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Wyniki wyszukiwania dla: inhibitory enzymu
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Highly Specific Substrates of Proteinase 3 Containing 3-(2-Benzoxazol-5-yl)-l-alanine and Their Application for Detection of This Enzyme in Human Serum
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Two small RNAs conserved in Enterobacteriaceae provide intrinsic resistance to antibiotics targeting the cell wall biosynthesis enzyme glucosamine-6-phosphate synthase
PublikacjaFormation of glucosamine-6-phosphate GlcN6P) by enzyme GlcN6P synthase (GlmS) represents the first step in bacterial cell envelope synthesis. In Escherichia coli, expression of glmS is controlled by small RNAs (sRNAs) GlmY and GlmZ. GlmZ activates the glmS mRNA by base-pairing. When not required, GlmZ is bound by adapter protein RapZ and recruited to cleavage by RNase E inactivating the sRNA. The homologous sRNA GlmY activates...
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Enzymy o aktywności aminotransferazy kwasu L-α-aminoadypinowego z Candida albicans - właściwości i rola w metabolizmie komórki grzybowej
PublikacjaCandida albicans jest elementem naturalnej flory drobnoustrojowej człowieka. Podobieństwo komórek grzybowych i ssaczych, wzrost częstości występowania infekcji grzybiczych wraz ze stopniowym wzrostem pojawiania się oporności patogenów stwarza potrzebę poszukiwania nowych związków przeciwgrzybowych. Jedną z dróg obraną przez naukowców jest analiza szlaków biosyntezy aminokwasów egzogennych dla człowieka. Przedmiotem badań w ramach...
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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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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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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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Simultaneous impedance and volumetric studies and additionally potentiodynamic polarization measurements of molasses as a carbon steel corrosion inhibitor in 1M hydrochloric acid solution
PublikacjaThe inhibition effect of molasses on the corrosion of low carbon steel in 1M hydrochloric acid solution was investigated by volumetric and electrochemical measurements. Potentiodynamic polarization and dynamic electrochemical impedance spectroscopy (DEIS) results were obtained and compared with to those, obtained with the hydrogen evolution technique. All results indicate that molasses functioned as a good inhibitor in 1M hydrochloric...
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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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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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Phytochemical screening and biological evaluation of Greek sage (Salvia fruticosa Mill.) extracts
PublikacjaThis study explores the influence of extraction solvents on the composition and bioactivity of Salvia fruticosa extracts. Ultrasound-assisted extraction with water, ethanol and their mixtures in variable proportions was used to produce four different extracts. An untargeted UPLC/MS‑based metabolomics was performed to discover metabolites profile variation between the extracts. In the analyzed samples, 2704 features had been detected,...
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Mrówczan sodu z nowym pakietem inhibitorów korozji jako ekologiczny środek do odladzania infrastruktury lotniczej.
PublikacjaPrzedstawiono wyniki badań korozji kadmowej powłoki na stali oraz korozji po zanurzeniu stopów metali w mrówczanie sodu z nowym pakietem inhibitorów korozji, zawierającym synergiczną kompozycję poliasparaginianu sodu oraz imidazolu. Ponadto wyznaczono zdolność penetracji lodu przez badany układ. Właściwo- ści opracowanej kompozycji odladzającej porównano z właściwościami środków dostępnych na rynku. Uzyskane wyniki wskazują, że otrzymany...
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Nowe estrowe i amidowe pochodne inhibitorów syntazy glukozamino-6-fosforanu - synteza i aktywność biologiczna
PublikacjaPrzedmiotem rozprawy doktorskiej są modyfikacje chemiczne analogów glutaminy – kwasu N3-(4-metoksyfumaroilo)-S-2,3-diaminopropanowego (FMDP) oraz kwasu N3-[(E)-4-fenylo-4-okso-2-butenoilo]-S-2,3-diaminoaminopropanowego (BADP). Związki te są inhibitorami syntazy glukozamino-6-fosforanu i mimo ich silnych właściwości inhibicyjnych, nie wykazują zdolności do hamowania wzrostu drobnoustrojów. Brak aktywności przeciwdrobnoustrojowej...
