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Search results for: proteinase inhibitors
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Structure-activity relationship study of a small cyclic peptide H-c[Lys-Pro-Glu]-Arg-OH: a potent inhibitor of Vascular Endothelial Growth Factor interaction with Neuropilin-1
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Andrzej Miszczyk dr hab. inż.
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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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Projektowanie, synteza oraz badanie aktywności biologicznej amidosiarczanowych inhibitorów sulfatazy steroidowej zawierających w swojej konstytucji ugrupowania fosforowe lub wiązania C-F
PublicationWedług Światowej Organizacji Zdrowia (WHO) estrogeny są jednymi z głównych czynników stymulujących wzrost nowotworów hormonozależnych. Dlatego też, projektowanie oraz synteza nowych, skuteczniejszych środków wpływających na biosyntezę estrogenów stanowi ogromne wyzwanie dla współczesnej medycyny. W ostatnich latach liczne ośrodki naukowe na całym świecie prowadzą intensywne badania związane z poszukiwaniem nowych, skutecznych inhibitorów...
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Determination of the MIC (minimum inhibitory concentration) of new bisacridines IKE16-19, IKE21 and IE10 against C. glabrata clinical strains
Open Research DataThe datasets contain the results of determining the MIC value (minimum inhibitory concentration) of new bisacridines IKE16-19, IKE21 and IE10 against Candida glabrata clinical strains CZD 310, 373, 377, 513 and collection strain DSM 11226 by the modified M27-A3 specified by the CLSI.
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The Early Stages of Photosystem II Assembly Monitored by Measurements of Fluorescence Lifetime, Fluorescence Induction and Isoelectric Focusing of Chlorophyll-Proteins in Barley Etiochloroplasts
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Diverse Expression of Selected SMN Complex Proteins in Humans with Sporadic Amyotrophic Lateral Sclerosis and in a Transgenic Rat Model of Familial Form of the Disease
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Heat shock proteins (HSP 90, 70, 60, and 27) in Galleria mellonella (Lepidoptera) hemolymph are affected by infection with Conidiobolus coronatus (Entomophthorales)
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Formation of Secondary and Supersecondary Structure of Proteins as a Result of Coupling Between Local and Backbone-Electrostatic Interactions: A View Through Cluster-Cumulant Scope
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Comparative Proteomic Profiling of Ectosomes Derived from Thyroid Carcinoma and Normal Thyroid Cells Uncovers Multiple Proteins with Functional Implications in Cancer
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The effect of high pressure at subzero temperature on proteins solubility, drip loss and texture of fish (cod and salmon) and mammal’s (pork and beef) meat
PublicationOne of the possibilities of using high pressure technique in inactivation of microorganism is conducting this process at subzero temperature. However, for its practical application in meat preservation the appropriate properties of meat should be kept. Therefore, the aim of this work was to examine the effect of pressure at subzero temperature (without freezing of water) on proteins and texture of mammal’s and cold-adapted fish...
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Charakterystyka elektrochemiczna odporności korozyjnej aluminium i jego stopów w wodnych środowiskach zasadowych
PublicationRozprawa doktorska przedstawia charakterystykę elektrochemiczną odporności korozyjnej aluminium i jego stopów w wodnych środowiskach zasadowych. Główne elementy pracy to część literaturowa, w której zarysowano problem badawczy i szczegółowo omówiono zagadnienia związane z korozją aluminium oraz, po przedstawieniu tez pracy i jej zakresu, część eksperymentalna i badawcza. Praca skupia się na kompleksowemu opisowi mechanizmów korozji...
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Genetic and Epigenetic Aspects of Atopic Dermatitis
PublicationAtopic dermatitis is a heterogeneous disease, in which the pathogenesis is associated with mutations in genes encoding epidermal structural proteins, barrier enzymes, and their inhibitors; the role of genes regulating innate and adaptive immune responses and environmental factors inducing the disease is also noted. Recent studies point to the key role of epigenetic changes in the development of the disease. Epigenetic modifications...
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Transport deficiency is the molecular basis of Candida albicans resistance to antifungal oligopeptides
Publication(FMDP), an inhibitor of glucosamine-6-phosphate synthase, exhibited growth inhibitory activity against Candida albicans, with minimal inhibitory concentration values in the 0.05–50 mg/L range. Uptake by the peptide permeases was found to be the main factor limiting an anticandidal activity of these compounds. Di- and tripeptide containing FMDP (F2 and F3) were transported by Ptr2p/Ptr22p peptide transporters (PTR) and FMDP-containing...
