Wyniki wyszukiwania dla: PEPTIDE CONJUGATES
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Conformational studies of highly potent 1-aminocyclohexane-1-carboxylic acid substituted V2 vasopressin agonists
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Effect of head-to-tail cyclization on conformation of histatin-5
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Conformational studies of vasopressin and mesotocin using NMR spectroscopy and molecular modelling methods. Part I: studies in water
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Lipopeptides - synthesis and their properties
PublikacjaZaprezentowano syntezę nowych pochodnych tripeptydu Gly-Hyp-Lys o potencjalnie lepszych właściwościach lipofilowych. Modyfikacje polegały na acylowaniu N-końca glicyny kwasami tłuszczowymi (np. palmitynowym i stearynowym). Syntezę lipopeptydów zawierających fragment Gly-X-Y (gdzie: X= Met,Hyp,Hyp-Met,Gly-Hyp; Y=Lys,D-Lys) przeprowadzono na fazie stałej z zastosowaniem procedury Fmoc. Do wydłużanie łańcucha peptydowego zastosowano...
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Novel analogues of bradykinin conformationally restricted in the C-terminal part of the molecule
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Analogues of Trypsin Inhibitor SFTI-1 with Disulfide Bridge Substituted by Various Length of Carbonyl Bridges
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Synthesis of analogues of anthraquinones linked to tuftsin or retro-tuftsin residues as potential topoisomerase inhibitors
PublikacjaZsyntetyzowano 10 nowych analogów antrachinonów z pochodnymi tuftsyny i retro-tuftsyny jako potencjalne inhibitory topoizomerazy. Substratem wyjściowym były zsyntetyzowane 1,4-, 1,5- i 1,8-bis(tosyloksy)-9,10-antrachinony oraz odpowiednio chronione pochodne tuftsyny i retro-tuftsyny, które otrzymano metodą mieszanych bezwodników z zastosowaniem chloromrówczanu izobutylu i NMM. Reakcje prowadzone były w acetonitrylu pod azotem w...
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The immunological properties, cytotoxic effect and antimicrobial activities of novel analogues of edeine antibiotics
PublikacjaOpisano syntezę kilku nowych analogów edein a i d z zastosowaniem klasycznych metod syntezy peptydów w roztworze oraz przedstawiono wyniki badań cytotoksycznych na kilku liniach komórek ludzkich oraz wyniki badań mikrobiologicznych w stosunku do bakterii gramododatnich i gramoujemnych. Opisano również wyniki badań immunologicznych na modelu myszy.
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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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Oligopeptide antifungals are exceptionally active against multidrug-resistant yeast
PublikacjaPermeazy peptydowe w komórkach drożdżowych są zdolne do transportu do wnętrza komórek oligopeptydów, zawierających w swojej strukturze niebiałkowe aminokwasy o właściwościach przeciwgrzybowych. Wśród szerokiego wachlarza tego rodzaju związków przebadanych pod względem aktywności biologicznej na wielolekoopornych komórkach drożdżowych, zaobserwowano liczna grupę, wykazującą zwiększoną aktywność względem komórek eksprymujących transportery...
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Structure-activity relationship studies on the antimicrobial activity of novel edeine a and d analogues
PublikacjaOpisano syntezę 4 nowych analogów peptydowego antybiotyku, edeiny a i d z wykorzystaniem klasycznej syntezy w roztworze. Stosowano metodę estrów aktywnych oraz metodę azydową do tworzenia wiązań peptydowych. Zbadano także aktywność przeciwgrzybową i przeciwbakteryjną opisanych połączeń.
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Low-Molecular-Weight Aldehyde Inhibitors of Cathepsin G
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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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Designing of Substrates and Inhibitors of Bovine α-Chymotrypsin with Synthetic Phenylalanine Analogues in Position P1
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Molecular Modeling of the Neurohypophyseal Receptor/Atosiban Complexes
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Theoretical conformational analysis of six arginine vasopressin analogs with the l -naphthylalanine in position 3
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Molecular Dynamics Study of the Internal Water Molecules in Vasopressin and Oxytocin Receptors
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Molecular dynamics simulation of human neurohypophyseal hormone receptors complexed with oxytocin—modeling of an activated state
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Analysis of interactions responsible for vasopressin binding to human neurohypophyseal hormone receptors—molecular dynamics study of the activated receptor–vasopressin–Gα systems
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Solid phase synthesis and biological activity of linear tuftsin and retro-tuftsin derivatives
PublikacjaPrzedstawiono syntezę na fazie stałej nowych pochodnych tuftsyny i retro-tuftsyny i ich mikrobiologiczne właściwości. Otrzymane pochodne zawierały wiązanie izopeptydowe między epsilon-aminową grupą lizyny a takimi aminokwasami jak: Ala, beta-Ala, Val, Ile, Gly.
