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Wyniki wyszukiwania dla: INHIBITORY MIKROTUBUL
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In vitro enzyme inhibitory properties, antioxidant activities, and phytochemical profile of Potentilla thuringiaca
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Cross-talk between DNA damage and cell survival checkpoints during G2 and mitosis: pharmacological implications
PublikacjaW pracy wyjaśnialiśmy rolę surwiwiny w ochronie komórek w czasie przejścia między G2 i mitozą, traktowanych związkiem uszkadzającym DNA. Jako model komórkowy wybraliśmy komórki ludzkiej białaczki MOLT-4, które wykazują zwiększoną ekspresję białka surwiwiny i niefunkcjonalnym p53. Ekspozycja tych komórek na melfalan, klasyczny związek uszkadzający DNA, prowadzi do uruchomienia punktu kontrolnego w G2 i zablokowania progresji cyklu...
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Steroid Sulfatase Inhibitors Based on Phosphate and Thiophosphate Flavone Analogs
PublikacjaA series of phosphate and thiophosphate flavone derivatives were synthesized and biologically evaluated in vitro for inhibition of steroid sulfatase (STS) activity. The described synthesis includes the straightforward preparation of 7-hydroxy-2-phenyl-4H-chromen-4-one 3a, 2-(4-fluorophenyl)-7-hydroxy-4H-chromen-4-one 3b, 7-hydroxy-2-(4-(trifluoromethyl)phenyl)-4H-chromen-4-one 3c, 7-hydroxy-2-(p-tolyl)-4H-chromen-4-one 3d modified...
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Procognitive activity of nitric oxide inhibitors and donors in animal models
PublikacjaNitric oxide is a small gaseous molecule that plays important roles in the majority of biological functions. Impairments of NO-related pathways contribute to the majority of neurological disorders, such as Alzheimer’s disease (AD), and mental disorders, such as schizophrenia. Cognitive decline is one of the most serious impairments accompanying both AD and schizophrenia. In the present study, the activities of NO donors, slow (spermine...
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Synthesis of novel, peptidic kinase inhibitors with cytostatic/cytotoxic activity
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Inhibitors of glucosamine-6-phosphate synthase as potential antifungal drugs.
PublikacjaPrzedstawiono stan obecny i perspektywy zastosowania inhibitorów enzymu syntazy GlcN-6-P jako leków skutecznych w leczeniu grzybic układowych. Używając metod modelowania molekularnego zaprojektowano struktury inhibitorów enzymu należących do dwóch grup strukturalnych: analogów glutaminy oraz analogów stanu przejściowego reakcji katalizowanej przez enzym. Opracowano metody syntezy pochodnych zoptymalizowanych inhibitorów, wykazujących...
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Wspólna lokalizacja jako katalizator i inhibitor rozwoju klastrów
PublikacjaStreszczenie: Głównym problemem badawczym poruszonym w artykule są zalety i wady wspólnej lokalizacji. Celem artykułu był przegląd koncepcji teoretycznych poświęconych konsekwencjom umiejscowienia podmiotów gospodarczych w konkretnych warunkach geograficznych i społecznych. Większość omawianych koncepcji została zaprezentowana w kontekście struktur klastrowych, dla których kwestia zakotwiczenia na określonym obszarze jest jedną...
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Sodium nitrite as a corrosion inhibitor of copper in simulated cooling water
PublikacjaThe corrosion inhibition behavior of sodium nitrite (NaNO2) towards pure copper (99.95%) in simulated cooling water (SCW) was investigated by means of electrochemical impedance spectroscopy (EIS) and dynamic electrochemical impedance spectroscopy (DEIS). NaNO2 interferes with metal dissolution and reduce the corrosion rate through the formation or maintenance of inhibitive film on the metal surface. Surface morphologies illustrated...
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Nuclear quantum effects in a HIV/cancer inhibitor: The case of ellipticine
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Variability of Hordeum vulgare L. Cultivars in Yield, Antioxidant Potential, and Cholinesterase Inhibitory Activity
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Structural analogues of reactive intermediates as inhibitors of glucosamine-6-phosphate synthase and phosphoglucose isomerase
PublikacjaCentra aktywne izomerazy fosfoglukozowej (PGI) oraz domeny izomerazowej (HPI) syntazy glukozamino-6-fosforanu (GlcN-6-P), wykazują podobieństwo ułożenia przestrzennego kluczowych reszt aminokwasowych, z wyjątkiem reszty Arg272 PGI i reszt Lys603 i Lys485 HPI. Dziesięć pochodnych D-heksitolo-6-P, kwasu 5-fosfoarabonowego i kwasu 6-fosfoglukonowego, strukturalnych analogów cis-enolaminy lub cis-enolanu, przypuszczalnych stanów przejściowych...