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Novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(1,3,5-triazin-2-ylamino)guanidine derivatives: Inhibition of human carbonic anhydrase cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII, anticancer activity, and molecular modeling studies
PublicationA series of novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(6-substituted-4-chloro-1,3,5-triazin-2-ylamino)guanidine derivatives 9–20 have been synthesized by substitution of chlorine atom at the 1,3,5-triazine ring in compounds 5–8 with 3- or 4-aminobenzenesulfonamide and 4-(aminomethyl)benzenesulfonamide hydrochloride. All the synthesized compounds were evaluated for their inhibitory activity toward hCA I, II,...
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Synthetic strategies in construction of organic macromolecular carrier–drug conjugates
PublicationMany metabolic inhibitors, considered potential antimicrobial or anticancer drug candidates, exhibit verylimited ability to cross the biological membranes of target cells. The restricted cellular penetration ofthose molecules is often due to their highhydrophilicity. One of the possible solutions to this problem is aconjugation of an inhibitor with a molecular organic nanocarrier. The conjugate thus formed should beable to penetrate...
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A Specific CD44lo CD25lo Subpopulation of Regulatory T Cells Inhibits Anti-Leukemic Immune Response and Promotes the Progression in a Mouse Model of Chronic Lymphocytic Leukemia
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Western blot analysis of autophagy-related proteins of A549, H226 and H460 cells after exposure to C4
Open Research DataThe dataset includes measurements of the density of autophagy-related proteins in A549, H226, and H460 cell lines following exposure to compound C4.
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Novel Highly Thermostable Endolysin from Thermus scotoductus MAT2119 Bacteriophage Ph2119 with Amino Acid Sequence Similarity to Eukaryotic Peptidoglycan Recognition Proteins
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A prototypical non-malignant epithelial model to study genome dynamics and concurrently monitor micro-RNAs and proteins in situ during oncogene-induced senescence
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Extension of the force-matching method to coarse-grained models with axially symmetric sites to produce transferable force fields: Application to the UNRES model of proteins
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Proteomic analysis of stipe explants reveals differentially expressed proteins involved in early direct somatic embryogenesis of the tree fern Cyathea delgadii Sternb
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Human Induced Pluripotent Stem Cell-Derived Microvesicles Transmit RNAs and Proteins to Recipient Mature Heart Cells Modulating Cell Fate and Behavior
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Dietary chicory root and chicory inulin trigger changes in energetic metabolism, stress prevention and cytoskeletal proteins in the liver of growing pigs – a proteomic study
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A vector-enzymatic DNA fragment amplification-expression technology for construction of artificial, concatemeric DNA, RNA and proteins for novel biomaterials, biomedical and industrial applications
PublicationA DNA fragment amplification/expression technology for the production of new generation biomaterials for scientific, industrial and biomedical applications is described. The technology enables the formation of artificial Open Reading Frames (ORFs) encoding concatemeric RNAs and proteins. It recruits the Type IIS SapI restriction endonuclease (REase) for an assembling of DNA fragments in an ordered head-to-tail-orientation. The...
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A new Toxoplasma gondii chimeric antigen containing fragments of SAG2, GRA1, and ROP1 proteins—impact of immunodominant sequences size on its diagnostic usefulness
PublicationThis study presents the first evaluation of new Toxoplasma gondii recombinant chimeric antigens containing three immunodominant regions of SAG2, GRA1, and one of two ROP1 fragments differing in length for the serodiagnosis of human toxoplasmosis. The recombinant chimeric antigens SAG2-GRA1-ROP1L (with large fragment of ROP1, 85-396 amino acid residues) and SAG2-GRA1-ROP1S (with a small fragment of ROP1, 85-250 amino acid residues)...
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Mateusz Brodowski
PeopleMateusz Brodowski received his engineer degree in 2019 at the of Chemical Technology with a specialization in Anti-Corrosion Protection Technologies, in his engineer thesis he examined the effectiveness of green corrosion inhibitors. He finished a Master's degree in the field of Mechatronics, realizing the work of creating software for data acquisition from the electrochemical measurement system. Since 2019, he has been working...
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Projektowanie, synteza fosforowych i tiofosforowych pochodnych kumaryny, bifenylu, tyraminy oraz flawonoidów i badanie ich aktywności biologicznej jako potencjalnych inhibitorów sulfatazy steroidowej (STS)
PublicationChoroby nowotworowe są jednym z najpoważniejszych problemów z jakimi zmaga się współczesne społeczeństwo. Rak piersi jest jedną z głównych przyczyn zgonów wśród kobiet w krajach rozwiniętych, dlatego też niezbędne jest opracowanie nowych, skutecznych metod leczenia. Podstawowym problemem w selektywnym zwalczaniu komórek nowotworowych jest ich wysokie podobieństwo do komórek prawidłowych. W związku z dowodami na znaczący udział...
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Increased susceptibility of PARP-1 KO cells to antitumor triazoloacridone C-1305 is associated with permanent G2 cell cycle arrest.
