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Do not die, become senescent: a new type of cellular resistance induced by topoisomerase II inhibitors in tumor cells with functional p53
PublikacjaJednym z efektów wywoływanych przez związki przeciwnowotworowe w komórkach nowotworowych jest trwałe zahamowanie wzrostu, związane z pojawieniem się markerów procesu starzenia komórkowego. Proponuje się, że może to być nowy sposób na zahamowanie postępu choroby nowotworowej. W naszych badaniach wykazujemy, że zahamowanie wzrostu indukowane przez związki z grupy inhibitorów topoizomerazy II w komórkach raka płuc A549 jest związane...
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Sulforaphene, an isothiocyanate present in radish plants, inhibits proliferation of human breast cancer cells
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Targeting of FLT3-ITD kinase contributes to high selectivity of imidazoacridinone C-1311 against FLT3-activated leukemia cells
PublikacjaDrugs targeting receptor tyrosine kinase FLT3 are of particular interest since activating FLT3-internal tandem duplication (ITD) mutations abundantly occur in fatal acute myeloid leukemias (AMLs). Imidazoacridinone C-1311, a DNA-reactive inhibitor of topoisomerase II, has been previously shown to be a potent and selective inhibitor of recombinant FLT3. Here, we expand those findings by studying its effect on leukemia cells with...
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Selective inhibition of cancer cells' proliferation by compounds included in extracts from Baltic Sea cyanobacteria
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In vitro characteristics ofLactobacillusspp. strains isolated from the chicken digestive tract and their role in the inhibition ofCampylobactercolonization
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A role for accessory genes rI.-1 and rI.1 in the regulation of lysis inhibition by bacteriophage T4
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Phytocomponents and evaluation of acetylcholinesterase inhibition by Ginkgo biloba L. leaves extract depending on vegetation period
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Inhibition of HIV‐1 or bacterial activation of macrophages by products of HIV‐1‐resistant human cells
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Antiplasmodial Activity of Nitroaromatic and Quinoidal Compounds: Redox Potential vs Inhibition of Erythrocyte Glutathione Reductase
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Inhibition of T-type calcium channel disrupts Akt signaling and promotes apoptosis in glioblastoma cells.
PublikacjaGlioblastoma multiforme (GBM) are brain tumors that are exceptionally resitant to both radio- and chemotherapy regimens and novel approaches to treatment are needed. T-type calcium channels are one type of low voltage-gated channel (LVCC) involved in embryonic cell proliferation and differentiation; however they are often over-expressed in tumors, including GBM. In this study, we found that inhibition of T-type Ca channels in GBM...
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Mangiferin Affects Melanin Synthesis by an Influence on Tyrosinase: Inhibition, Mechanism of Action and Molecular Docking Studies
PublikacjaMangiferin is a strong antioxidant that presents a wide range of biological activities. The aim of this study was to evaluate, for the first time, the influence of mangiferin on tyrosinase, an enzyme responsible for melanin synthesis and the unwanted browning process of food. The research included both the kinetics and molecular interactions between tyrosinase and mangiferin. The research proved that mangiferin inhibits tyrosinase...
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Development of potent and effective SARS-CoV-2 main protease inhibitors based on maleimide analogs for the potential treatment of COVID-19
PublikacjaIn the present work, we report a new series of potent SARS-CoV-2 Main Protease (Mpro) inhibitors based on maleimide derivatives. The inhibitory activities were tested in an enzymatic assay using recombinant Mpro (3CL Protease from coronavirus SARS-CoV-2). Within the set of new Mpro inhibitors, 6e demonstrated the highest activity in the enzymatic assay with an IC50 value of 8.52 ± 0.44 mM. The IC50 value for Nirmatrelvir (PF-07321332,...
