Search results for: INHIBITOR
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Inhibition of Human and Yeast 20S Proteasome by Analogues of Trypsin Inhibitor SFTI-1
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Eradication of LIG4-deficient glioblastoma cells by the combination of PARP inhibitor and alkylating agent
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Analogues of trypsin inhibitor SFTI-1 modified in the conserved P1′ position by synthetic or non-proteinogenic amino acids retain their inhibitory activity
PublicationA series of linear and monocyclic (with a disulfide bridge only) analogues of trypsin inhibitor SFTI-1 modified in the P-1 and/or P-1' positions were synthesized by the solid-phase method. In the substrate specificity P-1 position, Phe or N-benzylglycine (Nphe) were introduced, whereas the conserved Ser6 in Bownam-Birk (BBI) inhibitors was replaced by Hse (L-homoserine), Nhse [N-(2-hydroxyethyl)glycine], Sar, and Ala. Kinetic studies...
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Implication of the disulfide bridge in trypsin inhibitor SFTI-1 in its interaction with serine proteinases
PublicationFourteen monocyclic analogues of trypsin inhibitor SFTI-1 isolated from sunflower seeds were synthesized by the solid-phase method. The purpose of this work was to establish the role of a disulfide bridge present in inhibitor's side chains of Cys3 and Cys11 in association with serine proteinases. This cyclic fragment was replaced by the disulfide bridges formed by L-pencillamine (Pen), homo-L-cysteine (Hcy), N-sulfanylethylglycine...
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An animal model of the procognitive properties of cysteine protease inhibitor and immunomodulatory peptides based on colostrum.
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Novel Potential Binding Sites for Selective Inhibitor Design of Human Soluble Epoxide Hydrolase
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Triazoloacridone C-1305 impairs XBP1 splicing by acting as a potential IRE1α endoribonuclease inhibitor
PublicationInositol requiring enzyme 1 alpha (IRE1α) is one of three signaling sensors in the unfolding protein response (UPR) that alleviates endoplasmic reticulum (ER) stress in cells and functions to promote cell survival. During conditions of irrevocable stress, proapoptotic gene expression is induced to promote cell death. One of the three signaling stressors, IRE1α is an serine/threonine-protein kinase/endoribonuclease (RNase) that...
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Selection of peptomeric inhibitors of bovine α-chymotrypsin and cathepsin G based on trypsin inhibitor SFTI-1 using a combinatorial chemistry approach
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Multi-sensor monitoring of the corrosion rate and the assessment of the efficiency of a corrosion inhibitor in utility water installations
PublicationThis paper presents an implementation of the monitoring of the corrosion rate and the assessment of the efficiency of a corrosion inhibitor in a utility water installation using an automated corrosion monitoring system. Due to the fact that the corrosion inhibitor was added to water intended for human consumption, it was necessary to build a multi-sensor monitoring system. In order to implement corrosion monitoring using a linear...
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Assessment of copper surface coverage with corrosion inhibitor using AFM-based local electrical measurements
PublicationThe paper presents a new method of assessment of metal surface coverage with corrosion inhibitor and thus of inhibitor protective performance. It is based on the atomic force microscopy measurement performed in a contact mode. Apart from topography images the proposed approach allows acquisition of local DC maps and local electrical impedance spectra via application of DC bias voltage or AC perturbation signal between the conductive...
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Experimental and Quantum Chemical Evaluation of 8-Hydroxyquinoline as a Corrosion Inhibitor for Copper in 0.1 M HCl
PublicationThe corrosion inhibition properties of 8-hydroxyquinoline (8-HQ) in 0.1 M HCl for copper have been investigated by using experimental (electrochemical impedance spectroscopy (EIS), dynamic electrochemical impedance spectroscopy (DEIS), and potentiodynamic polarization) and theoretical methods complemented by surface morphological examination with the aid of scanning electron microscopy (SEM) and electron dispersive X-ray spectroscopy...
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Fluorescent analogs of trypsin inhibitor SFTI-1 isolated from sunflower seeds-synthesis and applications
PublicationThis article describes the synthesis and enzymatic study of newly synthesized analogs of trypsin inhibitors SFTI-1 that were fluorescent labeled on their N-terminal amino groups. Two fluorescent derivatives of benzoxazole (3-[2-(4-diphenylaminophenyl) benzoxazol-5-yl]-L-alanine[(4NPh(2)) Ph] Box-Ala and 3-[2-(2', 4', 5'-trimethoxyphenyl) benzoxazol-5-yl]-l-alanine-[2,4,5-(OMe)3Ph] Box-Ala) were used as efficient fluorescent labels....
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Multi-sensor monitoring of the corrosion rate and the assessment of the efficiency of a corrosion inhibitor in utility water installations
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Surface plasmon resonance imaging biosensor for cathepsin G based on a potent inhibitor: Development and applications
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Investigation of peptide splicing using two‐peptide‐chain analogs of trypsin inhibitor SFTI‐1
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Positional Scanning Identifies the Molecular Determinants of a High Affinity Multi-Leucine Inhibitor for Furin and PACE4
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Analogues of Trypsin Inhibitor SFTI-1 with Disulfide Bridge Substituted by Various Length of Carbonyl Bridges
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Genetic inactivation and chemical inhibition of PARP-1 lead to increased cytotoxicity to antitumor triazoloacridone C-1305
PublicationOkreśliliśmy aktywność cytotoksyczną związku C-1305 wobec komórek z obniżoną aktywnością PARP-1 w wyniku działania inhibitora tego enzymu związku NU1025. Dane wskazują, że w zależności od rodzaju inhibitora topoizomerazy II obniżenie aktywności PARP-1 przez związek NU1025 prowadzi do zwiększenia bądź obniżenia cytotoksyczności tych leków. Działanie NU1025 prowadzi również do re-aktywacji szlaku p53 w komórkach HeLa, czego jak dotąd...
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The corrosion studies of 3,4,5-trihydroxybenzoic acid as an effective corrosion inhibitor of low alloy steel
Open Research DataThe dataset contains the electrochemical studies evaluating if gallic acid is a corrosion inhibitor for low alloy steel. Three measurements were carried out each case; corrosion potential (label ecorr), electrochemical impedance spectroscopy (label eis) and cyclic polarization (label cp). The measurements were carried out in sodium chloride, acidified...
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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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