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N-Alkyl Derivatives of L-Glutamine As Inhibitors of Glutamine - Utilizing Enzymes
PublikacjaA general facile method to synthesize the N-gamma-alkyl and N-gamma,N-gamma-dialkyl derivatives of L-glutamine (1a-d) from L-glutamic acid as a starting substrate is presented. The obtained compounds are shown to inhibit three diferent glutamine-utilizing enzymes, namely: glutaminase, gamma-glutamyl transpeptidase, and glucosamine-6-phosphate synthase, with inhibitory constants within the milimolar range.
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Carboxylic acids as efficient corrosion inhibitors of aluminium alloys in alkaline media
PublikacjaThe efficiency of AA5754 aluminium alloy corrosion inhibition achieved with maleic, malic, succinic, tartaric, citric, tricarballylic acids and serine in alkaline environment (pH 11) was examined. Selected corrosion inhibitors are characterized by different numbers and distribution of carbonyl and hydroxyl groups within their molecules. We have proposed and verified a novel approach for determining the adsorption isotherms based...
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Diaryl Sulfide Derivatives as Potential Iron Corrosion Inhibitors: A Computational Study
PublikacjaThe present work aimed to assess six diaryl sulfide derivatives as potential corrosion inhibitors. These derivatives were compared with dapsone (4,4′-diaminodiphenyl sulfone), a common leprosy antibiotic that has been shown to resist the corrosion of mild steel in acidic media with a corrosion efficiency exceeding 90%. Since all the studied compounds possess a common molecular backbone (diphenyl sulfide), dapsone was taken as the...
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Acetylcholinesterase inhibitors: structure-activity relationship and kinetic studies on selected flavonoids
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Computational Selectivity Assessment of Protease Inhibitors against SARS-CoV-2
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The Combination of Beta-Blockers and ACE Inhibitors Across the Spectrum of Cardiovascular Diseases
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Epigenetic inhibitor zebularine activates ear pinna wound closure in the mouse
PublikacjaBackground:Most studies on regenerative medicine focus on cell-based therapies and transplantations.Small-molecule therapeutics, though proved effective in different medical conditions, have not been extensivelyinvestigated in regenerative research. It is known that healing potential decreases with development and devel-opmental changes are driven by epigenetic mechanisms, which suggests epigenetic repression of regenerativecapacity.Methods:We...
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Activation of endogenous regenerative potential in mammals using epigenetic inhibitor zebularine
PublikacjaIn this work, a nucleoside inhibitor of DNA methyltransferases, zebularine, was investigated as a wound healing and regeneration promoting agent. It was found that a high dose of intraperitoneally delivered zebularine improved punch wound closure in the ear pinna in mice. Both cytidine, a zebularine analogue, and uridine, a zebularine metabolite, did not promote ear pinna hole closure. The effect of zebularine on ear pinna healing...
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Chinifur, a Selective Inhibitor and "Subversive Substrate" for Trypanosoma congolense Trypanothione Reductase
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ACE Inhibitory Properties and Phenolics Profile of Fermented Flours and of Baked and Digested Biscuits from Buckwheat
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Both activating and inhibitory Fc gamma receptors mediate rituximab-induced trogocytosis of CD20 in mice
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Identification of 1H‐indene‐(1, 3, 5, 6)‐tetrol derivatives as potent pancreatic lipase inhibitors using molecular docking and molecular dynamics approach
PublikacjaPancreatic lipase is a potential therapeutic target to treat diet-induced obesity in humans, as obesity-related diseases continue to be a global problem. Despite intensive research on finding potential inhibitors, very few compounds have been introduced to clinical studies. In this work, new chemical scaffold 1H-indene-(1,3,5,6)-tetrol was proposed using knowledge-based approach, and 36 inhibitors were derived by modifying its...
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Fatty acyl benzamido antibacterials based on inhibition of DnaK-catalyzed protein folding
PublikacjaWe 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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Synthesis and biological evaluation of thiophosphate tricyclic coumarin derivatives as steroid sulfatase inhibitors
PublikacjaSteroid sulfatase (STS) enzyme inhibition is an important approach to the management of hormone-dependent breast cancer. In this paper, we report convenient methods for the synthesis and biological evaluation of thiophosphate tricyclic coumarin analogs exhibiting STS activity. The described methods are based on the straightforward preparation of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-2-one, 3-hydroxy- 7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one,...
