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Glutamine analogues containing a keto function - novel inhibitors of fungal glucosamine-6-phosphate synthase
PublicationW publikacji przedstawiono syntezę nowych pochodnych kwasu (S)-2,3-diaminopropanowego, zawierających reszty kwasów z funkcją ketonową. Dla otrzymanych związków zbadano właściwości inhibicyjne w stosunku do grzybowej syntazy glukozamino-6-fosforanu, ustalono właściwości lipofilowe otrzymanych związków a także aktywność przeciwgrzybową. Dla kilku wybranych pochodnych otrzymano ich dipeptydy, zbadano także ich aktywność przeciwgrzybową...
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The biological role of prolyl oligopeptidase and the procognitive potential of its peptidic inhibitors from food proteins
PublicationProlyl 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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Structure-based design and evaluation of novel N-phenyl-1H-indol-2-amine derivatives for fat mass and obesity-associated (FTO) protein inhibition
PublicationFat mass and obesity-associated (FTO) protein contributes to non-syndromic human obesity which refers to excessive fat accumulation in human body and results in health risk. FTO protein has become a promising target for anti-obesity medicines as there is an immense need for the rational design of potent inhibitors to treat obesity. In our study, a new scaffold N-phenyl-1H-indol-2-amine was selected as a base for FTO protein inhibitors...
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Cholinesterase inhibitory activity, antioxidative potential and microbial stability of innovative liver pâté fortified with rosemary extract (Rosmarinus officinalis)
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Potential DPP IV Inhibitory Peptides from Dry-Cured Pork Loins after Hydrolysis: An In Vitro and In Silico Study
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Inhibitory syntazy glukozamino-6-fosforanu o zwiększonej lipofilowości i ich peptydy - synteza i właściwości biologiczne
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Corrosion-inhibiting effect of Mimosa extract on brass-MM55 corrosion in 0.5 M H2SO4 acidic media
PublicationEkstrakt z mimosy był badany jako inhibitor korozji mosiądzu MM55 przy użyciu Elektrochemicznej Spektroskopii Impedancyjnej oraz techniki polaryzacyjnej. Badania te wykazały, że ekstrakt z mimosy wykazuje właściwości inhibitora anodowego. Własności inhibicyjne badanego ekstraktu rosły wraz ze wzrostem stężenia inhibitora w kwasie, związano to ze wzrostem adsorpcji cząsteczek inhibitora na powierzchni metalu.
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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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Investigation of peptide splicing using two‐peptide‐chain analogs of trypsin inhibitor SFTI‐1
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Surface plasmon resonance imaging biosensor for cathepsin G based on a potent inhibitor: Development and applications
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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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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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Do not die, become senescent: a new type of cellular resistance induced by topoisomerase II inhibitors in tumor cells with functional p53
PublicationJednym 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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Alternative and New Protein Sources
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Future of Protease Activity Assays
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On the Origin of Protein Superfamilies and Superfolds
PublicationDistributions of protein families and folds in genomes are highly skewed, having a small number of prevalent superfamiles/superfolds and a large number of families/folds of a small size. Why are the distributions of protein families and folds skewed? Why are there only a limited number of protein families? Here, we employ an information theoretic approach to investigate the protein sequence-structure relationship that leads to...
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Stabilizing agents and protein stability
PublicationBiałka są kluczowymi elementami żywych organizmów, jak również efektywnymi katalizatorami w biotechnologii i medycynie. Szybki rozwój wielu gałęzi biotechnologii wiąże się z coraz większym zapotrzebowaniem na produkty białkowe charakteryzujące się wysoką stabilnością. Jednym ze sposobów osiągnięcia większej stabilności białek jest wykorzystanie małych związków organicznych, tzw. osmolitów. Do tej grupy związków należą aminokwasy,...
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Colloidal aspects of protein digestion
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Protect our right to light
Publication“The struggle for light” is how the Swiss architect Le Corbusier described the history of architecture in 1935. Today, with the skies crowded out by buildings in modern cities, those words should ring in the ears of policymakers and planners. Skyscraper construction is booming. China is the leader, last year completing 88 of the 143 buildings around the world that are taller than 200 metres (see ‘Vertical growth’). As the nation’s...