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Genistein inhibits activities of methylenetetrahydrofolate reductase and lactate dehydrogenase, enzymes which use NADH as a substrate
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Antioxidative enzymes and expression of rbcL gene as tools to monitor heavy metal-related stress in plants
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Melatonin stimulates the activity of protective antioxidative enzymes in myocardial cells of rats in the course of doxorubicin intoxication
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Źródła, otrzymywanie i przydatność niektórych termostabilnych enzymów w przetwórstwie skrobi i mleka
PublikacjaPrezentowane wyniki wskazują na możliwość usprawnienia produkcji syropów skrobiowych przez zastosowanie rekombinantowej alfa-amylazy z Pyrococcus woesei i termostabilnej alfa-glukozydazy z Thermus thermophilus. Wykazano także przydatność rekombinantowej, termosta-bilnej beta-galaktozydazy z Pyrococcus woesei do wytwarzania bez-laktozowego mleka i serwatki. Enzym ten wykazuje dużą termostabil-ność i znaczną aktywność w szerokim...
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Molecular Characterization of a Novel Lytic Enzyme LysC from Clostridium intestinale URNW and Its Antibacterial Activity Mediated by Positively Charged N-Terminal Extension
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Synthesis of 3-indolylmethyl substituted (pyrazolo/benzo)triazinone derivatives under Pd/Cu-catalysis: Identification of potent inhibitors of chorismate mutase (CM)
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Experimental and Machine-Learning-Assisted Design of Pharmaceutically Acceptable Deep Eutectic Solvents for the Solubility Improvement of Non-Selective COX Inhibitors Ibuprofen and Ketoprofen
PublikacjaDeep eutectic solvents (DESs) are commonly used in pharmaceutical applications as excellent solubilizers of active substances. This study investigated the tuning of ibuprofen and ketoprofen solubility utilizing DESs containing choline chloride or betaine as hydrogen bond acceptors and various polyols (ethylene glycol, diethylene glycol, triethylene glycol, glycerol, 1,2-propanediol, 1,3-butanediol) as hydrogen bond donors. Experimental...
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Experimental and Machine-Learning-Assisted Design of Pharmaceutically Acceptable Deep Eutectic Solvents for the Solubility Improvement of Non-Selective COX Inhibitors Ibuprofen and Ketoprofen
PublikacjaDeep eutectic solvents (DESs) are commonly used in pharmaceutical applications as excellent solubilizers of active substances. This study investigated the tuning of ibuprofen and ketoprofen solubility utilizing DESs containing choline chloride or betaine as hydrogen bond acceptors and various polyols (ethylene glycol, diethylene glycol, triethylene glycol, glycerol, 1,2-propanediol, 1,3-butanediol) as hydrogen bond donors. Experimental...
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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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Anti-cancer effect of Rumex obtusifolius in combination with arginase/nitric oxide synthase inhibitors via downregulation of oxidative stress, inflammation, and polyamine synthesis
PublikacjaCancer continues to be a leading cause of death worldwide, making the development of new treatment methods crucial in the fight against it. With cancer incidence rates increasing worldwide, ongoing research must focus on identifying new and effective ways to prevent and treat the disease. The combination of herbal extracts with chemotherapeutic agents has gained much interest as a novel strategy to combat cancer. Rumex obtusifolius...
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Regulacja topologii DNA przez topoizomerazę typu II, czyli jak struktura DNA wpływa na funkcjonowanie genów
PublikacjaW wielu ważnych procesach jakie zachodzą w komórce zmienia się topologia DNA i struktura chromatyny. Enzym, topoizomeraza typu II, jest jednym z ważnych czynników, który reguluje zmiany topologiczne i strukturalne w jądrze, przez co ma bezpośredni lub pośredni wpływ na takie procesy jak uporządkowanie struktury chromatyny poprzez wiązanie pętli chromatyny do szkieletu jądrowego, transkrypcję i replikację DNA, reperację uszkodzeń...
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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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Analiza in silico bioaktywnych peptydów pochodzących z keratyny z piór drobiowych
PublikacjaKeratyna należy do najbardziej powszechnie występujących białek strukturalnych pochodzenia zwierzęcego. Stanowi ok. 90% masy piór wytwarzanych w dużych ilościach przez przemysł drobiarski. Ten odpadowy produkt pozostaje w dużym stopniu niezagospodarowany. Celem pracy była analiza bioinformatyczna pierwszorzędowej struktury keratyny z piór kurzych pod kątem występowania w niej peptydów bioaktywnych....
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Homoisocitrate dehydrogenase from Candida albicans: properties, inhibition, and targeting by an antifungal pro-drug
PublikacjaThe LYS12 gene from Candida albicans, coding for homoisocitrate dehydrogenase was cloned and expressed as a His-tagged protein in Escherichia coli. The purified gene product catalyzes the Mg2+- and K+-dependent oxidative decarboxylation of homoisocitrate to alpha-ketoadipate. The recombinant enzyme demonstrates strict specificity for homoisocitrate. SDS-PAGE of CaHIcDH revealed its molecular mass of 42.6±1 kDa, while in size-exclusion...
