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Search results for: amyloid inhibition
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Inhibition of amyloid fibril formation of hen egg white lysozyme by trimethylamine N-oxide at low pH
PublicationIn 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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JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
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[18F]Amylovis as a Potential PET Probe for β-Amyloid Plaque: Synthesis, In Silico, In vitro and In vivo Evaluations
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Inhibition of Human and Yeast 20S Proteasome by Analogues of Trypsin Inhibitor SFTI-1
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Towards gelsolin amyloid formation
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Current Enzyme Inhibition
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Antitumor triazoloacridinone C-1305 as a potent FLT3 tyrosine kinase inhibitor in human acute myeloid leukemia (AML) cells.
PublicationJednym z defektów molekularnych u pacjentów z ostrą białaczką szpikową (AML) jest konstytutywna aktywacja receptoroweej kinazy tyrozynowj FLT3.Najczęstszą mutacją genu kodującego FLT3 jest wewnętrzna tandemowa duplikacja ITD we fragmencie okołobłonowym receptora. W pracy zbadano, czy przeciwnowotworowy triazoloakrydon C-1305 może być inhibitorem kinazy tyrozynowej FLT3. Badania przeprowadzono na dwóch liniach komórkowych białaczek...
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PARP inhibition potentiates the cytotoxic activity of C-1305, a selective inhibitor of topoisomerase II, in human BRCA1-positive breast cancer cells
PublicationTwo cellular proteins encoded by the breast and ovarian cancer type 1 susceptibility (BRCA1 and BRCA2) tumor suppressor genes are essential for DNA integrity and the maintenance of genomic stability.Approximately 5-10% of breast and ovarian cancers result from inherited alterations or mutations in these genes.Remarkably, BRCA1/BRCA2-deficient cells are hypersensitive to selective inhibition of poly(ADPribose) polymerase 1 (PARP-1),...
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Amyloid fibril formation in the presence of water structure-affecting solutes
PublicationThe impact of the differently hydrated non-electrolytes (protein structure destabilizers) on the fibrillation of hen egg white lysozyme (HEWL) was investigated. Two isomeric urea derivatives i.e. butylurea (BU) and N,N,N′,N′-tetramethylurea (TMU) were chosen as a tested compounds. The obtained results show that butylurea exerts greater impact on HEWL and its fibrillation than tetramethylurea. Both substances decrease the time of...
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AMYLOID-JOURNAL OF PROTEIN FOLDING DISORDERS
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Influence of the ionic strength on the amyloid fibrillogenesis of hen egg white lysozyme
PublicationThe study investigates the role of the electrostatic interactions in the fibrillation of the hen egg white lysozyme (HEWL). In order to achieve this aim the influence of the cations Na+, Mg2+ and Al3+ on the amyloid fibril formation and amorphous aggregation was tested. The amyloids are formed in the solution without added salt but the Thioflavin T fluorescence gives the false-negative result. In these conditions, the HEWL fibrils...
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Molecular dynamics study of amyloid formation of two Abl-SH3 domain peptides
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Butyrylcholinesterase signal sequence self-aggregates and enhances amyloid fibril formation in vitro
PublicationAlzheimer’s disease (AD) pathogenesis has been attributed to extracellular aggregates of amyloid β (Aβ) plaques and neurofibrillary tangles in the human brain. It has been reported that butyrylcholinesterase (BChE) also accumulates in the brain Aβ plaques in AD. We have previously found that the BChE substitution in 5′UTR caused an in-frame N-terminal extension of 41 amino acids of the BChE signal peptide. The resultant variant...
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RAAS inhibition – a practice of medical progress
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Fibrillar aggregates in powdered milk
PublicationThis research paper addresses the hypothesis that powdered milk may contain amyloid fibrils. Amyloids are fibrillar aggregates of proteins. Up to this time, research on the presence of amyloids in food products are scarce. To check the hypothesis we performed thioflavin T fluorescence assay, X-ray powder diffraction, atomic force microscopy and fluorescence microscopy imaging. Our preliminary results show that commercially available...
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Inhibition of Polymer Photodegradation by Incorporation of Coffee Silverskin
PublicationOver the last years, the trend associated with the incorporation of materials from renewable resources into polymer technology is getting significantly more vital. Researchers are trying to transfer the properties of natural raw materials into the polymer world. Therefore, different natural materials are more often investigated as potential additives for polymers. Such an effect is noted for the coffee industry by-products, such...
