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Wyniki wyszukiwania dla: PROTEINASE INHIBITOR
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Design of serine proteinase inhibitors by combinatorial chemistry using trypsin inhibitor SFTI‐1 as a starting structure
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Proteinase 3 phosphonic inhibitors
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Inhibitors of Matriptase‐2 Based on the Trypsin Inhibitor SFTI‐1
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Inhibitory mikrotubul w terapii przeciwnowotworowej = Inhibitors of microtubule in cancer therapy
PublikacjaW artykule opisano inhibitory mikrotubul, różnorodne związki chemiczne, znajdujące się w zaawansowanych przedklinicznych i wstępnych badaniach klinicznych. Pośród nich na uwagę zasługują półsyntetyczne analogi taksolu, substancje pochodzenia naturalnego, takie jak: epotilony, kombretastatyny, kolchinoidy, dolastatyny oraz syntetyczne związki o niskim ciężarze czasteczkowym: heterokombretastatyny, sulfonamidy, fenostatyny, pochodne...
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Human proteinase 3 resistance to inhibition extends to alpha‐2 macroglobulin
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Implication of the disulfide bridge in trypsin inhibitor SFTI-1 in its interaction with serine proteinases
PublikacjaFourteen 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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Inhibition of Human and Yeast 20S Proteasome by Analogues of Trypsin Inhibitor SFTI-1
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Investigation of Serine‐Proteinase‐Catalyzed Peptide Splicing in Analogues of Sunflower Trypsin Inhibitor 1 (SFTI‐1)
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Substrate specificity and inhibitory study of human airway trypsin-like protease
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Computational Selectivity Assessment of Protease Inhibitors against SARS-CoV-2
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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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Inhibitors and Antibody Fragments as Potential Anti-Inflammatory Therapeutics Targeting Neutrophil Proteinase 3 in Human Disease
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Inhibitory activity of double‐sequence analogues of trypsin inhibitor SFTI‐1 from sunflower seeds: an example of peptide splicing
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Truncation of Huia versabilis Bowman-Birk inhibitor increases its selectivity, matriptase-1 inhibitory activity and proteolytic stability
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Introduction of Pro and Its Analogues in the Conserved P1 Position of Trypsin Inhibitor SFTI-1 Retains Its Inhibitory Activity
PublikacjaA number of monocyclic SFTI-1 analogues modified in the conserved inhibitor P1 position by Pro, its L-hydroxyproline (Hyp) derivative as well as mimetics with different ring size were synthesized by the solid-phase method. Replacement of Ser6 by Pro, Hyp, and a four-member ring, L-azetidine-2-carboxylic acid (Aze), retained trypsin or chymotrypsin inhibitory activity. The determined association equilibrium constants of these analogues...
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The biological role of prolyl oligopeptidase and the procognitive potential of its peptidic inhibitors from food proteins
PublikacjaProlyl oligopeptidase (POP) is a conserved serine protease belonging to proline-specific peptidases. It has both enzymatic and non-enzymatic activity and is involved in numerous biological processes in the human body, playing a role in e.g., cellular growth and differentiation, inflammation, as well as the development of some neurodegenerative and neuropsychiatric disorders. This article describes the physiological and pathological...
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Atomic resolution crystal structure of HV-BBI protease inhibitor from amphibian skin in complex with bovine trypsin
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Design, Chemical Synthesis and Kinetic Studies of Trypsin Chromogenic Substrates Based on the Proteinase Binding Loop of Cucurbita maxima Trypsin Inhibitor (CMTI-III)
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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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Analogues of trypsin inhibitor SFTI-1 modified in the conserved P1′ position by synthetic or non-proteinogenic amino acids retain their inhibitory activity
PublikacjaA 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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Substrate profiling of Finegoldia magna SufA protease, inhibitor screening and application to prevent human fibrinogen degradation and bacteria growth in vitro
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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
PublikacjaTwo 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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Introduction of non-natural amino acid residues into the substrate-specific P1 position of trypsin inhibitor SFTI-1 yields potent chymotrypsin and cathepsin G inhibitors
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Exploiting the S4–S5 Specificity of Human Neutrophil Proteinase 3 to Improve the Potency of Peptidyl Di(chlorophenyl)-phosphonate Ester Inhibitors: A Kinetic and Molecular Modeling Analysis
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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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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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Molecular modeling study of tectoquinone and acteoside from Tectona grandis linn: a new SARS-CoV-2 main protease inhibitor against COVID-19
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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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Synthesis of Cyano-Benzylidene Xanthene Synthons Using a Diprotic Brønsted Acid Catalyst, and Their Application as Efficient Inhibitors of Aluminum Corrosion in Alkaline Solutions
PublikacjaNovel cyano-benzylidene xanthene derivatives were synthesized using one-pot and condensation reactions. A diprotic Brønsted acid (i.e., oxalic acid) was used as an effective catalyst for the promotion of the synthesis process of the new starting xanthene–aldehyde compound. Different xanthene concentrations (ca. 0.1–2.0 mM) were applied as corrosion inhibitors to control the alkaline uniform corrosion of aluminum. Measurements were...