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The psychrotrophic yeast Sporobolomyces roseus LOCK 1119 as a source of a highly active aspartic protease for the in vitro production of antioxidant peptides
PublikacjaA psychrotrophic yeast strain producing a cold-adapted protease at low temperature was classified as Sporobolomyces roseus. In standard YPG medium, S. roseus LOCK 1119 synthesized an extracellular protease with an activity of approximately 560 U/L. Optimization of medium composition and process temperature considerably enhanced enzyme biosynthesis; an approximate 70% increase in activity (2060 U/L). The native enzyme was purified...
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Metodyka rozdzielania i oznaczania lotnych inhibitorów fermentacji w brzeczkach fermentacyjnych ciemnej fermentacji, techniką GC-MS
PublikacjaW pracy przedstawiono opracowaną w wyniku badań metodykę identyfikacji i oznaczania inhibitorów fermentacji w brzeczkach fermentacji ciemnej z biomasy ligno-celulozowej, z wykorzystaniem ekstrakcji ciecz-ciecz w sprzężeniu z chromatografią gazową ze spektrometrem mas (LLE-GC-MS). W ramach badań dokonano doboru korzystnych warunków ekstrakcji ciecz-ciecz, w tym: pH, objętości rozpuszczalnika ekstrakcyjnego, czasu ekstrakcji oraz warunków...
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Insect cuticular compounds affect Conidiobolus coronatus (Entomopthorales) sporulation and the activity of enzymes involved in fungal infection
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Modulation of the expression of enzymes metabolizing xenobiotics in rat liver and kidney by oral administration of cabbage and sauerkraut juice.
PublikacjaObydwa soki z kapusty mogą wpływać selektywnie na ekspresję genów zaangażowanych w aktywację i detoksykację kancerogenów. Efekt ten zależy od sposobu traktowania i może zależeć od rodzaju tkanki.
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Teloxantron inhibits the processivity of telomerase with preferential DNA damage on telomeres
PublikacjaTelomerase reactivation is one of the hallmarks of cancer, which plays an important role in cellular immortalization and the development and progression of the tumor. Chemical telomerase inhibitors have been shown to trigger replicative senescence and apoptotic cell death both in vitro and in vivo. Due to its upregulation in various cancers, telomerase is considered a potential target in cancer therapy. In this study, we identified...
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Antarctic marine bacterium Pseudoalteromonas sp. 22b as a source of cold adapted á-galaktosidase.
PublikacjaAntarktyczny morski szczep Pseudoalteromonas sp. 22b. jest źródłem wewnątrzkomórkowej beta-galaktozy. Enzym ten wykazuje wysoką aktywność hydrolizy laktozy w zakresie temperatur od 0 do 20 st. C oraz pH 6,0-8,0. W niniejszej pracy opisano metodykę uzyskania homogennego preparatu tego enzymu, oraz pełną charakterystykę jego własności enzymatycznych i kinetycznych.
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Solubilization of keratins and functional properties of their isolates and hydrolysates
PublikacjaThe keratinous wastes of the textile industry and poultry slaughterhouses may be used as sources of soluble keratins or hydrolysates. This review presents methods for processing raw keratin-based materials into bioproducts with functional and bioactive properties suitable for biomedical, cosmetic, food, and agricultural applications. Soluble keratin can be obtained by thermal treatment in some organic solvents, reduction, or oxidation...
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Design, synthesis, and molecular docking of new 5-HT reuptake inhibitors based on modified 1,2-dihydrocyclopenta[b] indol-3(4H)-one scaffold
PublikacjaA new group of serotonin reuptake inhibitors containing 1,2-dihydrocyclopenta[b]indol-3(4H)-one scaffoldwas synthesized, starting from indole 5-((1H-indol-3-yl)(1,3-dioxane-4,6-diones as a key intermediates. Following three transformations including intramolecular cyclization and formation of imines, a series of new ligand for human serotonin transporter was obtained. The ability of these ligands to inhibit human TS3 serotonin transporter...
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New potent steroid sulphatase inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives
PublikacjaIn the present work, we report a new class of potent steroid sulphatase (STS) inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives. Within the set of new STS inhibitors, 6-(1-(1,2,3-trifluorophenyl)-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate 3L demonstrated the highest activity in the enzymatic assay inhibiting the STS activity to 7.98% at 0.5 µM concentration. Furthermore, to verify...