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Solid phase synthesis of 4,5,8-trihydroxy-9,10-anthraquinone-1-yl-(tuftsin or retro-tuftsin) derivatives
PublikacjaPrzedstawiono syntezę na fazie stałej połączeń leuko-1,4,5,8-tetra-hydroksyantrachinonów z pochodnymi tuftsyny i retro-tuftsyny zawierającymi wiązanie izopeptydowe. Do syntezy wykorzystano standardową metodę Fmoc i DIC jako odczynnik aktywujący.
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Conformational latitude – activity relationship of KPPR tetrapeptide analogues toward their ability to inhibit binding of vascular endothelial growth factor 165 to neuropilin‐1
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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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Introduction of Pro and Its Analogues in the Conserved P1 Position of Trypsin Inhibitor SFTI-1 Retains Its Inhibitory Activity
PublikacjaA 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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Analogues of trypsin inhibitor SFTI-1 modified in the conserved P1′ position by synthetic or non-proteinogenic amino acids retain their inhibitory activity
PublikacjaA 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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In vitro evaluation of novel lipopeptides with potential therapeutic application
PublikacjaThe synthesis of derivatives of Gly-His-Lys was elaborated followed by their antimicrobial activity investigation.
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Maria Jolanta Milewska prof. dr hab. inż.
OsobyMaria Jolanta Milewska, po ukończeniu Technikum Chemiczno-Mechanicznego w Wąbrzeźnie (specjalizacja: przetwórstwo tworzyw sztucznych) kontynuowała naukę na Wydziale Chemicznym Politechniki Gdańskiej. W 1979 r. zdobywa tytuł mgr inżyniera na kierunku Chemia, o specjalizacji Lekka Synteza Organiczna. Studium Doktoranckie PG ukończyła w 1984 r. W 1983 r została zatrudniona na macierzystym wydziale w Katedrze Chemii Organicznej, początkowo...
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GPU-Accelerated LOBPCG Method with Inexact Null-Space Filtering for Solving Generalized Eigenvalue Problems in Computational Electromagnetics Analysis with Higher-Order FEM
PublikacjaThis paper presents a GPU-accelerated implementation of the Locally Optimal Block Preconditioned Conjugate Gradient (LOBPCG) method with an inexact nullspace filtering approach to find eigenvalues in electromagnetics analysis with higherorder FEM. The performance of the proposed approach is verified using the Kepler (Tesla K40c) graphics accelerator, and is compared to the performance of the implementation based on functions from...
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Isothiocyanates may chemically detoxify mutagenic amines formed in heat processed meat
PublikacjaMeat consumption represents a dietary risk factor increasing the incidence of common cancers, probably due to carcinogenic amines (HAAs) formed upon meat heating. Interestingly, cancers whose incidence is increased by meat consumption, are decreased in populations consuming brassica vegetables regularly. This inverse correlation is attributed to brassica anticarcinogenic components, especially isothiocyanates (ITCs) that stimulate...
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HDAC Inhibitors: Innovative Strategies for Their Design and Applications
PublikacjaHistone deacetylases (HDACs) are a large family of epigenetic metalloenzymes that are involved in gene transcription and regulation, cell proliferation, differentiation, migration, and death, as well as angiogenesis. Particularly, disorders of the HDACs expression are linked to the development of many types of cancer and neurodegenerative diseases, making them interesting molecular targets for the design of new efficient drugs...
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Processing, physico-mechanical and thermal properties of reclaimed GTR and NBR/reclaimed GTR blends as function of various additives
PublikacjaIn this work, ground tire rubber (GTR) was mechano-chemically reclaimed in the presence of bitumen and various additives. During studies three types of processing and curing additives: (i) peptizer P300; (ii) vulcanization accelerator tetramethylthiuram disulfide (TMTD) and (iii) organic peroxide di(2-tert-butyl-peroxyisopropyl)benzene (BIB1) were applied to enhance reclaiming of GTR. Reclaiming process was evaluated by oscillating...