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A. Computational analysis by molecular docking of thirty alkaloid compounds from medicinal plants as potent inhibitors of SARS-CoV-2 main protease(2020).
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Adsorption behavior and corrosion inhibitive characteristics of newly synthesized cyano-benzylidene xanthenes on copper/sodium hydroxide interface: Electrochemical, X-ray photoelectron spectroscopy and theoretical studies
PublikacjaElegant process for synthesis of 3-(7H-dibenzo[c,h]xanthen-7-yl)benzaldehyde (3), as new starting material to create a set of novel xanthene analogues, 2-(3-(7H-dibenzo[c,h]xanthen-7-yl)benzylidene)malononitrile (4), 3-(3-(7H-dibenzo[c,h]xanthen-7-yl)phenyl)-2-cyanoacrylic acid (5), and Ethyl-3-(3-(7H-dibenzo[c,h]xanthen-7-yl)phenyl)-2-cyanoacrylate (6), was achieved starting with available materials under mild conditions. Various...
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Distance between the Basic Group of the Amino Acid Residue's Side Chain in Position P1of Trypsin Inhibitor CMTI-III and Asp189in the Substrate Pocket of Trypsin Has an Essential Influence on the Inhibitory Activity
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Antifungal dipeptides incorporating an inhibitor of homoserine dehydrogenase
PublikacjaThe antifungal activity of 5‐hydroxy‐4‐oxo‐L‐norvaline (HONV), exhibited under conditions mimicking human serum, may be improved upon incorporation of this amino acid into a dipeptide structure. Several HONV‐containing dipeptides inhibited growth of human pathogenic yeasts of the Candida genus in the RPMI‐1640 medium, with minimal inhibitory concentration values in the 32 to 64 μg mL−1 range. This activity was not affected by multidrug...
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Neuroprotective Effect of SGLT2 Inhibitors
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In silico design of telomerase inhibitors.
PublikacjaTelomerase is a reverse transcriptase enzyme involved in DNA synthesis at the end of linear chromosomes. Unlike in most other cells, telomerase is reactivated most cancerous cells and, therefore, has become a promising new anticancer target. Despite extensive research, direct telomerase inhibitors have yet not been introduced to the clinics because of the complexity of this enzyme. Structures of this protein from simple organisms...
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Antifungal Activity of Homoaconitate and Homoisocitrate Analogs
PublikacjaThirteen structural analogs of two initial intermediates of the L-alpha-aminoadipate pathway of L-lysine biosynthesis in fungi have been designed and synthesized, including fluoro- and epoxy-derivatives of homoaconitate and homoisocitrate. Some of the obtainedcompounds exhibited at milimolar range moderate enzyme inhibitory properties against homoaconitase and/or homoisocitrate dehydrogenase of Candida albicans. The structural...
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Proteins
PublikacjaStruktura białek wpływa na ich wartość odżywczą, właściwości funkcjonalne wżywności oraz reakcje w surowcach i produktach żywnościowych. Warunki prze-chowywania oraz obróbki w przemyśle i w czasie przygotowywania kulinarnegowywołują przemiany białek istotne dla jakości żywności. Przez celowe, enzy-matyczne i chemiczne modyfikowanie składu i struktury białek można wpływaćna ich właściwości funkcjonalne w żywności i wartość...
