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Search results for: PROTEINASE INHIBITORS
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Anticandiadal properties of N-acylpeptides containing inhibitor of glucosamine-6-phosphate synthase
PublicationOtrzymano 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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Consequences of cathepsin C inactivation for membrane exposure of proteinase 3, the target antigen in autoimmune vasculitis
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Aktywność przeciwgrzybowa koniugatów inhibitorów enzymatycznych z nośnikami peptydowymi
PublicationCelem badań przedstawionych w rozprawie było określenie aktywności przeciwgrzybowej szeregu związków będących koniugatami peptydów z inhibitorami enzymatycznymi (FMDP, cispentacyna). Zakres badań obejmował zbadanie aktywności peptydów-FMDP, CPP oraz FMDP-CPP wobec grzybów z rodzaju Candida w różnego typu podłożach, określenie możliwości powstawania oporności na FMDP-CPP i peptydy-FMDP, a także określenie szybkości transportu i...
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Variability of Hordeum vulgare L. Cultivars in Yield, Antioxidant Potential, and Cholinesterase Inhibitory Activity
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Selection of New Chromogenic Substrates of Serine Proteinases Using Combinatorial Chemistry Methods
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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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Application of specific cell permeable cathepsin G inhibitors resulted in reduced antigen processing in primary dendritic cells
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Synthesis and biological evaluation of N-acylated tyramine sulfamates containing C-F bonds as steroid sulfatase inhibitors
PublicationSteroid sulfatase (STS) is responsible for the hydrolysis of biologically inactive sulfated steroids into their active un-sulfated forms and promotes the growth of various hormone-dependent cancers (e.g., breast cancer). Therefore, the STS enzyme is a promising therapeutic target for the treatment of steroid-sensitive cancers. Herein, we report the synthesis and biological evaluation of sulfamate analogs as potential STS inhibitors...
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Correction to “Emerging Anticancer Activity of Candidal Glucosamine-6-Phosphate Synthase Inhibitors upon Nanoparticle-Mediated Delivery”
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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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Does GISSI-AF change the concept of using RAS inhibitors in the primary prevention of atrial fibrillation in hypertensive patients?
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Structural and Evolutionary Analysis Indicate that the SARS-CoV-2 Mpro is an Inconvenient Target for Small-Molecule Inhibitors Design
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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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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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Divulging the anti-acetylcholinesterase activity of Colletotrichum lentis strain KU1 extract as sustainable AChE active site inhibitors
PublicationAlzheimer’s disease (AD), also called senile dementia is a neurodegenerative disease seen commonly in the elderly and is characterised by the formation of β-amyloid plaques and neurofbrillary tangles (NFT). Though a complete understanding of the disease is lacking, recent studies showed the role of the enzyme acetylcholinesterase (AChE) in pathogenesis. Finding new lead compounds from natural sources has always been a quest for...
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Molecular modelling of transition state analogue inhibitors of glucosamine-6-P synthase and glucose-6-P isomerase.
PublicationStruktura kompleksu 2-amino-2-deoksy-D-glucitolo-6-P (ADGP) z centrum aktywnym syntazy GlcN-6-P z E. coli została wykorzystAna jako punkt wyjścia do modelowania molekularnego analogów ADGP. Używając programu GROMOS96 wygenerowano konformacje analogów o najniższych energiach wewnętrznych, które następnie ''dokowano'' w centrum aktywnym enzymu. Dokonano syntezy wybranych związków i określono parametry kinetyczne i termodynamiczne...
