Wyniki wyszukiwania dla: PEPTIDE%20CONJUGATES
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Interactions of vasopressin and oxytocin receptors with vasopressin analogues substituted in position 2 with 3,3′-diphenylalanine - a molecular docking study
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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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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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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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Reverse vaccinology-based prediction of a multi-epitope SARS-CoV-2 vaccine and its tailoring to new coronavirus variants
PublikacjaThe genome feature of SARS-CoV-2 leads the virus to mutate and creates new variants of concern. Tackling viral mutations is also an important challenge for the development of a new vaccine. Accordingly, in the present study, we undertook to identify B- and T-cell epitopes with immunogenic potential for eliciting responses to SARS-CoV-2, using computational approaches and its tailoring to coronavirus variants. A total of 47 novel...
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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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Improved cytotoxicity and preserved level of cell death induced in colon cancer cells by doxorubicin after its conjugation with iron-oxide magnetic nanoparticles
PublikacjaA promising strategy for overcoming the problem of limited efficacy in antitumor drug delivery and in drug release is the use of a nanoparticle-conjugated drug. Doxorubicin (Dox) anticancer chemotherapeutics has been widely studied in this respect, because of severe cardiotoxic side effects. Here, we investigated the cytotoxic effects, the uptake process, the changes in cell cycle progression and the cell death processes in the...
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Development of Biocompatible Fe3O4@SiO2 Nanoparticles as Subcellular Delivery Platform for Glucosamine-6-phosphate Synthase Inhibitors
PublikacjaNumerous inhibitors of glucoseamine-6-phophate synthase (GlcN-6-P), the enzyme responsible from catalysis of the first step of metabolic pathway leading to metabolism 5’-diphospho-N-acetyl-D- glucosamine, were reported as effective agents for inhibiting the growth of various fungal pathogens. Among the reported inhibitors,...
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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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Investigations on the immunosuppressive activity of derivatives of mycophenolic acid in immature dendritic cell
PublikacjaThe main activity of mycophenolic acid (MPA) and its analogs is the inhibition of proliferation of T cells. Here, we hypothesized that MPA and its conjugates inhibits also the activity of antigen-presenting cells (APC) including dendritic cells (DCs). We tested the effect of novel amino acid derivatives of MPA and conjugates of MPA with acridines/acridones on DCs by flow cytometry, ELISA and MLR assay. Both acridines/acridone derivatives...
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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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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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Synthesis, characterization, and interactions of single-walled carbon nanotubes modified with doxorubicin with Langmuir–Blodgett biomimetic membranes
PublikacjaThe synthesis, characterization, and the influence of single-walled carbon nanotubes (SWCNTs) modified with an anticancer drug doxorubicin (DOx) on the properties of model biological membrane as well as the comparison of the two modes of modification has been presented. The drug was covalently attached to the nanotubes either preferentially on the sides or at the ends of the nanotubes by the formation of hydrazone bond. The efficiency...
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The compositional space of exhaled breath condensate and its link to the human breath volatilome
PublikacjaBreath analysis is commonly understood to target gaseous or volatile organic compounds (VOCs) for the characterization of different pathologies. Targeted analysis is most effective if a working hypothesis can be based on a plethora of data. The recently published volatilome builds an optimal basis for organizing powerful target sets. However, the origin and pathways of biosynthesis of many VOCs are not known, which complicates...
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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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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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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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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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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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Keratinocyte-derived small extracellular vesicles supply antigens for CD1a-resticted T cells and promote their type 2 bias in the context of filaggrin insufficiency
PublikacjaIntroduction: Exosome-enriched small extracellular vesicles (sEVs) are nanosized organelles known to participate in long distance communication between cells, including in the skin. Atopic dermatitis (AD) is a chronic inflammatory skin disease for which filaggrin (FLG) gene mutations are the strongest genetic risk factor. Filaggrin insufficiency affects multiple cellular function, but it is unclear if sEV-mediated cellular communication...
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Low-power microwave-induced fabrication of functionalised few-layer black phosphorus electrodes: A novel route towards Haemophilus Influenzae pathogen biosensing devices
PublikacjaIn this paper, various passivation schemes were applied at few-layer black phosphorus (FLBP) to achieve covalent functionalisation with 4-azidobenzoic acid, improving its electrochemical response intended for analytical and biosensing applications. The thermal and microwave assisted modification procedures in toluene and dime-thylformamide resulted in high reversibility of reactions on functionalised FLBP using a ferricyanide/ferrocya-nide...
