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Wyniki wyszukiwania dla: proteinase inhibitors
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Sulforaphane inhibits growth of phenotypically different breast cancer cells
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Teloxantron inhibits the processivity of telomerase with preferential DNA damage on telomeres
PublikacjaTelomerase reactivation is one of the hallmarks of cancer, which plays an important role in cellular immortalization and the development and progression of the tumor. Chemical telomerase inhibitors have been shown to trigger replicative senescence and apoptotic cell death both in vitro and in vivo. Due to its upregulation in various cancers, telomerase is considered a potential target in cancer therapy. In this study, we identified...
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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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Glucosylceramide Mimics: Highly Potent GCase Inhibitors and Selective Pharmacological Chaperones for Mutations Associated with Types 1 and 2 Gaucher Disease
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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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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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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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Influence of sub-inhibitory concentration of selected plant essential oils on the physical and biochemical properties of Pseudomonas orientalis
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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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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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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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Efficacious Alkaline Copper Corrosion Inhibition by a Mixed Ligand Copper(II) Complex of 2,2′-Bipyridine and Glycine: Electrochemical and Theoretical Studies
PublikacjaA mixed ligand copper(II) complex, namely, [Cu(BPy)(Gly)Cl]⋅2H2O (CuC) (BPy=2,2′-bipyridine and Gly=glycine), was synthesized and characterized. The synthesized CuC complex was tested as inhibitor to effectively mitigate the corrosion of copper in alkaline solutions using the linear sweep voltammetry (LSV) and linear polarization resistance (LPR) techniques. For the sake of comparison, such two D.C. electrochemical techniques were...
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Activity-based protein profiling guided identification of urine proteinase 3 activity in subclinical rejection after renal transplantation
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Extracting functional groups of ALLINI to design derivatives of FDA‐approved drugs: Inhibition of HIV‐1 integrase
PublikacjaHIV‐1 integrase (IN) is crucial for integration of viral DNA into the host genome and a promising target in development of antiretroviral inhibitors. In this work, six new compounds were designed by linking the structures of two different class of HIV‐1 IN inhibitors (active site binders and allosteric IN inhibitors (ALLINIs)). Among newly designed compounds, INRAT10b was found most potent HIV‐1 IN inhibitor considering different...
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Increased cytotoxicity of an unusual DNA topoisomerase II inhibitor compound C-1305 toward HeLa cells with downregulated PARP-1 activity results from re-activation of the p53 pathway and modulation of mitotic checkpoints
PublikacjaOur previous studies have shown that murine fibroblast cells, in which PARP-1 gene was inactivated by gene disruption, are extremely sensitive to triazoloacridone compound C-1305, an inhibitor of DNA topoisomerase II with unusual properties. Here, we show that pharmacological inhibition of PARP-1 activity by its inhibitor compound NU1025, sensitizes human cervical carcinoma HeLa cells to compound C-1305 compared to treatment with...
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Spliced analogues of trypsin inhibitor SFTI‐1 and their application for tracing proteolysis and delivery of cargos inside the cells
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Effect of Converting Enzyme Inhibitor on Copper and Iron Concentrations of Blood Plasma in Calves During the Neonatal Period
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The electrochemical studies of CB-PLA electrode after surface activation by proteinase K digestion
Dane BadawczeThe dataset contains the electrochemical studies performed to evaluate surface activation of the CB-PLA 3D printed electrodes by enzymatic hydrolysis in a solution containing proteinase K (72h digestion period). Different enzyme concentrations were evaluated: 0.2, 0.4, 0.6 and 0.8 mg/ml. The studies were performed before surface activation, during and...
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Oxidative Modification of Proteins in Pediatric Cystic Fibrosis with Bacterial Infections
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Contribution of small heat shock proteins to muscle development and function
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Structure and function of natural proteins for water transport: general discussion
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Carotenoid binding to proteins: Modeling pigment transport to lipid membranes
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Characteristic and specificity of protease activity of thermophilic bacteria Meiothermus ruber
PublikacjaThe primary purpose of research was to establish the possibility of using thermophilic bacteria Meiothermus ruber as a source of proteolytic enzymes. The main reason of searching new proteases is their commercial value especially in production of detergents, food, pharmaceuticals, leather, diagnostics or waste management. The development of this type processes will be possible by utilization of enzymes which have unique characteristics...
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Structural and Functional Analysis of Human HtrA3 Protease and Its Subdomains
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Core spliceosomal Sm proteins as constituents of cytoplasmic mRNPs in plants
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Biochemical and Structural Characterization of SplD Protease from Staphylococcus aureus
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Core spliceosomal Sm proteins as constituents of cytoplasmic mRNPs in plants
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Temperature-induced changes of HtrA2(Omi) protease activity and structure
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Modeling the Structure, Dynamics, and Transformations of Proteins with the UNRES Force Field
PublikacjaThe physics-based united-residue (UNRES) model of proteins ( www.unres.pl ) has been designed to carry out large-scale simulations of protein folding. The force field has been derived and parameterized based on the principles of statistical-mechanics, which makes it independent of structural databases and applicable to treat nonstandard situations such as, proteins that contain D-amino-acid residues. Powered by Langevin dynamics...
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Analysis of the Factors Affecting Static In Vitro Pepsinolysis of Food Proteins
PublikacjaIn this meta-analysis, we collected 58 publications spanning the last seven decades that reported static in vitro protein gastric digestion results. A number of descriptors of the pepsinolysis process were extracted, including protein type; pepsin activity and concentration; protein concentration; pH; additives; protein form (e.g., ‘native’, ‘emulsion’, ‘gel’, etc.); molecular weight of the protein; treatment; temperature; and...
