Search results for: CYP3A4 INHIBITION
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Surface plasmon resonance imaging biosensor for cathepsin G based on a potent inhibitor: Development and applications
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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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Prenylated Stilbenoids Affect Inflammation by Inhibiting the NF-κB/AP-1 Signaling Pathway and Cyclooxygenases and Lipoxygenase
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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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Photoprotection and Antiaging Activity of Extracts from Honeybush (Cyclopia sp.)—In Vitro Wound Healing and Inhibition of the Skin Extracellular Matrix Enzymes: Tyrosinase, Collagenase, Elastase and Hyaluronidase
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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
PublicationThe 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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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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Design of serine proteinase inhibitors by combinatorial chemistry using trypsin inhibitor SFTI‐1 as a starting structure
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Effectiveness of various solvent-produced thyme (Thymus vulgaris) extracts in inhibiting the growth of Listeria monocytogenes in frozen vegetables
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Dynamic impedance data for various carboxylic acids corrosion inhibition of aluminium in alkaline media (pH=11)
Open Research DataThis dataset contains the results of Dynamic Electrochemical Impedance Spectroscopy (DEIS) carried out in galvanostatic mode under iDC=0, carried out in order to define the corrosion inhibition effect of various studied carboxylic acids: citric acid, malic acid, maleic acid, succinic acid, tartaric acid, carballylic acid, and serine. The experiment...
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Increased cytotoxicity of an unusual DNA topoisomerase II inhibitor compound C-1305 toward HeLa cells with downregulated PARP-1 activity results from re-activation of the p53 pathway and modulation of mitotic checkpoints
PublicationOur previous studies have shown that murine fibroblast cells, in which PARP-1 gene was inactivated by gene disruption, are extremely sensitive to triazoloacridone compound C-1305, an inhibitor of DNA topoisomerase II with unusual properties. Here, we show that pharmacological inhibition of PARP-1 activity by its inhibitor compound NU1025, sensitizes human cervical carcinoma HeLa cells to compound C-1305 compared to treatment with...
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Evaluation of the Role of the Pharmacological Inhibition of Staphylococcus aureus Multidrug Resistance Pumps and the Variable Levels of the Uptake of the Sensitizer in the Strain-Dependent Response of Staphylococcus aureus to PPArg2-Based Photodynamic Ina
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Differential Response of MDA-MB-231 and MCF-7 Breast Cancer Cells to In Vitro Inhibition with CTLA-4 and PD-1 through Cancer-Immune Cells Modified Interactions
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Liver antioxidant defense after FAAH inhibitor - URB-597 administration to DOCA-salt-induced hypertension in rats
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Crosstalk between liver antioxidant and the endocannabinoid systems after chronic administration of the FAAH inhibitor, URB597, to hypertensive rats
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The cross talk between redox and endocannabinoids systems in the kidney of hypertensive rats after inhibitor FAAH - URB597 administration
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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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Structural and Evolutionary Analysis Indicate That the SARS-CoV-2 Mpro Is a Challenging Target for Small-Molecule Inhibitor Design
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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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Increased time varying heart rate and cardiovascular risk in hypertension – Benefit of selective I(f)channel 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
PublicationIn 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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Truncation of Huia versabilis Bowman-Birk inhibitor increases its selectivity, matriptase-1 inhibitory activity and proteolytic stability
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Introduction of Pro and Its Analogues in the Conserved P1 Position of Trypsin Inhibitor SFTI-1 Retains Its Inhibitory Activity
PublicationA 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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Antitumor triazoloacridinone C-1305 as a potent FLT3 tyrosine kinase inhibitor in human acute myeloid leukemia (AML) cells.
PublicationJednym 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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Structure-based design and in vivo anti-arthritic activity evaluation of a potent dipeptidyl cyclopropyl nitrile inhibitor of cathepsin C
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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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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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Antitumor DNA-Damaging C-1748 is a New Inhibitor of Autophagy that Triggers Apoptosis in Human Pancreatic Cancer Cell Lines
PublicationDespite 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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Removal of phenolic inhibitor compounds from hydrolysates and post-fermentation broths by using a Hydrophobic Magnetic Deep Eutectic Solvent
PublicationHydroxymethylfurfural (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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Modulation of mRNA and protein levels of CYP1A1, 1A2, and 1B1 in nontumorigenic breast epithelial cells (MCF10A) by cabbage juice and its active components
PublicationZbadano wpływ soków z kapusty oraz występujących w nich pochodnych indolowych i sulforafanu na poziom ekspresji enzymów odpowiedzialnych za metabolizm ksenobiotyków w tym estrogenów. Wykazano, że soki z kapusty i izolowane substancje mają podobny wpływ na poziom mRNA i białek enzymatycznych.
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X-ray Photoelectron Spectroscopy studies of various carboxylic acids adsorption on aluminium alloys in alkaline media
Open Research DataThis 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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Flavin monooxygenases, FMO1 and FMO3, not cytochrome p450 isoenzymes, contribute to metabolism of anti-tumour triazoloacridinone, C-1305, in liver microsomes and HepG2 cells.
PublicationCelem pracy było określenie roli wybranych enzymów frakcji mikrosomalnej komórek wątroby w metabolizmie pochodnej triazoloakrydonu, związku C-1305. Wykazano, że badana pochodna ulega transformacji wobec frakcji enzymów izolowanych z hepatocytów szczurzych i ludzkich oraz jest metabolizowana przez komórki linii HepG2. Badania wykazały ponadto, że enzymami odpowiedzialnymi za obserwowane przemiany były monooksygenazy flawinowe, FMO1...
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Rola polimorfizmu i zróżnicowanej ekspresji genów cytochromu P450 w metabolizmie ksenobiotyków.
PublicationZdolność do metabolizmu ksenobiotyków przez cytochromy P450 (CYP) określona jest przez polimorfizm i poziom ekspresji genów tych białek. Najwięcej, 40 odmian polimorficznych o zróżnicowanej aktywności enzymatycznej, poznano dla CYP2D6, natomiast tylko dwie w przypadku CYP2C9, których obecność powoduje zahamowanie metabolizmu wielu leków. Z kolei polimorfizm genu CYP3A4 nie miał istotnego wpływu na aktywność metaboliczną jego produktu...
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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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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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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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Induction of unique structural changes in guanine-rich DNA regions by the triazoloacridone C-1305, a topoisomerase II inhibitor with antitumor activities.
PublicationCelem 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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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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Analogues of trypsin inhibitor SFTI-1 modified in the conserved P1′ position by synthetic or non-proteinogenic amino acids retain their inhibitory activity
PublicationA 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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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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Drug-drug interaction potential of antitumor acridine agent C-1748: The substrate of UDP-glucuronosyltransferases 2B7, 2B17 and the inhibitor of 1A9 and 2B7
PublicationBackground 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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Inhibiting activity of HIV-1: protease, reverse transcriptase and integrase all together by novel compounds using computational approaches (flexible and rigid docking)
PublicationAcquired 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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Imidazoacridinone antitumor agent, c-1311, as a selective mechanism-based inactivator of human recombinant cytochrome P450 1A2
PublicationPrzedmiotem badań była przeciwnowotworowa pochodna imidazoakrydonu, C-1311, która pod nazwą Symadex R, znajduje się aktualnie w II fazie badań klinicznych. Wcześniejsze wyniki pozwoliły stwierdzić, że związek ten jest selektywnym inhibitorem niektórych enzymów cytochromowych. Podjęto zatem próbę wyjaśnienia mechanizmu inhibicji izoenzymów cytochromu P450 przez C-1311. Wykazano, że utrata aktywności katalitycznej obu izoenzymów...