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Inhibition of cancer antioxidant defense by natural compounds
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Determination of Effects and Mechanisms of Action of Bacterial Amyloids on Antibiotic Resistance
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PI3Kδ Inhibition by Idelalisib in Patients with Relapsed Indolent Lymphoma
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Telomerase inhibition - unfulfilled hopes in the perfect molecular target
PublicationTelomerase 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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Multiple β-sheet molecular dynamics of amyloid formation from two ABl-SH3 domain peptides
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Specific Binding of Cholesterol to the Amyloid Precursor Protein: Structure of the Complex and Driving Forces Characterized in Molecular Detail
PublicationC99 is the C-terminal membrane-bound fragment of the amyloid precursor protein that is cleaved by γ-secretase to release Aβ peptides, the hallmark of Alzheimer’s disease (AD). Specific interactions of C99 with cholesterol have been proposed to underlie the recognized role of cholesterol in promoting amyloidogenesis. By using molecular dynamics simulations, we studied cholesterol binding to C99 in a lipid bilayer. We determined...
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The effect of mangiferin on skin: Penetration, permeation and inhibition of ECM enzymes
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Desensitization of glucosamine-6-phosphate synthase to inhibition by UDP-GlcNAc
PublicationGlucosamine-6-phosphate (GlcN-6-P) synthase, known also as L-Glutamine: D-fructose-6-phosphate amidotransferase, catalyzes the first committed step in the pathway leading to the ultimate formation of UDP-GlcNAc. The final product of this pathway is an activated precursor of numerous macromolecules containing amino sugars, including chitin and mannproteins in fungi, peptidoglycan and lipopolysaccharides in bacteria, and glycoproteins...
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Inhibition of the granular anammox process by the high concentration of free ammonia.
PublicationHigh concentrations of ammonia and nitrite, typical for reject water treatment in the anammox process with the use of high temperatures and pH, may cause free ammonia (FA) inhibition. In this study, the inhibitory effect of FA on anammox process rate was investigated in a bench-scale sequencing batch reactor (SBR) with granular anammox biomass. Results of the study present that the anammox process could be successfully operated...
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IN SEARCH OF A NEW EXHIBITION SPACE
PublicationThe buildings considered as raising the prestige and promoting cities are those related to culture. Their impact on urban life is undeniable, which is reflected in a continuous increase in the number of new museum buildings. Apart from places intrinsically linked with culture, which, as such, may be considered as standard - like museum, theatres or galleries - there also appear alternative places of development and promotion of...
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Inhibition of protein glycosylation reverses the MDR phenotype of cancer cell lines
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Human proteinase 3 resistance to inhibition extends to alpha‐2 macroglobulin
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Development of dynamic method for evaluation of inhibition efficiency on the example of 8-hydroxyquinolin
PublicationSelection of a proper inhibitor should be based on the evaluation of its mechanism and effective concentrations. Mechanism of inhibition usually has dynamic character due to changing physicochemical conditions of the environment and corroding metal surface. Most of actually used methods are stationary or contain assumptions which highly influences obtained values. Development of new dynamic method, based on modified EIS, allows...
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Growth inhibition of cultured cancer cells by Ribes nigrum leaf extract
PublicationThe present article includes data on the possible selective cytotoxic effect of extract of Ribes nigrum L. growing at high Armenian landscape. For this purpose, different non-cancer (microglial BV-2 wild type (Wt), acyl-CoA oxidase 1 (ACOX1) deficient (Acox1-/-) and cancer (human colon adenocarcinoma HT29 and human breast cancer MCF7) cell lines were applied. R. nigrum leaf ethanol extract showed a growth inhibition effect towards...
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Elastic moduli of biological fibers in a coarse-grained model: crystalline cellulose and β-amyloids
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Region-Specific Methylation Profiling in Acute Myeloid Leukemia
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Myeloid-derived suppressor cells: a double-edged sword?
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Fatty acyl benzamido antibacterials based on inhibition of DnaK-catalyzed protein folding
PublicationWe have reported that the hsp70 chaperone DnaK from Escherichia coli might assist protein folding by catalyzing the cis/trans isomerization of secondary amide peptide bonds in unfolded or partially folded proteins. In this study a series of fatty acylated benzamido inhibitors of the cis/trans isomerase activity of DnaK was developed and tested for antibacterial effects in E. coli MC4100 cells. Nα-[Tetradecanoyl-(4-aminomethylbenzoyl)]-l-asparagine...