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N-acylpeptides with glucosamine-6-phosphate synthase inhibitors - synthesisand antifungal activity
PublikacjaOpracowano syntezę kilku peptydów (di i tripeptydów) zawierających inhibitory syntazy glukozamino-6-fosforanu oraz przeprowadzono je w N-acylopochodne (acetylowe, heksanoilowe, dekanoilowe) oraz zbadano ich aktywność przeciwgrzybową w stosunku do szczepów Candida albicans z opornością wielolekową. Stwierdzono, że N-acylopeptydy wykazują aktywność przeciwgrzybową oraz określono wartości MIC.
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Phosphate tricyclic coumarin analogs as steroid sulfatase inhibitors: synthesis and biological activity.
PublikacjaIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate tricyclic coumarin derivatives as potential steroid sulfatase inhibitors. The described synthesis includes the straightforward preparation of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c]chromen-6-one modified...
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Geometry optimization of steroid sulfatase inhibitors - the influence on the free binding energy with STS
PublikacjaIn the paper we review the application of two techniques (molecular mechanics and quantum mechanics) to study the influence of geometry optimization of the steroid sulfatase inhibitors on the values of descriptors coded their chemical structure and their free binding energy with the STS protein. We selected 22 STS-inhibitors and compared their structures optimized with MM+, PM7 and DFT B3LYP/6–31++G* approaches considering separately...
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Electrochemical Evaluation of Sustainable Corrosion Inhibitors via Dynamic Electrochemical Impedance Spectroscopy
PublikacjaFinding suitable measurement methods for the effective management of electrochemical problems is of paramount importance, particularly for improving efficiency in corrosion protection. The need for accurate measurement techniques specific to nonstationary conditions has long been recognized, and promising approaches have emerged. This chapter introduces dynamic electrochemical impedance spectroscopy as a novel advancement in electrochemistry...
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X-ray Photoelectron Spectroscopy of Carboxylic Acids as Corrosion Inhibitors of Aluminium Alloys
PublikacjaThe datasets, titled X-ray Photoelectron Spectroscopy studies of citric acid adsorption on aluminium alloy 5754 in alkaline media and X-ray Photoelectron Spectroscopy studies of various carboxylic acids adsorption on aluminium alloys in alkaline media, contain XPS studies of the corrosion inhibitory action of selected dicarboxylic acids towards commercially available aluminium alloy 5754 in alkaline media at pH=11. These datasets...
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Inhibitors of glucosamine-6-phosphate synthase as potential antimicrobials or antidiabetics – synthesis and properties
PublikacjaGlucosamine-6-phosphate synthase (GlcN-6-P synthase) is known as a promising target for antimicrobial agents and antidiabetics. Several compounds of natural or synthetic origin have been identified as inhibitors of this enzyme. This set comprises highly selective L-glutamine, amino sugar phosphate or transition state intermediate cis-enolamine analogues. Relatively low antimicrobial activity of these inhibitors, poorly penetrating...
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Efficient Extraction of Fermentation Inhibitors by Means of Green Hydrophobic Deep Eutectic Solvents
PublikacjaThe methods for hydrogen yield efficiency improvements, the gaseous stream purification in gaseous biofuels generation, and the biomass pretreatment are considered as the main trends in research devoted to gaseous biofuel production. The environmental aspect related to the liquid stream purification arises. Moreover, the management of post-fermentation broth with the application of various biorefining techniques gains importance....
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Application 2D Descriptors and Artificial Neural Networks for Beta-Glucosidase Inhibitors Screening
PublikacjaBeta-glucosidase inhibitors play important medical and biological roles. In this study, simple two-variable artificial neural network (ANN) classification models were developed for beta-glucosidase inhibitors screening. All bioassay data were obtained from the ChEMBL database. The classifiers were generated using 2D molecular descriptors and the data miner tool available in the STATISTICA package (STATISTICA Automated Neural...
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Overcome the tumor immunotherapy resistance by combination of the HDAC6 inhibitors with antitumor Immunomodulatory agents.
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Uric acid and xantine-oxidase inhibitors in patients with gout: A re-assessment and an update
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Facilitated diffusion of glucosamine-6-phosphate synthase inhibitors enhances their antifungal activity
PublikacjaKwas N-3(4-metoksyfumaroilo)-L-2,3-diaminopropanowy (FMDP) i 2-amino-2-deo-ksy-D-glucitolo-6-fosforan (ADGP) są silnymi inhibitorami syntazy glukoza-mino-6-fosforanu, istotnego enzymu grzybowego, jednak ich aktywność przeciwgrzybowa jest słaba, ze względu na powolną penetrację tych związków przez błonę cytoplazmatyczną. W tej pracy badaliśmy możliwość poprawy działania przeciwgrzybowego ADGP i FMDP poprzez zwiększenie ich własności...