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Hydrophobic derivatives of 2-amino-2-deoxy-D-glucitol-6-phosphate: a newtype of D-glucosamine-6-phosphate synthase inhibitors with antifungal action.
PublikacjaDokonano syntezy szeregu N-acylowych i estrowych pochodnych 2-amino-2-deok-sy-glucitolo-6-fosforanu (ADGP) i zbadano ich aktywność przeciwgrzybową oraz wobec enzymów zaangażowanych we wczesne etapy biosyntezy chityny w komórkach grzybów. Wszystkie badane pochodne okazały się słabszymi inhibitorami enzymu syntezy GlcN-6-P aniżeli ADGP, ale niektóre z nich wykazywały znacznie wyższą aktywność przeciwgrzybową niż związek macierzysty....
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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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Support Materials of Organic and Inorganic Origin as Platforms for Horseradish Peroxidase Immobilization: Comparison Study for High Stability and Activity Recovery
PublikacjaIn the presented study, a variety of hybrid and single nanomaterials of various origins were tested as novel platforms for horseradish peroxidase immobilization. A thorough characterization was performed to establish the suitability of the support materials for immobilization, as well as the activity and stability retention of the biocatalysts, which were analyzed and discussed. The physicochemical characterization of the obtained...
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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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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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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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Comparative molecular dynamics study of dimeric and monomeric forms of HIV-1 protease in ligand bound and unbound state
PublikacjaHuman immunodeficiency virus type 1 protease (HIV-1 PR) is a viral-encoded enzyme that forms a homodimer. HIV-1 PR is essential for replication and assembly of the virus and inactivation of HIV-1 PR enzyme causes production of immature, noninfectious viral particles and thus HIV-1 PR is an attractive target in anti-AIDS drug design. In our current work, we performed molecular dynamics (MD) calculations (500 ns) for two different...
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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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Efficacy and safety of B-cell receptor signaling pathway inhibitors in relapsed/refractory chronic lymphocytic leukemia: a systematic review and meta-analysis of randomized clinical trials
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Development of Sulfamoylated 4‑(1-Phenyl‑1H‑1,2,3-triazol-4-yl)phenol Derivatives as Potent Steroid Sulfatase Inhibitors for Efficient Treatment of Breast Cancer
PublikacjaWe present here the advances achieved in the development of new sulfamoylated 4-(1-phenyl-1H-1,2,3-triazol-4-yl)phenol derivatives as potent steroid sulfatase (STS) inhibitors for the treatment of breast cancer. Prompted by promising biological results and in silico analysis, the initial series of similar compounds were extended, appending a variety of m-substituents at the outer phenyl ring. The inhibition profiles of the newly...
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Diclofenac Degradation—Enzymes, Genetic Background and Cellular Alterations Triggered in Diclofenac-Metabolizing Strain Pseudomonas moorei KB4
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Electrochemistry meets enzymes: Investigation of the biotransformation pathway of C-1311 based on electrochemical simulation in comparison to in vitro methods.
PublikacjaThe knowledge of the metabolic pathways and the biotransformation of new drugs is one of the major challenges in pharmaceutical research. It is crucial for elucidation of degradation routes of the new biologically active compounds, especially in the area of possible toxicity. Conventional in vitro drug metabolism studies are based on incubating drug candidate with e.g. hepatocytes or, most importantly, liver cell microsomes and...
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The inhibition effect of mad Honey on corrosion of 2007-type aluminium alloy in 3.5% NaCl solution
PublikacjaThe inhibition effect of mad honey on corrosion of 2007-type aluminium alloy in 3.5% NaCl solution was investigated by Tafel extrapolarisation (TP), electrochemical impedance spectroscopy (EIS) and dynamic electrochemical impedance spectroscopy (DEIS). All the studied parameters exhibited good anti-corrosive properties against corrosion of 2007-type aluminium alloy in the test solution; the corrosion rates decreased with the increase...
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THE GENE CLONING, OVEREXPRESSION, PURIFICATION AND BIOCHEMICAL CHARACTERISATION OF A NEW COLD-ADAPTED β–GALACTOSIDASE FROM ARTHROBACTER SP. VII-4
PublikacjaINTRODUCTION. β-Galactosidase [EC 3.2.1.23] is an enzyme that catalyzes the hydrolysis of O-glycosidic linkages in galactosides. It is commercially used in dairy industry for the production of milk with reduced lactose content. Potentially, the best method for lactose removal under cooling conditions should be carried out with a cold-adapted enzyme. AIM. The aim of this study was to determine the taxonomic affiliation of the isolate...