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Recent Developments in Data-Assisted Modeling of Flexible Proteins
PublikacjaMany proteins can fold into well-defined conformations. However, intrinsically-disordered proteins (IDPs) do not possess a defined structure. Moreover, folded multi-domain proteins often digress into alternative conformations. Collectively, the conformational dynamics enables these proteins to fulfill specific functions. Thus, most experimental observables are averaged over the conformations that constitute an ensemble. In this...
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Novel Functionalization of Boron-Doped Diamond by Microwave Pulsed-Plasma Polymerized Allylamine Film
PublikacjaWe report the novel modification of a hydrogen-terminated polycrystalline boron-doped electrode with a microwave pulsed-plasma polymerized allylamine. Boron-doped diamond (BDD) was coated with a very thin layer of adherent cross-linked, pinhole- and additive-free allylamine plasma polymer (PPAAm) resistant to hydrolysis and delamination and characterized by a high density of positively charged amino groups. The pulsed microwave...
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Niebiałkowe związki azotowe
PublikacjaNiebiałkowe związki azotowe powstają w żywności wskutek enzymatycznych prze-mian różnych substratów zawierających w swym składzie azot. Są wśród nichprzede wszystkim aminokwasy, peptydy, nukleotydy, tlenek trimetyloaminy orazaminy i ich pochodne. Wywierają one korzystny lub niepożądany wpływ na smak,zapach i barwę żywności, mogą służyć jako wskaźniki świeżości, lub mogą byćspożywane w nadmiernych ilościach, wywierać działanie...
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Zastosowanie bakteriocyn - peptydów o aktywności bakteriobójczej
PublikacjaBakteriocyny są to peptydy bakteriobójcze produkowane przez wiele rodzajów bakterii w celu eliminacji ze środowiska bakterii innych rodzajów lub konkurowania z nimi. Cechą charakterystyczną tych peptydów jest to, że są one syntetyzowane na rybosomach. Mogą być modyfikowane potranslacyjnie lub nie. W chwili obecnej bakteriocyny stosowane są w przemyśle spożywczym jako dodatek do produktów żywnościowych, jednak ich potencjał aplikacyjny...
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Antifungal activity of thionated analogues of nva-fmdp and lys-nva-fmdp
Publikacjaotrzymano dwa peptydy w których wiązanie amidowe łączące aminokwasy zamieniono na tioamidowe w wyniku kilkunastoetapowej syntezy chemicznej. do reakcji tionowania zastosowano odczynnik lawessona. otrzymane związki poddano badaniom aktywności z wykorzystaniem pięciu szczepów candida , w tym szczepów opornych na flukonazol. stwierdzono, ze obecniość wiązania tioamidowego znacznie obniża aktywność przeciwgrzybową testowanych związków...
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Citropin 1.1 Trifluoroacetate to Chloride Counter-Ion Exchange in HCl-Saturated Organic Solutions: An Alternative Approach
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Ageing-Time Dependent Changes of Angiotensin I-Converting Enzyme-Inhibiting Activity of Protein Hydrolysates Obtained from Dry-Cured Pork Loins Inoculated with Probiotic Lactic Acid Bacteria
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A cryptic ribosome binding site, false signals in reporter systems and avoidance of protein translation chaos
PublikacjaThe expression of reporter gene may be induced by activation of cryptic signalling sequences, as we found while constructing the mutS-lacZ fusion gene. We cloned the Escherichia coli lacZ gene encoding beta-galactosidase into a plasmid vector carrying the Thermus thermophilus mutS gene. The clones expected to produce beta-galactosidase as the C-terminal fusion were selected for the complementation of beta-galactosidase activity...
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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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Specific Binding of Cholesterol to the Amyloid Precursor Protein: Structure of the Complex and Driving Forces Characterized in Molecular Detail
PublikacjaC99 is the C-terminal membrane-bound fragment of the amyloid precursor protein that is cleaved by γ-secretase to release Aβ peptides, the hallmark of Alzheimer’s disease (AD). Specific interactions of C99 with cholesterol have been proposed to underlie the recognized role of cholesterol in promoting amyloidogenesis. By using molecular dynamics simulations, we studied cholesterol binding to C99 in a lipid bilayer. We determined...
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Synthesis of amides under microwave irradiation
PublikacjaAmides belong to the most important carboxylic acid derivatives. They are constituents of natural compounds like peptides and proteins. They found applications in many branches of science and industry, especially in pharmaceutical and polymer science. Conventional procedures for amide preparation involve reaction between amine and carboxylic acid or their more active derivatives such as acid chlorides, acid anhydrides or esters....