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The measurement of conformational stability of proteins adsorbed on siloxanes
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1.21 Computation of Structure, Dynamics, and Thermodynamics of Proteins
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Coarse-Grained Models of Proteins: Theory and Applications
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Computational techniques for efficient conformational sampling of proteins
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Design and synthesis of new substrates of HtrA2 protease
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Molecular basis of TRF proteins and their interactions with peptides
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Applications of Unnatural Amino Acids in Protease Probes
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Potentilla erecta extract inhibits arterial thrombosis in rat
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Novel Potential Binding Sites for Selective Inhibitor Design of Human Soluble Epoxide Hydrolase
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Vitamin B9 as a new eco-friendly corrosion inhibitor for copper in 3.5% NaCl solution
PublicationFolic acid salt (sodium folate) was studied as an eco-friendly and non-toxic copper corrosion inhibitor in 3.5% NaCl solution. Electrochemical impedance spectroscopy, polarization resistance and weight-loss measurements show that the inhibitor efficiency increases with concentration (the highest value- approx. 96% was reported for the solution containing 16 mM sodium folate after 24 h). EIS data and Tafel plots indicate that sodium...
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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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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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Synthesis of Cyano-Benzylidene Xanthene Synthons Using a Diprotic Brønsted Acid Catalyst, and Their Application as Efficient Inhibitors of Aluminum Corrosion in Alkaline Solutions
PublicationNovel 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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Enzymes of the L-methionine biosynthesis pathway in Candida albicans as potential novel targets for antifungal chemotherapy
PublicationFungal pathways of essential amino acids biosynthesis provide an abundant source of molecular targets for new antifungal compounds, among which the L-methionine biosynthesis pathway (MBP) may be promising. In this dissertation I characterized three C. albicans enzymes involved in MBP: homoserine O-acetyltransferase (CaMet2p), O-acetyl-L-homoserine sulfhydrylase (CaMet15p), and cystathionine-γ-synthase (CaStr2p). I performed crystallization...
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Both activating and inhibitory Fc gamma receptors mediate rituximab-induced trogocytosis of CD20 in mice
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ACE Inhibitory Properties and Phenolics Profile of Fermented Flours and of Baked and Digested Biscuits from Buckwheat
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Enhanced sorption of inhibitory compounds from fermentation broth using a MOF@pseudo-DES composite
PublicationThe increase in biorefinery processes underscores the need for effective biofuel generation; nevertheless, inhibitors such as hydroquinone (HQ), 5-hydroxymethylfurfural (HMF), furfural (FF), and vanillin (VAN) resulting from biomass degradation impede microbial growth and process efficiency. Herein, a deep eutectic solvent (DES)-like substance was in-situ generated on the surface of NH2-UiO-66 via a post-synthetic coating process...
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Discussion on 3-hydroxy-3-methylglutaryl-coenzyme a reductase inhibitors reduce human pancreatic cancer cell invasion and metastasis
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Separate synthesis and evaluation of glucitol bis-phosphate and mannitol bis-phosphate, as competitive inhibitors of fructose bis-phosphate aldolases
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Analysis of Procollagen C-Proteinase Enhancer-1/Glycosaminoglycan Binding Sites and of the Potential Role of Calcium Ions in the Interaction
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Neutrophil proteinase 3 and dipeptidyl peptidase I (cathepsin C) as pharmacological targets in granulomatosis with polyangiitis (Wegener granulomatosis)
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Design, Synthesis, and Enzymatic Evaluation of Novel ZnO Quantum Dot-Based Assay for Detection of Proteinase 3 Activity
PublicationHerein, the synthesis and application of functionalized quantum dot-based protease probes is described. Such probes are composed of nontoxic ZnO nanocrystals decorated by amino groups followed by linker and labeled peptide attachment. Spherical NH2-terminated ZnO quantum dots (QDs) with the average size ranging from 4 to 8 nm and strong emission centered at 530 nm were prepared using the sol−gel method. The fluorescence of ZnO...
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New Selective Peptidyl Di(chlorophenyl) Phosphonate Esters for Visualizing and Blocking Neutrophil Proteinase 3 in Human Diseases
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Proteinase release from activated neutrophils in mechanically ventilated patients with non-COVID-19 and COVID-19 pneumonia
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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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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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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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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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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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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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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.