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Docking simulations, Molecular properties and ADMET studies of novel Chromane6,7diol analogues as potential inhibitors of Mushroom tyrosinase
PublikacjaResearch on inhibition of tyrosinase enzyme has attained significant value, because tyrosinase inhibitors have potential applications in medicine, cosmetics (as whitening agents) and in agriculture (as bioinsecticides). Determination and elucidation of new tyrosinase inhibitors are not only beneficial for medical purposes, but their promising applications in improving food quality and nutritional...
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Novel Inhibitor-Based Therapies for Thyroid Cancer—An Update
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Metylotransferazy ssaków – inhibitory i aktywatory
PublikacjaWśród metylotransferaz ssaków możemy wyróżnić metylotransferazy histonowe oraz metylotransferazy DNA. Metylacja DNA w obrębie wysp CpG oraz metylacja histonów wpływają na poziom ekspresji genów w komórkach ssaczych. Dodatkowo dzięki metylacji zapewniana jest stabilność i integralność genomu ludzkiego. Metylotransferazy DNA, będące głównym tematem tego artykułu, są często przedmiotem badań, gdyż nieprawidłowa metylacja DNA jest...
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Clays as Inhibitors of Polyurethane Foams’ Flammability
PublikacjaPolyurethanes are a very important group of polymers with an extensive range of applications in different branches of industry. In the form of foams, they are mainly used in bedding, furniture, building, construction, and automotive sectors. Due to human safety reasons, these applications require an appropriate level of flame retardance, often required by various law regulations. Nevertheless, without the proper modifications,...
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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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Nuclear quantum effects in a HIV/cancer inhibitor: The case of ellipticine
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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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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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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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New potent cathepsin G phosphonate inhibitors
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ACEI and ARB — Each Unique RAAS Inhibitors
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Inhibitors of amino acids biosynthesis as antifungal agents
PublikacjaFungal microorganisms, including the human pathogenic yeast and filamentous fungi, are able to synthesize all proteinogenic amino acids, including nine that are essential for humans. A number of enzymes catalyzing particular steps of human-essential amino acid biosynthesis are fungi specific. Numerous studies have shown that auxotrophic mutants of human pathogenic fungi impaired in biosynthesis of particular amino acids exhibit...
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COMPUTER-AIDED DESIGN OF ORGANOPHOSPHORUS INHIBITORS OF UREASE
PublikacjaBased on the structure of the most potential inhibitor diamidophosphate, various novel groups of inhibitors were developed by knowledge-based design approach with covalent carbon-phosphorus or carbon-phosphorus-carbon bond to improve hydrolytic stability to inhibit the microbial ureases. Designed compounds were evaluated with 10 (LigScore1, LigScore2, PLP1, PLP2, JAIN, PMF, PMF04, LUDI_1, LUDI_2 and LUDI_3) different scoring functions...
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HDAC Inhibitors: Innovative Strategies for Their Design and Applications
PublikacjaHistone deacetylases (HDACs) are a large family of epigenetic metalloenzymes that are involved in gene transcription and regulation, cell proliferation, differentiation, migration, and death, as well as angiogenesis. Particularly, disorders of the HDACs expression are linked to the development of many types of cancer and neurodegenerative diseases, making them interesting molecular targets for the design of new efficient drugs...
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Therapeutic Potential of Multifunctional Derivatives of Cholinesterase Inhibitors
PublikacjaThe aim of this work is review of tacrine analogues from the last three years, which were not included in the latest review work, donepezil and galantamine hybrids from 2015 and rivastigmine derivatives from 2014. In this account we summarize the efforts toward the development and characterization of non-toxic inhibitors of cholinesterases based on mentioned drugs with various interesting additional properties such as antioxidant,...
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Catalytic topoisomerase II inhibitors in cancer therapy.
PublikacjaDNA topoizomeraza II jest jednym z głównych celów molekularnych dla leków stosowanych w terapii przeciwnowotworowej. Wszystkie inhibitory tego enzymu są zdolne do zakłócania w jeden z etapów cyklu katalitycznego topoizomerazy II. Związki, które stabilizują kowalencyjny kompleks DNa i topoizomerazy II (znany jako kompleks rozszczepialny) są nazywane truciznami topoizomerazy, inne związki, które hamują aktywność enzymu na innych...