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Development of biocompatible iron oxide-silicon oxide core-shell nanoparticles as subcellular delivery platform for glucosamine-6-phosphate synthase inhibitors
PublikacjaIn order to develop the preparation of iron oxide-silica coreshell nanoparticles (CSNPs), thesis deeply explores the cetyltrimethylammonium (CTA+) directed silica coating methods of the oleic-acid capped iron oxide nanoparticles (OA-IONPs) initialized under near-neutral pH conditions. It is demonstrated that the initial alkaline hydrolysis of ethyl acetate in the presence of CTA+ and OA-IONPs induces an unusual ligand exchange...
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Poly-L-Lysine-modified boron-doped diamond electrodes for the amperometric detection of nucleic acid bases
PublikacjaBoron-doped diamond (BDD) is a very promising supporting material used in the construction of biosensors for molecular recognition. The direct immobilization of structurally-organized huge molecules, such as poly-L-Lysine (PLL) provides the possibility of determining organic molecules, e.g. nucleic acid bases (e.g. adenine, guanine) or peptides and proteins. This paper describes the direct method for chemical and electrochemical...
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Tuning matrix-vector multiplication on GPU
PublikacjaA matrix times vector multiplication (matvec) is a cornerstone operation in iterative methods of solving large sparse systems of equations such as the conjugate gradients method (cg), the minimal residual method (minres), the generalized residual method (gmres) and exerts an influence on overall performance of those methods. An implementation of matvec is particularly demanding when one executes computations on a GPU (Graphics...
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A MODEL FOR FORECASTING PM10 LEVELS WITH THE USE OF ARTIFICIAL NEURAL NETWORKS
PublikacjaThis work presents a method of forecasting the level of PM10 with the use of artificial neural networks. Current level of particulate matter and meteorological data was taken into account in the construction of the model (checked the correlation of each variable and the future level of PM10), and unidirectional networks were used to implement it due to their ease of learning. Then, the configuration of the network (built on the...
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Selected organophosphorus compounds with biological activity. Applications in medicine
PublikacjaThe purpose of this article is to provide an overview of the latest applications of organophosphorus compounds (OPs) that exhibit biological activity. A large family of OPs have become popular in recent years. The practical application of OPs in modern medicine has been attributed to their unique properties. In this article, the methods used to select these compounds will be emphasized. This paper will first outline the findings...
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Interaction of the conserved region 4.2 of sigma(E) with the RseA anti-sigma factor
PublikacjaEo-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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Chemical and biological stability of polyene macrolides
PublikacjaThe polyene macrolide antibiotics have been used in an-tifungal therapy since first o f them were discovered in 1950's. Up to now, four polyene macrolides are being used in medical practice, namely amphotericin B, nystatin, candi-cidin and pimaricin.The antifungal activity and mode of ac-tion of polyene macrolides is determined by their structure, chemical and physical properties.The main fragment of polyene...
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Morphology control via dual solvent crystallization for high-mobility functionalized pentacene-blend thin film transistors
PublikacjaWe present an approach to improving the performance of solution processed organic semiconductor transistors based on a dual solvent system. We here apply this to a blend containing the π-conjugated small molecule 6,13 bis(triisopropylsilylethynyl) pentacene (TIPS-pentacene) and polystyrene, which acts as an inert binder. Using a semiconductor-binder solution of two solvents, where the main solvent is a better solvent of the small...
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The Drop-in-Drop Encapsulation in Chitosan and Sodium Alginate as a Method of Prolonging the Quality of Linseed Oil
PublikacjaNowadays, the encapsulation of sensitive products by various techniques has become popular as a promising preservation method. In particular, this applies to oils with a high content of unsaturated fatty acids and a high susceptibility to deterioration. This work presents the possibility of using a chitosan and sodium alginate in the form of a hydrogel membrane to protect food ingredients such as linseed oil, which is stored in...