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Structure-activity relationship study of tetrapeptide inhibitors of the Vascular Endothelial Growth Factor A binding to Neuropilin-1
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Flavonoids as tyrosinase inhibitors in in silico and in vitro models: basic framework of SAR using a statistical modelling approach
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Development of Biocompatible Fe3O4@SiO2 Nanoparticles as Subcellular Delivery Platform for Glucosamine-6-phosphate Synthase Inhibitors
PublicationNumerous inhibitors of glucoseamine-6-phophate synthase (GlcN-6-P), the enzyme responsible from catalysis of the first step of metabolic pathway leading to metabolism 5’-diphospho-N-acetyl-D- glucosamine, were reported as effective agents for inhibiting the growth of various fungal pathogens. Among the reported inhibitors,...
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Structure–activity relationships study on biological activity of peptides as dipeptidyl peptidase IV inhibitors by chemometric modeling
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Inhibitors and Antibody Fragments as Potential Anti-Inflammatory Therapeutics Targeting Neutrophil Proteinase 3 in Human Disease
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LY294002 and sorafenib as inhibitors of intracellular survival pathways in the elimination of human glioma cells by programmed cell death
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Effect of selected ammonia escape inhibitors on carbon dioxide capture and utilization via calcium carbonate precipitation
PublicationCarbon dioxide was used to precipitate CaCO3 with CaCl2 solution in the presence of NH3 as a CO2 absorption promoter. Compounds that were previously indicated as inhibitors of ammonia escape during CO2 absorption were also added to the reaction mixture. Inorganic salts, i.e. ZnCl2, CuCl2, CoCl2, and organic substances, i.e. glycerol, ethylene glycol and triethanolamine were tested inhibitors in this work. A model post-distillation...
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Chloroacridine derivatives as potential anticancer agents which may act as tricarboxylic acid cycle enzyme inhibitors
PublicationThe chloroacridines affect biological forms of melanoma in different ways. Amelanotic (Ab) melanoma (with inhibited melanogenesis and higher malignancy) was particularly sensitive to the action of the chloroacridines. The Ab melanoma cells died through apoptosis and through death without caspase activation. Diminished activity of TAC enzymes was noticed among Ab melanoma cells together with ATP/NAD depletion, especially in the...
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The Distribution of Glucosinolates in Different Phenotypes of Lepidium peruvianum and Their Role as Acetyl- and Butyrylcholinesterase Inhibitors—In Silico and In Vitro Studies
PublicationThe aim of the study was to present the fingerprint of different Lepidium peruvianum tu- ber extracts showing glucosinolates-containing substances possibly playing an important role in preventinting dementia and other memory disorders. Different phenotypes of Lepidium peruvianum (Brassicaceae) tubers were analysed for their glucosinolate profile using a liquid chromatograph coupled with mass spectrometer (HPLC-ESI-QTOF-MS/MS platform)....
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Design of new cholinesterase inhibitors based on phosphorus analogs of tacrine as potential anti-Alzheimer’s disease agents
PublicationBased on the analysis of the determined free binding energy (using the AutoDock Vina 1.1.2 docking program), the most potent cholinesterase inhibitors were selected. Moreover, studies of 3D visualization of the results of molecular modeling led to the identification of potential sites for the interaction of new potential inhibitors with amino acid residues building active sites of investigated cholinesterases.
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Emerging anticancer activity of candidal glucoseamine-6-phosphate synthase inhibitors upon nanoparticle-mediated delivery
PublicationNumerous glutamine analogues have been reported as irreversible inhibitors of the glucosamine-6-phosphate (GlcN-6-P) synthase in pathogenic Candida albicans in the last 3.5 decades. Among the reported inhibitors, the most effective N3-(4-methoxyfumaroyl)-L-2,3- diaminopropanoic acid (FMDP) has been extensively studied in order to develop its more active analogues. Several peptide−FMDP conjugates were tested to deliver FMDP to its...