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Fragmentomic analysis of biopeptides in silico released from milk proteins
PublikacjaThe fragmentomic-assisted method was employed to predict the biological potential of peptides derived from milk proteins hydrolyzed by papain and bromelain. Firstly, protein sequences were acquired from the BIOPEP-UWM database and then hydrolyzed by the above enzymes using a BIOPEP-UWM tool called “Enzyme(s) action”. The released peptides were defined as parent peptides and further analyzed for the presence of shorter peptidic...
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Modeling SARS‐CoV‐2 proteins in the CASP‐commons experiment
PublikacjaCritical Assessment of Structure Prediction (CASP) is an organization aimed at advancing the state of the art in computing protein structure from sequence. In the spring of 2020, CASP launched a community project to compute the structures of the most structurally challenging proteins coded for in the SARS-CoV-2 genome. Forty-seven research groups submitted over 3000 three-dimensional models and 700 sets of accuracy estimates on...
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Immunogenic and protective activity of recombinant chimeric Toxoplasma gondii proteins
PublikacjaToxoplasmosis, one of the most common parasitic invasions worldwide, may pose a great threat for individuals with weakened immune system. The parasite also causes considerable economic losses due to infection of livestock. To date there is no efficient immunoprophylaxis for humans and animals, which would provide long-lasting protection against T. gondii invasion. Chimeric proteins, containing several selected fragments of parasite...
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Erratum to: Sulforaphane inhibits growth of phenotypically different breast cancer cells
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BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS
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Generation of inhibitory compounds during pre-treatment of lignocellulosic biomass
Dane BadawczeDataset contains calibration curves and typical resultsa obtained during biomass pre-treatment. Data are converted from digital raw files to xlsx files
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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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Development of biocompatible iron oxide-silicon oxide core-shell nanoparticles as subcellular delivery platform for glucosamine-6-phosphate synthase inhibitors
PublikacjaIn order to develop the preparation of iron oxide-silica coreshell nanoparticles (CSNPs), thesis deeply explores the cetyltrimethylammonium (CTA+) directed silica coating methods of the oleic-acid capped iron oxide nanoparticles (OA-IONPs) initialized under near-neutral pH conditions. It is demonstrated that the initial alkaline hydrolysis of ethyl acetate in the presence of CTA+ and OA-IONPs induces an unusual ligand exchange...
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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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Synthesis, anticandidal activity of N3-(4-methoxyfumaroyl)-(S)-2,3-diaminopropanoic amide derivatives – Novel inhibitors of glucosamine-6-phosphate synthase
PublikacjaNovel FMDP amiders 4-6 have been synthesized and tested against Candida strains. The anticandidal activity has been confined only to Candida albicans. Anticandidal activity of the tested amides has correlated with their inhibitory activity of glucosamine-6-phosphate synthase in cell free extract from Candida albicans.
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Dipeptidyl Peptidase IV Inhibitory Peptides Generated in Dry-Cured Pork Loin during Aging and Gastrointestinal Digestion
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Antioxidant potential, mineral composition and inhibitory effects of conifer needle extract on hyaluronidase - prospects of application in functional food
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Synthesis and steroid sulfatase inhibitory activities of N-phosphorylated 3-(4-aminophenyl)-coumarin-7-O-sulfamates
PublikacjaIn the present work, we report convenient methods for the synthesis and biological evaluation of N-phosphorylated derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as potential steroid sulfatase (STS) inhibitors. Their binding modes were modeled using docking techniques. The inhibitory effects of the synthesized compounds were tested on STS isolated from human placenta. All of the newly synthesised coumarin derivatives were...
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Carbonic anhydrase inhibitors. Synthesis, and molecular structure of novel series N-substituted N'-(2-arylmethylthio-4-chloro-5- methylbenzenesulfonyl)guanidines and their inhibition of human cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII
PublikacjaA series of novel N-substituted N'-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)guanidines 9 e41 have been synthesized and investigated as inhibitors of four isoforms of zinc enzyme carbonic anhydrase (CA.EC 4.2.1.1), that is the cytosolic CA I and II, and cancer-associated isozymes CA IX and XII. Against the human CA I investigated compounds showed KI in the range of 87e6506 nM, toward hCA II ranging from 7.8 to 4500 nM,...
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Impedancyjne monitorowanie szybkości korozji w układach wodnych z zastosowaniem inhibitorów korozji
PublikacjaNiniejsza praca jest poświęcona opracowaniu metodyki pomiarowej pozwalającej na wyznaczanie szybkości korozji za pomocą metody galwanodynamicznej elektrochemicznej spektroskopii impedancyjnej (GDEIS). Zaproponowana metoda pozwala na wykonywanie badań korozyjnych w których klasyczne metody pomiarowe (polaryzacja liniowa, metoda EIS, polaryzacja Tafela) charakteryzują się otrzymywaniem wyników ze znaczną dozą niepewności. W przypadku...
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Synthesis and biological evaluation of fluorinated N-benzoyl and N-phenylacetoyl derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as steroid sulfatase inhibitors
PublikacjaIn the present work, we report convenient methods for the synthesis of 3-(4-aminophenyl)-coumarin-7-O-sulfamate derivatives N-acylated with fluorinated analogues of benzoic or phenylacetic acid as steroid sulfatase (STS) inhibitors. The design of these potential STS inhibitors was supported by molecular modeling techniques. Additionally, computational docking methods were used to determine the binding modes of the synthesized inhibitors...
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Liver antioxidant defense after FAAH inhibitor - URB-597 administration to DOCA-salt-induced hypertension in rats
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