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Wyniki wyszukiwania dla: inhibitory enzymu
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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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[Chapter] 2. Thermostable enzymes in food processing
PublikacjaW rozdziale przedstawiono charakterystykę termostabilnych hydrolaz glikozydów, izomeraz, transferaz,lipaz i enzymów proteolitycznych w przetwórstwie rozmaitych surowców źywnościowych. Podano przyczyny termostabilności tych enzymów oraz wymieniono korzyści wynikające z ich stosowania.
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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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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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Glucosamine-6-phosphate synthase - the multi-facets enzyme
PublikacjaAmidotransferaza L-glutamina: D-frukozo-6-fosforan, nazywana zwyczajowo syntazą glukozamino-6-fosforanu, jako jedyny enzym należący do grupy amidotransferaz, nie wykazuje aktywności amoniakozależnej. Enzym ten, katalizujący pierwszy wyjątkowy etap w szlaku metabolicznym prowadzącym do ostatecznego wytworzenia 5´difosfourydyno-N-acetylo-D-glukozaminy (UDG-GlcNAc) stanowi ważny punkt kontroli metabolicznej biosyntezy makromolekuł...
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Enzyme-conjugated MXene nanocomposites for biosensing and biocatalysis acuities
PublikacjaEngineered two-dimensional (2-D) MXenes-based materials with tunable characteristics and multi-functionalities have brought up new paradigms in the biosensing and catalysis of chemical compounds. The profusion of electroactive functional moieties on the surface of few/multi-layer MXenes facilitates their ability to retain biomolecules such as enzymes resulting in unique dimensions for bioanalytical and biosensing applications....
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Substrate specificity and inhibitory study of human airway trypsin-like protease
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Pochodne fosforylowanych cukrów jako inhibitory syntazy glcn-6-p
PublikacjaW artykule został opisany mechanizm działania syntazy glukozamino-6-fosforanu i syntezy wybranych analogów blokujących domenę wiążących D-fruktozo-6-fosforanu, którym jest cis-enolamina.
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Synthesis and Cholinesterase Inhibitory Activity of N-Phosphorylated /N-Tiophosphorylated Tacrine
PublikacjaNovel phosphorus and thiophosphorus tacrine derivatives were designed, synthesized and their biological activity and molecular modeling was investigated as a new potential anti-Alzheimer's disease (AD) agents. All new synthesized compound exhibited lower toxicity against neuroblastoma cell line (SH-SY5Y) in comparison with tacrine. Two analogues in the series, 7 and 9, demonstrated lack of cytotoxicity against hepatocellular cells...
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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
PublikacjaThe 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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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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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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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
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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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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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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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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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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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Novel Inhibitor-Based Therapies for Thyroid Cancer—An Update
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Influence of dipalmitoylphosphatidylcholine (or dioleoylphosphatidylcholine) and phospholipase A2 enzyme on the properties of emulsions
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Computer-assisted enzyme engineering by modification of tunnels, channels and gates
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Synthesis and antimicrobial and nitric oxide synthase inhibitory activities of novel isothiourea derivatives
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Synthesis and steroid sulfatase inhibitory activities of N-alkanoyl tyramine phosphates and thiophosphates
PublikacjaA series of phosphate and thiophosphate analogs based on the frameworks of N-alkanoyl tyramines have been synthesized and biologically evaluated. Their binding modes have been modeled using docking techniques. The inhibitory effects of the synthesized compounds were tested on STS isolated from the human placenta as well as the MCF-7, MDA-MB-231 and SkBr3 cancer cell lines. Most of the new STS inhibitors possessed potent activity...
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KONSTRUKCJA AUKSOTROFICZNEGO WZGLĘDEM L-LIZYNY SZCZEPU CANDIDA ALBICANS
PublikacjaEnzymy szlaku kwasu L-α-aminoadypinowego biosyntezy L-lizyny z Candida albicans są potencjalnymi celami molekularnymi w terapii przeciwgrzybowej. Niektóre grupy badawcze wykazały, że auksotrofia wobec L-lizyny u pewnych gatunków grzybów powoduje zmniejszenie ich zjadliwości i może mieć wpływ na wzrost in vivo [Liebmann i in. 2004]. Oznacza to, że można się spodziewać zahamowania wzrostu komórek grzybowych w wyniku działania selektywnych...
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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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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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Phosphate tricyclic coumarin analogs as steroid sulfatase inhibitors: synthesis and biological activity.
PublikacjaIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate tricyclic coumarin derivatives as potential steroid sulfatase inhibitors. The described synthesis includes the straightforward preparation 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 modified...
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Synthesis and steroid sulfatase inhibitory activities of N-phosphorylated 3-(4-aminophenyl)-coumarin-7-O-sulfamates
PublikacjaIn the present work, we report convenient methods for the synthesis and biological evaluation of N-phosphorylated derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as potential steroid sulfatase (STS) inhibitors. Their binding modes were modeled using docking techniques. The inhibitory effects of the synthesized compounds were tested on STS isolated from human placenta. All of the newly synthesised coumarin derivatives were...
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Soil enzymes in a changing climate
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Synthesis of phosphono and phosphate derivatives of hydroxyimino-D-alditols as new potential antifungal agents
PublikacjaIn search for new effective we antyfungals we focus on two enzymes involved in biosynthesis of the fungal cell wall. The first enzyme is glucosamine-6-phosphate (GlmS), which catalyzes transformation of D-fructose-6-phosphate (Fru-6P) to D-glucosamine-6-phodphate (GlcN-6P) in the chitin biosynthesis pathway. The second enzyme is phosphomannose isomerase (PMI) repored to play a crucial role in biosynthesis of many mannosylated structures,...
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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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Synthesis and biological evaluation of thiophosphate tricyclic coumarin derivatives as steroid sulfatase inhibitors
PublikacjaSteroid sulfatase (STS) enzyme inhibition is an important approach to the management of hormone-dependent breast cancer. In this paper, we report convenient methods for the synthesis and biological evaluation of thiophosphate tricyclic coumarin analogs exhibiting STS activity. The described methods are based on the straightforward preparation of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-2-one, 3-hydroxy- 7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one,...
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Structural analogues of reactive intermediates as inhibitors of glucosamine-6-phosphate synthase and phosphoglucose isomerase
PublikacjaCentra aktywne izomerazy fosfoglukozowej (PGI) oraz domeny izomerazowej (HPI) syntazy glukozamino-6-fosforanu (GlcN-6-P), wykazują podobieństwo ułożenia przestrzennego kluczowych reszt aminokwasowych, z wyjątkiem reszty Arg272 PGI i reszt Lys603 i Lys485 HPI. Dziesięć pochodnych D-heksitolo-6-P, kwasu 5-fosfoarabonowego i kwasu 6-fosfoglukonowego, strukturalnych analogów cis-enolaminy lub cis-enolanu, przypuszczalnych stanów przejściowych...
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Inactivation of glucosamine-6-phosphate synthase by N3-oxoacyl derivatives of L-2,3-diaminopropanoic acid
PublikacjaN3-oksoacylowe pochodne kwasu l-2,3-diaminopropanowego zawierające ugrupowanie epoksydowe lub układ sprzężonych wiązań podwójnych inaktywują syntaze glukozamino-6-fosforanu (GlcN-6-P) z S. cerevisiae. Wyniki badań kinetycznych inaktywacji enzymu wskazują na dwuetapowy przebieg tej reakcji, przy czym tworzenie kompleksu enzym:ligand poprzedza nieodwracalną modyfikację enzymu. Badane związki różniły się powinowactwem do centrum aktywnego...
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Variability of Hordeum vulgare L. Cultivars in Yield, Antioxidant Potential, and Cholinesterase Inhibitory Activity
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The wetting and interfacial properties of alumina surface treated with dipalmitoylphosphatidylcholine and lipase enzyme
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Modelling of Thyroid Peroxidase Reveals Insights into Its Enzyme Function and Autoantigenicity
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Enzyme Conjugation - A Promising Tool for Bio-catalytic and Biotransformation Applications – A Review
PublikacjaEnzymes have revolutionized conventional industrial catalysts as more efficient, eco-friendly, and sustainable substitutes that can be used in different biotechnological processes, food, and pharmaceutical industries. Yet, the enzymes from nature are engineered to make them adapt and enhance their durability in the industrial environment. One promising approach involves the combined use of multiple enzymes that catalyze highly...
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Quinone- and nitroreductase reactions of Thermotoga maritima peroxiredoxin–nitroreductase hybrid enzyme
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Novel steroid sulfatase inhibitors based on N ‐thiophosphorylated 3‐(4‐aminophenyl)‐coumarin‐7‐O‐sulfamates
PublikacjaIn 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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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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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,...