinowactwa oraz zbadano ich podstawowe właściwości. Wyznaczono parametry kinetyczne...
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Diversity of fecal coliforms and their antimicrobial resistance patterns in wastewater treatment model plant.
PublikacjaThe occurrence of resistance patterns among wastewater fecal coliforms was determined in the study. Susceptibility of the isolates was tested against 19 antimicrobial agents: aminoglycosides, aztreonam, carbapenems, cephalosporines, b-lactam/b-lactamase inhibitors, penicillines, tetracycline, trimethoprim/sulfamethoxazole, and fluoroquinolones. Additionally the removal of resistant isolates was evaluated in the laboratory-scale...
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Phylogenetic relationship and antimicrobial resistance in Escherichia coli isolated from the Reda River and the Oliwski Stream, Northern Poland = Lekooporność i przynależność filogenetyczna szczepów Escherichia Coli izolowanych z rzeki Redy i Potoku Oliwskiego
PublikacjaThe high abundance of fecal bacteria in surface water is usually related to poor agricultural practice, pollution caused by domesticated and wild animals as well as with septic tank failures. Identification of fecal contamination sources seems to be crucial in order to effectively estimate the inherent risk. In this study, the phylogenetic relationship of 30 isolates of E. coli, originated from surface water, was estimated by employing...
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Novel molecules containing structural features of NSAIDs and 1,2,3-triazole ring: Design, synthesis and evaluation as potential cytotoxic agents
PublikacjaFor the first time the template containing structural features of more than one NSAIDs and the 1,2,3-triazole ring was explored for the identification of potential cytotoxic agents. These new and complex molecules were predicted to be effective inhibitors of PDE4B by molecular modelling studies in silico. The multi-step synthesis of these compounds were carried out starting from the well-known drug nimesulide and involved the use...
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Increased concentration of Taq DNA polymerase as a solution for GC-rich templates from clinical and environmental samples
PublikacjaDNA polymerase is an enzyme which plays crucial role in replication and DNA repair. It found application in PCR (polymerase chain reaction) where catalyses process of in vitro DNA synthesis. To meet the demands posed by mod- ern diagnostic, molecular biology or genetic engineering it is necessary to improve DNA polymerases to obtain new or better features useful in these fields. So far implemented modifications in majority are...
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Population-based case-control study of alpha 1-antitrypsin and SLC11A1 in Crohn's disease and ulcerative colitis.
PublikacjaBackground: Crohn’s disease (CD) and ulcerative colitis (UC) are chronic inflammatory diseases of the digestive tract. Genetic factors and an abnormal immune response to infections are suspected to be involved in inflammatory bowel diseases. Methods: In the present study 300 blood samples from CD patients (n 100), UC patients (n 100), and healthy controls (n 100) were taken from a population-based case-control study. PCR assays...
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Selective Cytostatic and Cytotoxic Anticancer Effects of Bisfunctional Agents: A Strategy for the Design of DNA Binding Agents
PublikacjaVarious agents have been synthesized and proved useful for the National Cancer Institute's anticancer testing as potential new drugs, but most agents suffer side effects from their limited selectivity against cancer cells over healthy ones. Therefore, this paper attempts to describe drugs in terms of the level of tumor cell selectivity which they possess to define the features of mols. that are essential for useful cytotoxicity....
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The Effect of Posaconazole, Itraconazole and Voriconazole in the Culture Medium on Aspergillus fumigatus Triazole Resistance
PublikacjaTriazoles are the only compounds used as antibiotics in both medicine and agriculture. The presence of triazoles in the environment can contribute to the acquisition of azole resistance among isolates of Aspergillus fumigatus. The objective of this study was to investigate the effect of A. fumigatus exposure to triazoles on susceptibility to these compounds. Seventeen triazole-resistant and 21 triazole-sensitive A. fumigatus isolates...
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Evaluating the antibacterial activity of muramyl dipeptide derivatives, retro-tuftsin derivatives, and anthraquinone oligopeptides against a range of pathogenic bacteria
PublikacjaSearch for new and efficient antibiotic is crucial because of microbial drug resistance and problems with side effects of the administered medication. In this study, we evaluate the in vitro microbiological activity of muramyl dipeptide derivatives, retro-tuftsin derivatives (i.e., tuftsin with reversed amino acid sequences), and combinations of retro-tuftsin derivatives with substituted anthraquinones. The potency of the investigated...
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Triazoloacridone C-1305 abrogates the restriction checkpoint in cells lacking functional p53 and promotes their accumulation in the G2/M phase of the cell cycle
PublikacjaTriazoloakrydon C-1305, nowy inhibitor topoizomerazy II, wykazuje wysoką aktywość cytotoksyczną wobec komórek wielu typów nowotworów. Komórki mysie pozbawione genu PARP-1 wykazywały nadwrażliwość na działanie tego związku. W pracy testowaliśmy działanie związku wobec dwóch różnych komóek nowotworowych różniących się statusem p53: komórkami białaczki myelocytarnej HL-60 i raka sutka MCF-7. Wykazaliśmy, że inkubacja ze związkiem...