PublicationTriazoloakrydon C-1305 jest nowym inhibitorem topoizomerazy II wykazującym wysoką aktywność przeciwnowotworową. W tej pracy badaliśmy działanie cytotoksyczne pochodnej C-1305 i jej analogu strukturalnego C-1533 wobec komórek fibroblastów mysich i dwóch mutantów, w których uszkodzono gen PARP-1. Jak wykazaliśmy, komórki z uszkodzonym genem PARP-1 są nadwrażliwe na działanie związku C-1305 w porównaniu z komórkami PARP-1 +/+ podczas...
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Molecular docking studies towards development of novel Gly-Phe analogs for potential inhibition of Cathepsin C (dipeptidyl peptidase I).
PublicationCathepsin C is a cysteine protease required for activation of various pro-inflammatory serine proteases and, essentially, is of interest as a therapeutic target. Cathepsin C coordinate system was employed as a model to study the interaction of some already available inhibitors of Cathepsin C. Compounds containing Gly-Phe fragment with functional groups at its ends were designed by knowledge based approach. Using AutoDock and...
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Radiation-induced Changes in Levels of Selected Proteins in Peripheral Blood Serum of Breast Cancer Patients as a Potential Triage Biodosimeter for Large-scale Radiological Emergencies
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Genes encoding proteins regulating fatty acid metabolism and cellular response to lipids are differentially expressed in porcine luminal epithelium during long-term culture
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Correction to: A prototypical non-malignant epithelial model to study genome dynamics and concurrently monitor micro-RNAs and proteins in situ during oncogene-induced senescence
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Systemy ekspresyjne białek cytochromu P450 w badaniach in vitro metabolizmu leków = Expression systems of cytochrome P450 proteins in studies of drug metabolism in vitro
PublicationBiałka cytochromu P450 to najważniejsze enzymy biorące udział w metabolizmie większości stosowanych w klinice leków, odpowiedzialne za ich aktywację lub detoksykację. Niektóre z dróg metabolizmu leku mogą być jednak odpowiedzialne za jego podwyższoną toksyczność. Nowe systemy ekspresyjne białek cytochromu P450 w komórkach ssaków, w tym człowieka, projektowane są w celu poznania roli metabolizmu w mechanizmie działania potencjalnych,...
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Western blot analysis of DDR- and apoptosis-related proteins of A549 and H460 cells after exposure to TXT2 and TXT4
Open Research DataThe data set contains full-length blot images of DDR- and apoptosis-related proteins of A549 and H460 cells after exposure to TXT2 and TXT4.
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Inhibitor kinazy Brutona u chorych z nawrotowym lub opornym na leczenie chłoniakiem z komórek płaszcza – wyniki międzynarodowego, wieloośrodkowego, badania II fazy z ibrutynibem (PCI-32765) – EHA Encore
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Synthesis of 11,12-dihydro benzo[c]phenanthridines via a Pd-catalyzed unusual construction of isocoumarin ring/FeCl3-mediated intramolecular arene-allyl cyclization: First identification of a benzo[c]phenanthridine based PDE4 inhibitor
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Hybrid analogues of SFTI-1 modified in P1 position by β- and γ-amino acids and N-substituted β-alanines
PublicationA series of compounds containing either non-proteinogenic beta-/gamma-amino acids or N-substituted beta-alanine residues (beta-peptoid units) in P-1 specificity position were synthesized based on the structure of sunflower trypsin inhibitor 1 (SFTI-1). The compounds were synthesized on a solid support; the N-substituted beta-alanines (beta Nhlys and beta Nhphe) were introduced into a peptidomimetic chain via a two-step approach...
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Interaction of the conserved region 4.2 of sigma(E) with the RseA anti-sigma factor
PublicationEo-E RNA polymerase transcribes a regulon of folding factors for the bacterial envelope and is induced by physical and chemical stresses. The RseA anti-sigma factor inhibits the activity of Esigma(E) RNA, polymerase. It is shown here that the N-terminal portion of sigma(E), residues 1-153, binds core RNA polymerase. RseA interacts with residues 154-191 of sigma(E), a site that is homologous to region 4, the sigma factor binding...
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α-Lipoic Acid Strengthens the Antioxidant Barrier and Reduces Oxidative, Nitrosative, and Glycative Damage, as well as Inhibits Inflammation and Apoptosis in the Hypothalamus but Not in the Cerebral Cortex of Insulin-Resistant Rats
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Molecular basis and quantitative assessment of TRF1 and TRF2 protein interactions with TIN2 and Apollo peptides
PublicationShelterin is a six-protein complex (TRF1, TRF2, POT1, RAP1, TIN2, and TPP1) that also functions in smaller subsets in regulation and protection of human telomeres. Two closely related proteins, TRF1 and TRF2, make high-affinity contact directly with double-stranded telomeric DNA and serve as a molecular platform. Protein TIN2 binds to TRF1 and TRF2 dimer-forming domains, whereas Apollo makes interaction only with TRF2. To elucidate...