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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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The influence of food phytochemicals on cyclic phosphodiesterase 4 (PDE4) activity
PublikacjaCyclic phosphodiesterase 4 (PDE4) belongs to family of cyclic phosphodiesterases, which are expressed predominantly in inflammatory cells, airway smooth muscles, cardiovascular tissues and brain. Inhibitors of this family of enzymes found medicinal applications as antidepressants, antiinflamatory drugs (mainly in airway diseases) or antiasthmatics (Ibudilast). PDE4 inhibitors are also being tested for preventing the development...
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PEGylated substrates of NSP4 protease: A tool to study protease specificity
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New potent STS inhibitors based on fluorinated 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamates
PublikacjaA series of fluorinated analogs based on the frameworks of 4-(1- phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamates have been synthesized as steroid sulfatase (STS) inhibitors. The design of chemical structures of new potential STS inhibitors was supported by molecular docking techniques to identify potential interactions between inhibitors and amino acid residues located in the STS active site. The STS inhibitory potency was evaluated...
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Chinifur, a Selective Inhibitor and "Subversive Substrate" for Trypanosoma congolense Trypanothione Reductase
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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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Adrenal Secretory Protease
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The Role of Proteins in Food
PublikacjaThis chapter describes the effect of proteins on the sensory attributes and the biological value and safety of foods. The role of proteins depends on their amino acid composition and structure, on changes due to storage and processing, as well as on interactions with other food components. The effect on the sensory quality of foods is brought about by hydrophobicity, solubility, water holding capacity, gelling, film formation,...
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Synthesis of anthraquinone-tuftsin analogues as potential topoisomerase inhibitors
PublikacjaZaprezentowano syntezę nowych analogów antrachinonów z pochodnymi tuftsyny i retro-tuftsyny oraz wstępne badania biologiczne (aktywność cytotoksyczną na wybranych liniach nowotworowych oraz zdolność hamowania topoizomerazy I).
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Low-Molecular-Weight Aldehyde Inhibitors of Cathepsin G
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Inhibitors of cathepsin G: a patent review (2005 to present)
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CDK9 inhibitors in multiple myeloma: a review of progress and perspectives
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An Overview of Several Inhibitors for Alzheimer’s Disease: Characterization and Failure
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Inhibitory endopeptydazy prolinowej pochodzące z białek żywności
PublikacjaBioaktywne peptydy pochodzące z białek żywności mają nie tylko znaczenie żywieniowe, ale szczególnie profilaktyczne i terapeutyczne w przypadku wielu chorób. Są to małocząsteczkowe fragmenty białek, które po uwolnieniu podczas hydrolizy mogą wykazywać m.in. właściwości przeciwcukrzycowe, przeciwnadciśnieniowe, przeciwdrobnoustrojowe, przeciwutleniające, immunomodulujące...
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Synthesis of the inosine 5′-monophosphate dehydrogenase (IMPDH) inhibitors
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Direct renin inhibitors in hypertension – Approaching the moment of truth
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Cyclic Peptidic Furin Inhibitors Developed by Combinatorial Chemistry
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Synthesis of the inosine 5'-monophosphate dehydrogenase (IMPDH) inhibitors
PublikacjaIn this review are summrized newly described IMPDH inhibitors. The article concerns both synthetic pathways and biological activities of the most promising compounds.
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Phosphate and Thiophosphate Biphenyl Analogs as Steroid Sulfatase Inhibitors
PublikacjaIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate and thiophosphate biphenyl derivatives exhibiting steroid sulfatase (STS) activity. The described synthesis is based on straightforward preparation of biphenyl-4-ol and 40-hydroxybiphenyl- 4-carboxylic acid ethyl ester modified with various phosphate or thiophosphate moieties. The inhibitory effects of these compounds were...
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Synthesis of bicoumarin thiophosphate derivatives as steroid sulfatase inhibitors
PublikacjaBased on the frameworks 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, a series of bicoumarin thiophosphate analogs have been synthesized and biologically evaluated. Additionally, their binding modes have been modeled using docking techniques. The inhibitory properties of the synthesized compounds...