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Screening of potential inhibitors for COVID-19 main protease from phytoconstituents of Tectona grandis Linn: application of molecular modeling studies
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Changes in Gene and Protein Expression of Metalloproteinase-2 and -9 and Their Inhibitors TIMP2 and TIMP3 in Different Parts of Fluoride-Exposed Rat Brain
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Trypsin inhibitors from the garden four o’clock (Mirabilis jalapa) and spinach (Spinacia oleracea) seeds: Isolation, characterization and chemical synthesis
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Glucosylceramide Mimics: Highly Potent GCase Inhibitors and Selective Pharmacological Chaperones for Mutations Associated with Types 1 and 2 Gaucher Disease
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Branched pentapeptides as potent inhibitors of the vascular endothelial growth factor 165 binding to Neuropilin-1: Design, synthesis and biological activity
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Alternative method for the synthesis of imidazo[5,1-f][1,2,4]triazin-4(3H)-one—a substrate for the preparation of phosphodiesterase (5) inhibitors
PublikacjaImidazo[5,1-f][1,2,4]triazin-4(3H)-ones, as isosteres of purine, are of interest for pharmaceutical research as potential substrates for the synthesis of cGMP-PDE5 inhibitors. We present a novel, alternative method for the synthesis of imidazotriazinones, that differs from the previously reported ones with respect to the method of construction of the triazinone ring in the molecule. The key step in our approach is condensation...
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Manganese(III) Promoted Cyclization of N-alkenyl-N-(2-hydroxyethyl) amides to Iso-Oxacepham Potent β-Lactamase Inhibitors
PublikacjaBackground: β-Lactams are still a subject of interest of organic chemists. The main reason for this interest is due to their application as a chemotherapeutic. β-Lactam antibiotics are still the most commonly used drugs in bacterial infections. Method: Methods using 4-exo-trig radical cyclization leading to β-lactams are an alternative to classical Staudinger`s β-Lactams formation. We prepared N-alkenyl-N-(2-hydroxyethyl)amides...
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Fracture surface topography measurements analysis of low-alloyed corrosion resistant steel after bending-torsion fatigue tests
PublikacjaIn this paper, an assessment of a topography measurement method for fracture surfaces of 10HNAP steel after bending-torsion fatigue tests was performed. Surface roughness was measured by using a non-contact Focus Variation Microscopy (FVM) technique in which the non-measured points (NMPs) and outliers (spikes) were removed by the application of general methods. The results revealed, that the optical measurement method introduced...
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DEIS evaluation of the relative effective surface area of AISI 304 stainless steel dissolution process in conditions of intergranular corrosion
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Impact of sensitization on dissolution process of AISI 304 stainless steel during intergranular corrosion evaluated using DEIS technique
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Investigation of the Process of Automatic Control of Current Polarity Reversal in the Conditions of Hybrid Technology of Electrochemical Processing of Corrosion-Resistant Steels
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Electrical mapping of AISI 304 stainless steel subjected to intergranular corrosion performed by means of AFM-LIS in the contact mode
PublikacjaThe paper presents results of the AFM-based approach to local impedance spectroscopy (LIS) measurements performed in a 20 20 lm grid within an austenite grain–grain boundary region for sensitized AISI 304 stainless steel (SS). Maps of electrical parameters obtained on the basis of localized impedance spectra were demonstrated, presenting their changes and correlation with the sample topography. Performed research revealed significant...
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The evaluation methodology of corrosion protection of tanks from hull structural steels with Acoustic Emission use and first results of investigations
PublikacjaW referacie przedstawiono metodykę badań mającą na celu ocenę stopnia ochrony przed korozją konstrukcji zbiorników ładunkowych i balastowych wykonanych ze stali kadłubowych z wykorzystaniem Emisji Akustycznej (EA). W metodyce wykorzystano wymagania obowiązujących norm, standardów oraz doświadczenia zdobyte w dotychczasowych badaniach poświęconych zastosowaniu metody EA do wykrywania i lokalizacji źródeł korozji na statkach. Do...