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Widening of the electroactivity potential range by composite formation – capacitive properties of TiO2/BiVO4/PEDOT:PSS electrodes in contact with an aqueous electrolyte
PublikacjaComposites based on the titania nanotubes were tested in aqueous electrolyte as a potential electrode material for energy storage devices. The nanotubular morphology of TiO2 was obtained by Ti anodization. TiO2 nanotubes were covered by a thin layer of bismuth vanadate using pulsed laser deposition. The formation of the TiO2/BiVO4 junction leads to enhancement of pseudocapacitance in the cathodic potential range. The third component,...
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Anticandiadal properties of N-acylpeptides containing inhibitor of glucosamine-6-phosphate synthase
PublikacjaOtrzymano 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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Enzymatic degradation and transport of endothiopeptides into Escherichia coli K12 mutant strains
PublikacjaZbadano transport trzech otrzymanych na drodze syntezy ditiopeptydów do komórek Escherichia coli K12. Ponadto zbadano szybkość hydrolizy tych związków. Wszystkie peptydy są transportowane przez permeazy, natomiast są bardziej oporne na hydrolizę enzymatyczną w stosunku do naturalnych peptydów.
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A novel chemiluminescent immunoassay based on original acridinium ester labels as better solution for diagnosis of human toxoplasmosis than conventional ELISA test
PublikacjaToxoplasma gondii infection is one of the most common human zoonosis. Laboratory diagnosis of this disease is mainly based on the results of serological methods detecting specific antibodies in the patient’s sera. In this study we aimed to evaluate the performance of a chemiluminescence immunoassay (CLIA) based on the use of a novel immunochemical reagent in the form of the conjugate of original acridinium label (AL) attached to...
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A non-linear direct peridynamics plate theory
PublikacjaIn this paper a direct non-local peridynamics theory for thin plates is developed. Peridynamic points are assumed to behave like rigid bodies with independent translation and finite rotation degrees of freedom. The non-local mechanical interaction between points is characterized by force and moment vectors. The balance equations including the linear momentum, the angular momentum and the energy are presented. Peridynamic deformation...
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Interactions of fish gelatin and chitosan in uncrosslinked and crosslinked with EDC films: FT-IR study
PublikacjaFilms based on fish gelatin, chitosan and blend of fish gelatin and chitosan before and after cross-linking with EDC have been characterized by FT-IR spectroscopy. The FT-IR spectrum of fish gelatin film showed the characteristic amide I, amide II and amide III bands, and the FT-IR spectrum of chitosan film confirmed that the polymer was only a partially deacetylated product, and included CH3-C=O and NH2 groups, the latter both...
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Mechanism of Osmolyte Stabilization–Destabilization of Proteins: Experimental Evidence
PublikacjaIn this work, we investigated the influence of stabilizing (N,N,N-trimethylglycine) and destabilizing (urea) osmolytes on the hydration spheres of biomacromolecules in folded forms (trpzip-1 peptide and hen egg white lysozyme─hewl) and unfolded protein models (glycine─GLY and N-methylglycine─NMG) by means of infrared spectroscopy. GLY and NMG were clearly limited as minimal models for unfolded proteins and should be treated with...
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Interactions in Ternary Aqueous Solutions of NMA and Osmolytes—PARAFAC Decomposition of FTIR Spectra Series
PublikacjaIntermolecular interactions in aqueous solutions are crucial for virtually all processes in living cells. ATR-FTIR spectroscopy is a technique that allows changes caused by many types of such interactions to be registered; however, binary solutions are sometimes difficult to solve in these terms, while ternary solutions are even more difficult. Here, we present a method of data pretreatment that facilitates the use of the Parallel...
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Naturalne związki organiczne
PublikacjaKsiążka zawiera dwanaście rozdziałów merytorycznych, w których omówiono występowanie, właściwości, otrzymywanie i zastosowanie następujących naturalnych organicznych: aminokwasy, peptydy, białka, cukry, lipidy, alkaloidy, steroidy, kwasy nukleinowe, polifenole i flawonoidy, hormony owadzie i roślinne, terpenoidy i izoterpenoidy oraz związki sygnałowe (feromony).
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One-dimensional chaos in a system with dry friction: analytical approach
PublikacjaWe introduce a new analytical method, which allows to find chaotic regimes in non-smooth dynamical systems. A simple mechanical system consisting of a mass and a dry friction element is considered. The corresponding mathematical model is being studied. We show that the considered dynamical system is a skew product over a piecewise smooth mapping of a segment (the so-called base map). For this base map we demonstrate existence of...