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Perturbation of cellular functions by topoisomerase II inhibitors: all roads lead to cell death?
PublikacjaPraca przeglądowa opisuje jakie funkcje mogą ulec zahamowaniu/zmianie pod wpływem działania inhibitorów topoizomerazy typu II w komórkach nowotworowych. W szczególności dyskutujemy jakie zmiany w szlakach sygnalizacji wewnątrzkomórkowej mogą prowadzić do zahamowania wzrostu oraz indukcji różnych rodzajów śmierci komórkowej i czy rodzaj śmierci komórkowej może decydować o skuteczności leków przeciwnowotoworowych, które hamują aktywność...
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Inhibitory and antimicrobial activities of OGTI and HV-BBI peptides, fragments and analogs derived from amphibian skin
PublikacjaA series of linear and cyclic fragments and analogs of two peptides (OGTI and HV-BBI) isolated from skin secretions of frogs were synthesized by the solid-phase method. Their inhibitory activity against several serine proteinases: bovine beta-trypsin, bovine alpha-chymotypsin, human leukocyte elastase and cathepsin G from human neutrophils, was investigated together with evaluation of their antimicrobial activities against Gram-negative...
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Chocolate desserts with ricotta hydrolysates: In vitro study of inhibitory activity against angiotensin‐converting enzyme and cholinesterase
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Inhibitory Effect of Eugenol and trans‐Anethole Alone and in Combination with Antifungal Medicines on Candida albicans Clinical Isolates
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Antiplasmodial Activity of Nitroaromatic Compounds: Correlation with Their Reduction Potential and Inhibitory Action on Plasmodium falciparum Glutathione Reductase
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Influence of sub-inhibitory concentration of selected plant essential oils on the physical and biochemical properties of Pseudomonas orientalis
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Galvanostatic impedance measurements for the efficient adsorption isotherm construction in corrosion inhibitor studies
PublikacjaWe present an approach towards an accurate and time-efficient adsorption isotherm determination to evaluate the corrosion inhibitor interaction in electrolytic environments. The approach is based on dynamic impedance spectroscopy measurements in galvanostatic mode (g-DEIS). The studied corrosion inhibitor is continuously injected between the secondary cell and the corrosion cell. The efficiency corresponding to instantaneous inhibitor...
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Development Of Dynamic Method For Evaluation Of Corrosion Rate On The Example Of Organic Corrosion İnhibitor
PublikacjaMeasurements of the corrosion rate belong to the most important aspects of materials science. In order to reduce material loss corrosion inhibitors are used. However selection of proper inhibitor should be based on evaluation of its mechanism and effective concentrations. Mechanism of inhibition usually has dynamic character so physicochemical parameters are changing in time. Most of actually used methods...
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Corrosion hazards and inhibitor protection in the seawater injection system on the Baltic sea rig
PublikacjaOil extraction efficiency in LOTOS Petrobaltic Company is increased by means of injection of seawater into an oilfield aquifer, which is implemented on the Baltic Beta rig, operating on the Baltic Sea. Operational experience has shown a significant degree of corrosion aggressiveness in the injected water, which necessitates frequent repairs of the seawater injection installation. Evaluation of the corrosion phenomena is crucial...
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Anticandiadal properties of N-acylpeptides containing inhibitor of glucosamine-6-phosphate synthase
PublikacjaOtrzymano serię N-acylopeptydów zawierających inhibitor syntazy glukozamino-6-fosforanu i zbadano ich aktywność w stosunku do szczepów Candida albicans. Aktywność przeciwgrzybową skorelowano z właściwościami lipofilowymi otrzymanych peptydów. Peptydy zawierające resztę kwasu dekanowego wykazywały najwyższą aktywność przeciwgrzybową.
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Eradication of LIG4-deficient glioblastoma cells by the combination of PARP inhibitor and alkylating agent
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Tissue Factor and Tissue Factor Pathway Inhibitor in Chronically Inflamed Gallbladder Mucosa
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Peptomeric analogues of trypsin inhibitor SFTI-1 isolated from sunflower seeds
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Inhibition of Human and Yeast 20S Proteasome by Analogues of Trypsin Inhibitor SFTI-1
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