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Wyniki wyszukiwania dla: INHIBITION DBFC
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Increased time varying heart rate and cardiovascular risk in hypertension – Benefit of selective I(f)channel inhibitor?
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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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Peptide splicing in a double‐sequence analogue of trypsin inhibitor SFTI‐1 substituted in the P1 positions by peptoid monomers
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Determination of cathepsin G in endometrial tissue using a surface plasmon resonance imaging biosensor with tailored phosphonic inhibitor
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Inhibiting Activity of HIV-1: Protease, Reverse Transcriptase and Integrase All Together by Novel Compounds Using Computational Approaches
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Synthesis and biological evaluation of novel analogues of batracylin with synthetic amino acids and adenosine: an unexpected effect on centromere segregation in tumor cells through a dual inhibition of topoisomerase IIa and Aurora B
PublikacjaIn the search for new anticancer agents we designed and synthesized batracylin derivatives with linking synthetic amino acid side chains of different lengths and adenosine. Unexpectedly, we have found that in water and the culture media adenosine–amino acid–BAT conjugates form supramolecular structures and this prevents these compounds from entering cells. Consequently, these compounds exerted no biological activity when tested...
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X-ray Photoelectron Spectroscopy studies of various carboxylic acids adsorption on aluminium alloys in alkaline media
Dane BadawczeThis dataset contains the results of high-resolution XPS studies obtained during evaluation of high corrosion inhibition efficiency of various carboxylic acids towards aluminium alloy 5754 in bicarbonate buffer pH=11.
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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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Antitumor triazoloacridinone C-1305 as a potent FLT3 tyrosine kinase inhibitor in human acute myeloid leukemia (AML) cells.
PublikacjaJednym 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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Binding modes of a new epoxysuccinyl–peptide inhibitor of cysteine proteases. Where and how do cysteine proteases express their selectivity?
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New and potent production platform of the acetylcholinesterase inhibitor huperzine A by gamma-irradiated Alternaria brassicae under solid-state fermentation
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Removal of phenolic inhibitor compounds from hydrolysates and post-fermentation broths by using a Hydrophobic Magnetic Deep Eutectic Solvent
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Structure-based design and in vivo anti-arthritic activity evaluation of a potent dipeptidyl cyclopropyl nitrile inhibitor of cathepsin C
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Removal of phenolic inhibitor compounds from hydrolysates and post-fermentation broths by using a Hydrophobic Magnetic Deep Eutectic Solvent
PublikacjaHydroxymethylfurfural (HMF), furfural (FF), hydroquinone (HQ), and vanillin (VAN) are among the main inhibitors generated during most of biomass pre-treatments prior to fermentation processes. They are recognized as toxic to several fermentative microorganisms and therefore cause a decrease in biohydrogen or biofuel production (after hydrolysis). Moreover, if they are released into aqueous solutions (after fermentation), they can...
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Antitumor DNA-Damaging C-1748 is a New Inhibitor of Autophagy that Triggers Apoptosis in Human Pancreatic Cancer Cell Lines
PublikacjaDespite the enormous progress that has been made over the past decades in diagnosis, treatment and prevention of many types of tumors, survival rates in pancreatic cancer still remain poor. Pancreatic cancer is one of the most malignant and chemoresistant tumors and the profound mechanism supporting these phenomena is the constitutively activated prosurvival autophagy. The antitumor 1-nitroacridine derivative C-1748 belongs to...
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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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Design, synthesis and in vitro biological evaluation of a small cyclic peptide as inhibitor of vascular endothelial growth factor binding to neuropilin-1
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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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Induction of unique structural changes in guanine-rich DNA regions by the triazoloacridone C-1305, a topoisomerase II inhibitor with antitumor activities.
PublikacjaCelem pracy było scharakteryzowanie odziaływania związku C-1305 z DNA w porównaniu do innych inhibitorów topoizomerazy II. Badania pokazują, że C-1305 odziaływuje preferencyjnie z parami CG, interkaluje do DNA i zaburza sąsiednie otoczenie w bardzo charakterystyczny sposób, który nie został zaobserwowany u pozostałych 22 badanych związków.
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Trypsin inhibitor, antioxidant and antimicrobial activities as well as chemical composition of potato sprouts originating from yellow- and colored-fleshed varieties
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Activity of Patents in Fuel Cells and Hydrogen Production in the Context of Passenger Car Fleet in the V4 Countries
PublikacjaThe hydrogen market in the world today is capable ovule and em-pirical evidence on activity of patents in fuel cells and hydrogen production islimited so far. Patent applications in zero-emission mobility in the aspect of fuelcells include: DAFC/DMFC&DMFC, PEMFC, SOFC, AFC, PAFC. As for thepatents relating to the hydrogen production, they concern low carbon, electrol-ysis and inorganic. The purpose of the study was to investigate...