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The influence of food phytochemicals on cyclic phosphodiesterase 4 (PDE4) activity
PublicationCyclic 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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Endocrine responses following exhaustive strength exercise with and without the use of protein and protein-carbohydrate supplements
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The importance of the shape of the protein–water interface of a kinesin motor domain for dynamics of the surface atoms of the protein
PublicationA single kinesin motor domain immersed in water has been investigated using molecular dynamics. It has been found that local properties of water in the solvation shell change along with the nature of the neighboring protein surface. However, a detailed analysis leads to the conclusion that the geometrical features of hydrogen bonds and overall structure of kinesin hydration water are not very different from bulk water. The local...
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The importance of the shape of the protein-water interface of a kinesin motor domain for dynamics of the surface atoms of the protein
PublicationSingle kinesin motor domain immersed in water has been investigated using molecular dynamics. It has been found that local properties of water in solvation shell change along with the nature of neighboring protein surface. However, a detailed analysis leads to the conclusion that the geometrical features of hydrogen bonds and overall structure of kinesin hydration water is not very different from bulk water. The local values of...
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Recent progress in the development of steroid sulfatase inhibitors – examples of the novel and most promising compounds from the last decade
PublicationThe purpose of this review article is to provide an overview of recent achievements in the synthesis of novel steroid sulfatase (STS) inhibitors. STS is a crucial enzyme in the biosynthesis of active hormones (including estrogens and androgens) and, therefore, represents an extremely attractive molecular target for the development of hormone-dependent cancer therapies. The inhibition of STS may effectively reduce the availability...
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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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Investigation of Serine‐Proteinase‐Catalyzed Peptide Splicing in Analogues of Sunflower Trypsin Inhibitor 1 (SFTI‐1)
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Sprawność elastycznych protez stóp w kontekście współczesnych materiałów
PublicationKlasyfikacja protez stóp opiera się głównie na ich zachowaniu w momencie kontaktu z podłożem. Pod tym względem wyróżniamy stopy sztywne oraz sprężyste, charakteryzujące się możliwością tłumienia drgań i magazynowania oraz uwalniania energii. Współczesne elastyczne protezy stóp przeznaczone dla osób wykazujących wysoką i bardzo wysoką aktywność wytwarzane są z materiałów kompozytowych zawierających włókna węglowe. W zależności od...
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Occlusion phenomenon of redox probe by protein as a way of voltammetric detection of non-electroactive C-reactive protein
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Novel steroid sulfatase inhibitors based on N ‐thiophosphorylated 3‐(4‐aminophenyl)‐coumarin‐7‐O‐sulfamates
PublicationIn the present work, we described convenient methods for the synthesis ofN-thiophosphorylated 3-(4-aminophenyl)-coumarin-7-O-sulfamates as steroid sulfatase(STS) inhibitors. To design the structures of the potential STS inhibitors, molecularmodeling techniques were used. A computational docking method was used to deter-mine the binding modes of the synthesized inhibitors as well as to identify potentialinteractions between specified...
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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
PublicationA 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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Antifungal activity of L-homoserine O-acetyltransferase (CaMet2p) inhibitors.
Open Research DataThe dataset contains a set of optical densities at 600 nm measured at microplate reader to determine the rate of fungal growth in the presence of Candida albicans homoserine O-acetyltransferase inhibitors. Antifungal activities were determined against several strains from Candida spp. and others by the modified M27-A3 method specified by the CLSI. We...
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Indukcja procesu pseudostarzenia komórkowego przez inhibitory DNA topoizomerazy II i jego rola w oporności na leki przeciwnowotworowe
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New Polymethoxyflavones from Hottonia palustris Evoke DNA Biosynthesis-Inhibitory Activity in An Oral Squamous Carcinoma (SCC-25) Cell Line
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Gamma irradiation mediated production improvement of some myco-fabricated nanoparticles and exploring their wound healing, anti-inflammatory and acetylcholinesterase inhibitory potentials
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Crystallographic studies of piperazine derivatives of 3-methyl-5-spirofluorenehydantoin in search of structural features of P-gp inhibitors
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