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Antibody reactivity in patients with IgE-mediated wheat allergy to various subunits and fractions of gluten and non-gluten proteins from ω-gliadin-free wheat genotypes
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Partial characterization of white cabbages (Brassica oleracea var. capitata f. alba) from different regions by glucosinolates, bioactive compounds, total antioxidant activities and proteins
PublicationW pracy przedstawiono wyniki oznaczeń glukozynolanów (GLS), aktywności przeciwutleniającej (TRSA) oraz białek w próbkach białej kapusty pochodzącej z różnych rejonów geograficznych Europy. Glukobrassycyna i sinigryna były dominującymi GLS we wszystkich próbkach kapusty. Całkowita zawartość GLS mieściła się w zakresie od 3,3-7,7 µmol/g sm. Aktywność przeciwulteniająca próbek kapusty została oszacowana za pomocą testów ABTS,...
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Determination of the minimum inhibitory concentration of C-1311 derivatives (C-1296, C-1410, Compound 1, Compound 1-R8) against Candida strains
Open Research DataThe datasets contain the results of determining the minimum inhibitory concentration of imidazoacridinone derivatives against C. albicans ATCC 10231, C. glabrata ATCC 90030, C. krusei ATCC 6258 and C. parapsilosis ATCC 22019 and C. albicans clinical strains by the modified M27-A3 specified by the CLSI.
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Corrosion Inhibition Mechanism and Efficiency Differentiation of Dihydroxybenzene Isomers Towards Aluminum Alloy 5754 in Alkaline Media
PublicationThe selection of efficient corrosion inhibitors requires detailed knowledge regarding the interaction mechanism, which depends on the type and amount of functional groups within the inhibitor molecule. The position of functional groups between different isomers is often overlooked, but is no less important, since factors like steric hinderance may significantly affect the adsorption mechanism. In this study, we have presented how...
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Peptide dendrimers as antifungal agents and carriers for potential antifungal agent—N3‐(4‐methoxyfumaroyl)‐(S)‐2,3‐ diaminopropanoic acid—synthesis and antimicrobial activity
PublicationA series of peptide dendrimers and their conjugates with antimicrobial agent FMDP (N3‐(4‐methoxyfumaroyl)‐(S)‐2,3‐diamino‐propanoic acid) were synthesized. The obtained compounds were tested for the antibacterial and antifungal activity. All novel dendrimers displayed much better activity against the tested strains than FMDP itself. Moreover, their conjugates with FMDP also exhibited antimicrobial activity. The most promising molecules...
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Selected symmetrically substituted carbazoles: Investigation of anticancer activity and mechanisms of action at the cellular and molecular levels
PublicationDNA topoisomerases play a critical role as essential enzymes in controlling alterations in the topology of DNA. They achieve this by orchestrating the coordinated process of breaking and rejoining DNA strands, which is crucial for maintaining the proper structure of DNA during regular cellular development. The search for and development of new potential anticancer drugs is a challenging yet immensely important area of research...
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Potential diagnostic utility of recombinant Toxoplasma gondii proteins for detecting anti-Toxoplasma gondii IgG antibodies in horses serum samples
Open Research DataToxoplasmosis is caused by an intracellular protozoan, Toxoplasma gondii, and is a parasitic disease that occurs in all warm-blooded animals, including humans. Toxoplasmosis is one of the most common parasitic diseases of animals and results in reproductive losses. Diagnosis of toxoplasmosis is currently based on serological assays using native antigens...
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Potential diagnostic utility of recombinant Toxoplasma gondii proteins for detecting anti-Toxoplasma gondii IgG antibodies in goat serum samples
Open Research DataToxoplasmosis is caused by an intracellular protozoan, Toxoplasma gondii, and is a parasitic disease that occurs in all warm-blooded animals, including humans. Toxoplasmosis is one of the most common parasitic diseases of animals and results in reproductive losses. Diagnosis of toxoplasmosis is currently based on serological assays using native antigens...
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Potential diagnostic utility of recombinant Toxoplasma gondii proteins for detecting anti-Toxoplasma gondii IgG antibodies in feline serum samples
Open Research DataToxoplasmosis is caused by an intracellular protozoan, Toxoplasma gondii, and is a parasitic disease that occurs in all warm-blooded animals, including humans. Toxoplasmosis is one of the most common parasitic diseases of animals and results in reproductive losses. Diagnosis of toxoplasmosis is currently based on serological assays using native antigens...