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The Effect of Long-Term Administration of Fatty Acid Amide Hydrolase Inhibitor URB597 on Oxidative Metabolism in the Heart of Rats with Primary and Secondary Hypertension
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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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Different expression level of CYP3A4 isoenzyme modulate cellular response of CHO cells following treatment with the CYP3A4 inhibitor, C-1311 compound
PublikacjaEfektywność terapii przeciwnowotworowej może być zmieniana przez różne czynniki. Jednym z ograniczeń jest odmienny u każdego pacjenta poziom enzymów metabolizujących odpowiedzialnych za aktywację i detoksykację leków, co może zmieniać jego odpowiedź na zastosowaną terapię. Co więcej, enzymy metabolizujące często są celem molekularnym wielu ksenobiotyków, co dodatkowo może zmieniać skuteczność terapii. Zatem zrozumienie oddziaływań...
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PdCl2-catalyzed synthesis of a new class of isocoumarin derivatives containing aminosulfonyl / aminocarboxamide moiety: First identification of a isocoumarin based PDE4 inhibitor
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Drug-drug interaction potential of antitumor acridine agent C-1748: The substrate of UDP-glucuronosyltransferases 2B7, 2B17 and the inhibitor of 1A9 and 2B7
PublikacjaBackground The compound 9-(2′-hydroxyethylamino)-4-methyl-1-nitroacridine (C-1748), the promising antitumor agent developed in our laboratory was determined to undergo phase I metabolic pathways. The present studies aimed to know its biotransformation with phase II enzymes – UDP-glucuronosyltransferases (UGTs) and its potential to be engaged in drug-drug interactions arising from the modulation of UGT activity. Methods UGT-mediated...
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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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Inhibiting activity of HIV-1: protease, reverse transcriptase and integrase all together by novel compounds using computational approaches (flexible and rigid docking)
PublikacjaAcquired immunodeficiency syndrome (AIDS), caused by human immunodeficiency virus type 1 (HIV-1) infection, is one of the most challenging diseases in recent decades. Nevertheless the shortcomings of chemical drugs such as toxicity, lack of curative effects, the search for more potent anti-HIV agents have been focused in our study. In current study, novel scaffold was designed having a benzyl and imidazole in it which are very...
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The corrosion studies of 3,4,5-trihydroxybenzoic acid as an effective corrosion inhibitor of low alloy steel
Dane BadawczeThe 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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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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Long range molecular dynamics study of interactions of the eukaryotic glucosamine-6-phosphate synthase with fructose-6-phosphate and UDP-GlcNAc
PublikacjaGlucosamine-6-phosphate synthase (EC 2.6.1.16) is responsible for catalysis of the first and practically irreversible step in hexosamine metabolism. The final product of this pathway, uridine 5 diphospho Nacetyl- d-glucosamine (UDP-GlcNAc), is an essential substrate for assembly of bacterial and fungal cell walls. Moreover, the enzyme is involved in phenomenon of hexosamine induced insulin resistance in type II diabetes, which...
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Need for multiple risk reduction strategies in clinical trials enrolling high risk patients - FOURIER investigating PCSK-9 inhibitor to lower cholesterol revisited
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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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Fluconazole resistant Candida auris clinical isolates have increased levels of cell wall chitin and increased susceptibility to a glucosamine-6-phosphate synthase inhibitor
PublikacjaIn 2009 Candida auris was first isolated as fungal pathogen of human disease from ear canal of a patient in Japan. In less than a decade, this pathogen has rapidly spread around the world and has now become a major health challenge that is of particular concern because many strains are resistant to multiple class of antifungal drugs. The lack of available antifungals and rapid increase of this fungal pathogen provides an incentive...
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DNA-reactive anticancer imidazoacridinone C-1311 is a new inhibitor of hypoxia-inducible factor 1 alpha, vascular endothelial growth factor and tumor angiogenesis
PublikacjaHypoxia-inducible factor 1 (HIF-1) plays a critical role for tumor adaptation to hypoxia and promotes angiogenesis. Antitumor imidazoacridinone C-1311 is a DNA reactive topoisomerase II and FLT3 receptor tyrosine kinase inhibitor selected for phase II clinical trials for breast cancer. Here, we demonstrate the new mechanism of C-1311 action involving HIF-1a, vascular endothelial growth factor (VEGF) and angiogenesis as additional...