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Investigating the disease‐modifying properties of sclerotiorin in Alzheimer's therapy using acetylcholinesterase inhibition
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Prolonged pharmacological inhibition of cathepsin C results in elimination of neutrophil serine proteases
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Lung Protection by Cathepsin C Inhibition: A New Hope for COVID-19 and ARDS?
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Will we ever use angiotensin receptor neprilysin inhibition (ARNi) for the treatment of hypertension?
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Polyphosphates used for membrane scaling inhibition during water desalination by membrane distillation
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Cytotoxic effect on human melanoma cell lines and tyrosinase inhibition of Hottonia palustris
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Investigating the disease- modifying properties of sclerotiorin in Alzheimer's therapy using acetylcholinesterase inhibition
PublicationAlzheimer's disease (AD) is a progressive neurodegenerative disorder caused due to the damage and loss of neurons in specific brain regions. It is the most common form of dementia observed in older people. The symptoms start with memory loss and gradually cause the inability to speak and do day-to-day activities. The cost of caring for those affected individuals is huge and is probably beyond most developing countries capability....
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Quinoline-based thiazolyl-hydrazones target cancer cells through autophagy inhibition
PublicationHeterocyclic pharmacophores such as thiazole and quinoline rings have a significant role in medicinal chemistry. They are considered privileged structures since they constitute several Food and Drug Administration (FDA)-approved drugs for cancer treatment. Herein, we report the synthesis, in silico evaluation of the ADMET profiles, and in vitro investigation of the anticancer activity of a series of novel thiazolyl-hydrazones based...
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Evaluation of corrosion inhibition of brass-118 in artificial seawater by benzotriazole using Dynamic EIS
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Inhibition Ability of Natural Compounds on Receptor-Binding Domain of SARS-CoV2: An In Silico Approach
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Antiplasmodial activity of quinones: Roles of aziridinyl substituents and the inhibition of Plasmodium falciparum glutathione reductase
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Evaluation of corrosion inhibition of brass -118 in artificial seawater by benzotriazole using dynamic EIS
PublicationPrzedstawiono wyniki korozji mosiądzu 118 w sztucznej wodzie morskiej oraz efekt inhibicyjny benzotriazolu (BTA) przy użyciu nowoczesnej dynamicznej elektrochemicznej spektroskopii impedancyjnej (DEIS). metoda ta pozwala śledzić dynamikę procesu korozyjnego i efektu inhibicyjnego poprzez ocenę parametrów elektrycznych obwodu zastępczego. Chwilowe widma impedancyjne rejestrowane przez 10h wykazują iż ekspozycja przez okres kilku...
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In vitro antioxidant, anti-inflammatory activities and acetylcholinesterase inhibition properties of selected plant extracts
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Kinetic characterization of hydrogen sulfide inhibition of suspended anammox biomass from a membrane bioreactor
PublicationThe inhibition effects of hydrogen sulfide (H2S) on anammox-enriched biomass from a laboratory membrane reactor were analyzed in a series of batch respirometric experiments. The determined half maximal inhibitory concentration (IC50) was 4.67 mg H2S-S L−1 at the constant pH = 7.0 and the total sulfide concentration varying between 1 and 15 mg TS-S L−1. In another test, the IC50 was found to be 4.25 mg H2S-S L−1 under a constant...
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Homoisocitrate dehydrogenase from Candida albicans: properties, inhibition, and targeting by an antifungal pro-drug
PublicationThe LYS12 gene from Candida albicans, coding for homoisocitrate dehydrogenase was cloned and expressed as a His-tagged protein in Escherichia coli. The purified gene product catalyzes the Mg2+- and K+-dependent oxidative decarboxylation of homoisocitrate to alpha-ketoadipate. The recombinant enzyme demonstrates strict specificity for homoisocitrate. SDS-PAGE of CaHIcDH revealed its molecular mass of 42.6±1 kDa, while in size-exclusion...
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The Application of Dynamic Electrochemical Impedance Spectroscopy (DEIS) Technique in Corrosion and Corrosion Inhibition Studies
Publicationorrosion studies have attracted considerable interest in the areas of materials chemistry and industrial chemistry, as it affects the direct and indirect costs of industry, leading to huge economic setbacks due to the need for repair, maintenance, and even shutdowns due corrosion damage. This new volume is a comprehensive resource that presents new and up-to-date, theoretical, and experimental corrosion inhibition studies.