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DEIS evaluation of the relative effective surface area of AISI 304 stainless steel dissolution process in conditions of intergranulatar corrosion
PublikacjaWyniki przedstawione w tej pracy stanowią dalszą część badań dotyczących procesu roztwarzania wysokostopowej stali AISI 304 w warunkach zachodzenia korozji międzykrystalicznej z wykorzystaniem techniki dynamicznej elektrochemicznej spektroskopii impedancyjnej (DEIS). Po raz pierwszy zaprezentowano zmiany względnej powierzchni efektywnej procesu roztwarzania stali AISI 304 w warunkach zachodzenia korozji międzykrystalicznej w funkcji...
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Impact of sensitization on dissolution process of AISI 304 stainless steel during intergranular corrosion evaluated using DES technique
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Corrosion degradation monitoring of ship stiffened plates using guided wave phase velocity and constrained convex optimization method
PublikacjaThe study presents an experimental investigation on the corrosion degradation level assessment using nondestructive wave-based methods. The degradation level of ship structural elements has been assessed in two different ways. The first one is based on the spectral decomposition and zero-crossing incorporated reconstruction of the dispersion curve approach of the antisymmetric Lamb wave mode and the best matching of the theoretical...
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High-temperature Corrosion of ~ 30 Pct Porous FeCr Stainless Steels in Air: Long-Term Evaluation Up to Breakaway
PublikacjaIn this work, a long-term (up to 6000 hours) corrosion evaluation of three porous (~ 30 pct of initial porosity) ferritic iron-chromium alloys with different Cr contents (20, 22, and 27 wt pct of Cr) was carried out at 600 C, 700 C, 800 C, and 900 C in air. Mass gain measurements and SEM analyses revealed that at temperatures above 600 C, all alloys exhibit breakaway corrosion, whereas at 600 C, none of the alloys were heavily...
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The synthesis and biological activity of lipophilic derivatives of bicine conjugated with n3-(4-methoxyfumaroyl)-l-2,3-diaminopropanoic acid(fmdp) - an inhibitor of glucosamine-6-phosphate synthase
PublikacjaOtrzymano serię pochodnych bicyny połączonych z inhibitorem syntazy glukozamino-6-fosforanu (fmdp)oraz zbadano ich właściwości lipofilowe i aktywność przeciwgrzybową. otrzymane związki charakteryzowały się wyższą llipofilowością niż fmdp. wszystkie otrzymane związki wykazywały także wyższą aktywność przeciwgrzybową niż fmdp.
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The PARAGON Heart Failure trial – ongoing investigation of the angiotensin receptor antagonist/neprilysin inhibitor sacubitril/valsartan in heart failure patients with hypertension and preserved ejection fraction
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Stress corossion cracking susceptibility of dissimilar stainless steels welded joints
PublikacjaW artykule przedstawiono wyniki badań odporności na naprężeniowe pękanie korozyjne złączy różnoimiennych stali odpornych na korozję; austenitycznej 316L oraz typu duplex 2205. Badania próbek przeprowadzono techniką odkształcania z małą prędkością w agresywnym środowisku roztworu chlorku magnezowego. Wyniki badań korozyjnych uzupełniono analizą metalograficzną z obszarów przełomów.
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Stratification of nano-pigments in anti-corrosive coatings by means of magnetic field
PublikacjaThe concept of self-stratification of coatings, although attractive, causes difficulties in its practical use, especially when pigments are added to the resins. An alternative way of obtaining a multilayer structure in a single step was presented. Using the inhomogeneous magnetic field and magnetically active components of the coating, the possibility of vertically graded differentiation of the one layer properties has been verified....
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Phenethyl Isothiocyanate Inhibits Shiga Toxin Production in Enterohemorrhagic Escherichia coli by Stringent Response Induction
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Sulforaphane, a cruciferous vegetable-derived isothiocyanate, inhibits protein synthesis in human prostate cancer cells
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Genistein inhibits activities of methylenetetrahydrofolate reductase and lactate dehydrogenase, enzymes which use NADH as a substrate
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Palindromic carbazole derivatives: unveiling their antiproliferative effect via topoisomerase II catalytic inhibition and apoptosis induction
PublikacjaHuman DNA topoisomerases are essential for crucial cellular processes, including DNA replication, transcription, chromatin condensation, and maintenance of its structure. One of the significant strategies employed in cancer treatment involves the inhibition of a specific type of topoisomerase, known as topoisomerase II (Topo II). Carbazole derivatives, recognised for their varied biological activities, have recently become a significant...