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Inhibitors of angiogenesis in cancer therapy – synthesis and biological activity
PublikacjaAngiogenesis is the process of formation of new capillaries from preexisting blood vessels. Angiogenesis is involved in normal physiological processes, and plays an important role in tumor invasion and development of metastases. Vascular endothelial growth factor (VEGF) plays a key role in angiogenesis. VEGF is a mitogen for vascular endothelial cells and stimulates their proliferation. By inhibiting the biological activity of...
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Design of selective substrates of proteinase 3 using combinatorial chemistry methods
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Chromatographic analysis of extracts isolated from different poplar species as potential inhibitors of enzymatic hydrolysis Analiza chromatograficzna substancji ekstrakcyjnych pozyskanych z różnych odmian topoli jako potencjalnych inhibitorów hydrolizy enzymatycznej
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Fluorescent analogs of trypsin inhibitor SFTI-1 isolated from sunflower seeds-synthesis and applications
PublikacjaThis 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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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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Eradication of LIG4-deficient glioblastoma cells by the combination of PARP inhibitor and alkylating agent
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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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Examination of epigenetic inhibitor zebularine in treatment of skin wounds in healthy and diabetic mice
PublikacjaDNA methyltransferase inhibitor zebularine was proven to induce regeneration in the ear pinna in mice. We utilized a dorsal skin wound model to further evaluate this epigenetic inhibitor in wound healing. Full-thickness excisional wounds were made on the dorsum of 2 and 10-month-old healthy BALB/c and 3 and 8-month-old diabetic (db/db) mice, followed by topical or intraperitoneal zebularine delivery. Depending on the strain, age,...
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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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Three Wavelength Substrate System of Neutrophil Serine Proteinases
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Electrochemical, theoretical and surface physicochemical studies of the alkaline copper corrosion inhibition by newly synthesized molecular complexes of benzenediamine and tetraamine with π acceptor
PublikacjaTwo charge transfer complexes, namely [(BDAH)+(PA−)] CT1 [(BTAH)2+(PA−)2] and CT2 (BDAH = 1,2-benzenediamine, BTAH = 1,2,4,5-benzenetetramine, and PA− = 2,4,6-trinitrophenolate), were synthesized and fully characterized using various spectroscopic techniques. CT1 and CT2 were tested as inhibitors to effectively control the uniform and anodic corrosion processes of copper in an alkaline electrolyte (1.0 M KOH) using various electrochemical...
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RAAS inhibition – a practice of medical progress
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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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Cadmium inhibitory action leads to changes in structure of ferredoxin:NADP+ oxidoreductase
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Synthesis of novel, peptidic kinase inhibitors with cytostatic/cytotoxic activity
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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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Analogi glutaminy jako inhibitory syntazy Glcn-6-P
PublikacjaArtykuł stanowi przegląd stanu wiedzy z ostatnich trzyciestu lat dotyczący inhibitorów syntazy glukozamino-6-fosforanu będących analogami glutaminy, ze szczególnym naciskiem na właściwości wybranych inhibitorów oraz ich syntezę.
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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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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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The new fluorogenic substrates of neutrophil proteinase 3 optimized in prime site region
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A new proteinase 3 substrate with improved selectivity over human neutrophil elastase
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Future of Protease Activity Assays
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Concentration of proteins in the whey stream
PublikacjaZastosowano metodę separacji pianowej do odzyskiwania białka z serwatki. Wykazano silny wpływ prędkości powietrza w kolumnie, początkowego stężenia białka w serwatce i pH roztworu na przebieg i skuteczność flotacji. Współczynnik wzbogacenia maleje ze wzrostem prędkości przepływu powietrza oraz ze wzrostem początkowego stężenia białka serwatkowego. Najwyższą wartość współczynnika wzbogacenia uzyskano dla pH naturalnej serwatki.
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Conservation and diversity of MutS proteins
PublikacjaThe homologues of MutS, mismatch repair protein, exist in all prokaryotes, with the exception of Actinobacteria, Mollicutes and part of the Archaea. Multiple alignments of 316 MutS amino acid sequences from 169 species revealed conserved residues and sequence motifs distinguishing MutS homologues. All MutS homologues show high conservation within the ATPase domain. MutS1, the homologue responsible for DNA mismatch recognition,...