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In vitro and in silico assessment of anti-inflammatory activity of cocoa powders
PublikacjaPlants are considered the major sources of biologically active compounds, which provide unlimited opportunities for their use either as medical treatments or as novel drug formulations. Cocoa powder is frequently used in nutrition and is known to have many benefits thanks to its wide range of biological activities. The presented study was focused on th evaluation of the anti-inflammatory potential of extracts obtained from cocoa...
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Targeting of FLT3-ITD kinase contributes to high selectivity of imidazoacridinone C-1311 against FLT3-activated leukemia cells
PublikacjaDrugs targeting receptor tyrosine kinase FLT3 are of particular interest since activating FLT3-internal tandem duplication (ITD) mutations abundantly occur in fatal acute myeloid leukemias (AMLs). Imidazoacridinone C-1311, a DNA-reactive inhibitor of topoisomerase II, has been previously shown to be a potent and selective inhibitor of recombinant FLT3. Here, we expand those findings by studying its effect on leukemia cells with...
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The PARAGON Heart Failure trial – ongoing investigation of the angiotensin receptor antagonist/neprilysin inhibitor sacubitril/valsartan in heart failure patients with hypertension and preserved ejection fraction
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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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The synthesis and biological activity of lipophilic derivatives of bicine conjugated with n3-(4-methoxyfumaroyl)-l-2,3-diaminopropanoic acid(fmdp) - an inhibitor of glucosamine-6-phosphate synthase
PublikacjaOtrzymano serię pochodnych bicyny połączonych z inhibitorem syntazy glukozamino-6-fosforanu (fmdp)oraz zbadano ich właściwości lipofilowe i aktywność przeciwgrzybową. otrzymane związki charakteryzowały się wyższą llipofilowością niż fmdp. wszystkie otrzymane związki wykazywały także wyższą aktywność przeciwgrzybową niż fmdp.
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Selectivity Tuning by Natural Deep Eutectic Solvents (NADESs) for Extraction of Bioactive Compounds from Cytinus hypocistis—Studies of Antioxidative, Enzyme-Inhibitive Properties and LC-MS Profiles
PublikacjaIn the present study, the extracts of Cytinus hypocistis (L.) L using both traditional solvents (hexane, ethyl acetate, dichloromethane, ethanol, ethanol/water, and water) and natural deep eutectic solvents (NADESs) were investigated in terms of their total polyphenolic contents and antioxidant and enzyme-inhibitive properties. The extracts were found to possess total phenolic and total flavonoid contents in the ranges of 26.47–186.13...
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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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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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Effect of new bisacridines IKE16, IKE18 and IE10 on the yeast topoisomerase II relaxation activity
Dane BadawczeThe datasets contain the results of new bisacridines IKE16, IKE18 and IE10 inhibition activity against yeast topoisomerase II. DNA topoisomerases (Topo) are enzymes that catalyze changes in the spatial structure of DNA and play an important role in replication, transcription and recombination. Beyond their normal functions, DNA topo are significant...
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Structural motifs in the Cu(II), Mn(II) and Zn(II) complexes based on N,N,N-donor dipodal or N,N,N,N-donor tripodal ligands obtained in situ: Synthesis, crystal structures and xanthine oxidase inhibition properties
PublikacjaA series of four novel transition metal complexes, [Cu(NCS)2L1] (1), [Mn(NCS)2L1] (2) where L1 = bis(1-(3,5-dimethylpyrazolyl)methyl)amine, [Mn(NCS)2L2] (3) and [Zn(NCS)L2]2[Zn(NCS)4] (4) where L2 = tris(1-(3,5-dimethylpyrazolyl)methyl)amine, has been obtained in situ by a one-step, one-pot synthetic path starting from 1-hydroxymethyl-3,5-dimethylpyrazole (L). The isolated complexes were fully characterised by elemental analysis,...
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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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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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Long range molecular dynamics study of regulation of eukaryotic glucosamine-6-phosphate synthase activity by UDP-GlcNAc
PublikacjaGlucosamine-6-phosphate (GlcN-6-P) synthase catalyses the first and practically irreversible step in hexosamine metabolism. The final product of this pathway, uridine 5' diphospho N-acetyl-D-glucosamine (UDPGlcNAc), is an essential substrate for assembly of bacterialand fungal cell walls. Moreover, the enzyme is involved in phenomenon of hexosamine induced insulin resistance in type II diabetes, which makes it a potential target...
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Ageing-Time Dependent Changes of Angiotensin I-Converting Enzyme-Inhibiting Activity of Protein Hydrolysates Obtained from Dry-Cured Pork Loins Inoculated with Probiotic Lactic Acid Bacteria
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