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Biowaste chicken eggshell powder as a potential cure modifier for epoxy/anhydride systems: competitiveness with terpolymer-modified calcium carbonate at low loading levels
PublikacjaBiowaste chicken eggshell (ES) powder was applied as a potential cure modifier in epoxy/anhydride systems. Cure behaviour and kinetics of composites filled with very low content (0.1 wt% based on epoxy resin) of ES, calcium carbonate (CaCO3), and terpolymer-modified fillers, mES and mCaCO3, were discussed comparatively. Surface analysis was performed by X-ray photoelectron spectroscopy. Cure kinetics was investigated by differential...
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Niebiałkowe związki azotowe. Rozdział 8
PublikacjaAzot związków niebiałkowych stanowi od kilku do kilkudziesięciu procent ogólnej ilości azotu w różnych surowcach żywnościowych. Wskutek enzymatycznych i chemicznych przemian w czasie przechowywania i przetwarzania zmienia się udział i skład tych związków. Niebiałkowe związki azotowe uczestniczą w tworzeniu zapachu i smaku produktów żywnościowych, niektóre z nich, np. histamina są szkodliwe dla zdrowia, inne np N-nitrozoaminy lub...
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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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Quantum and carbon dots conjugated molecularly imprinted polymers as advanced nanomaterials for selective recognition of analytes in environmental, food and biomedical applications
PublikacjaSamples with complex matrix analyzed during explanation of pathogenesis of various diseases and food or environmental monitoring request advanced analytical and instrumental devices. Among the materials used for described purposes, quantum (QDs) or carbon dots (CDs) layered by molecularly imprinted polymer (MIP) shells have gained widespread attention. Unique optical and physicochemical properties of QDs/CDs together with high...
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Human carnosinases: A brief history, medicinal relevance, and in silico analyses
PublikacjaCarnosine, an endogenous dipeptide, has been found to have a plethora of medicinal properties, such as antioxidant, antiageing, and chelating effects, but with one downside: a short half-life. Carnosinases and two hydrolytic enzymes, which remain enigmatic, are responsible for these features. Hence, here we emphasize why research is valuable for better understanding crucial concepts like ageing, neurodegradation, and cancerogenesis,...
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Silica In Silico: A Molecular Dynamics Characterization of the Early Stages of Protein Embedding for Atom Probe Tomography
PublikacjaA novel procedure for the application of atom probe tomography (APT) to the structural analysis of biological systems, has been recently proposed, whereby the specimen is embedded by a silica matrix and ablated by a pulsed laser source. Such a technique, requires that the silica primer be properly inert and bio-compatible, keeping the native structural features of the system at hand, while condensing into an amorphous, glass-like...
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Anharmonic Infrared Spectroscopy through the Fourier Transform of Time Correlation Function Formalism in ONETEP
PublikacjaDensity functional theory molecular dynamics (DFT-MD) provides an efficient framework for accurately computing several types of spectra. The major benefit of DFTMD approaches lies in the ability to naturally take into account the effects of temperature and anharmonicity, without having to introduce any ad hoc or a posteriori corrections. Consequently, computational spectroscopy based on DFT-MD approaches plays a pivotal role in...
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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
PublikacjaA 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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Cytocompatibility of stabilized black phosphorus nanosheets tailored by directly conjugated polymeric micelles for human breast cancer therapy
PublikacjaThe novel procedure of few-layer black phosphorus (FLBP) stabilization and functionalisation was here proposed. The cationic polymer PLL and non-ionic PEG have been involved into encapsulation of FLBP to allow sufficient time for further nanofabrication process and overcome environmental degradation. Two different spacer chemistry was designed to bind polymers to tumor-homing peptides. The efficiency of functionalisation was examined...
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Naturalne związki organiczne
PublikacjaNowoczesny podręcznik stanowiący kompendium podstawowych wiadomości o najważniejszych naturalnych związkach organicznych, takich jak: aminokwasy, peptydy, białka, cukry, lipidy, alkaloidy, steroidy, terpeny i terpenoidy. Omówiono w nim właściwości chemiczne i fizyczne, działanie fizjologiczne oraz otrzymywanie i zastosowanie tych związków. Przedstawiono również najnowsze osiągnięcia naukowe dotyczące produktów naturalnych, m.in....
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Naturalne związki organiczne.
PublikacjaNowoczesny podręcznik stanowiący kompendium podstawowych wiadomości o najważniejszych naturalnych związkach organicznych, takich jak: aminokwasy, peptydy, białka, cukry, lipidy, alkaloidy, steroidy, terpeny i terpenoidy. Omówono w nim właściwości chemiczne i fizyczne, działanie fizjologiczne oraz otrzymywanie i zastosowanie tych związków. Przedstawiono również najnowszeosiągnięcia naukowe dotyczące produktów naturalnych, m.in....