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The effect of 1,4-butanediol on the efficiency of CO2 absorption and inhibition of NH3 escape during the mineral carbonation of gypsum
PublikacjaThis study explored the optimal concentration of 1,4-butanediol for maximizing CO2 absorption and minimizing ammonia desorption. Mineral carbonation of gypsum slurry was carried out in a bubble reactor with a magnetic stirrer maintaining constant speed for 1 hour. The gas introduced to the reactor was a mixture of CO2 and air. The gas flow was controlled by the mass controllers. Gas sensors were used to determine the concentration...
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C-1305 inactivation of recombinant human cytochrome P450, CYP1A2 and CYP3A4, is due to mechanism-based inhibition
PublikacjaPodjęto próbę określenia mechanizmu obserwowanej inhibicji izoenzymów CYP1A2 i CYP3A4 przez pochodną triazoloakrydonu C-1305.W pierwszym kroku stwierdzono, że hamowanie aktywnosci obu enzymów jest procesem nieodwracalnym. W kolejnych etapach badań wykazano między innymi, że obecność NADPH zwiększa istotnie stopień obserwowanej inhibicji, co wskazało, że mamy do czynienia z inhibicją samobójczą opartą na mechanizmie działania (ang....
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Isoform-specific inhibition of DNA topoisomerase II as the mechanism of action of novel anticancer agent C-1305
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Inhibition of phthalocyanine-sensitized photohemolysis of human erythrocytes by polyphenolic antioxidants: description of quantitative structure–activity relationships
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The Potential Mechanism of Tiliroside-Dependent Inhibition of t-Butylhydroperoxide-Induced Oxidative Stress in Endometrial Carcinoma Cells
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Improvement of CO2 absorption and inhibition of NH3 escape during CaCO3 precipitation in the presence of selected alcohols and polyols
PublikacjaThis research aims to investigate the effect of selected organic substances containing hydroxyl groups on the reduction of NH3 escape and the improvement of CO2 capture during the precipitation of calcium carbonate by carbonation method using post-distillation liquid from the Solvay process and gas stream containing CO2 in the amount corresponding to the exhausted gases produced by the combustion of fossil fuels. Glycerol, ethylene...
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Inhibition of amyloid fibril formation of hen egg white lysozyme by trimethylamine N-oxide at low pH
PublikacjaIn vitro inhibition of the formation of fibrous aggregates of proteins (amyloids) has gained increasing attention due to the number of diseases associated with protein misfolding and fibrillation. An interesting group of compounds for which pronounced activity against this phenomenon can be expected consists of low molecular weight substances (osmolytes) which have the ability to change protein stability. Here we investigate the...
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Meat Proteins as Dipeptidyl Peptidase IV Inhibitors and Glucose Uptake Stimulating Peptides for the Management of a Type 2 Diabetes Mellitus In Silico Study
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Efficacy of high-dose corticosteroid-based treatment for chronic lymphocytic leukemia patients with p53 abnormalities in the era of B-cell receptor inhibitors
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Indukcja procesu pseudostarzenia komórkowego przez inhibitory DNA topoizomerazy II i jego rola w oporności na leki przeciwnowotworowe
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Gamma irradiation mediated production improvement of some myco-fabricated nanoparticles and exploring their wound healing, anti-inflammatory and acetylcholinesterase inhibitory potentials
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Microbial acetylcholinesterase inhibitors for Alzheimer’s therapy: recent trends on extraction, detection, irradiation-assisted production improvement and nano-structured drug delivery
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New Polymethoxyflavones from Hottonia palustris Evoke DNA Biosynthesis-Inhibitory Activity in An Oral Squamous Carcinoma (SCC-25) Cell Line
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