Search results for: conjugate transporters
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The Role of Hypoxia-Inducible Factor-1α, Glucose Transporter-1, (GLUT-1) and Carbon Anhydrase IX in Endometrial Cancer Patients
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Life-long norepinephrine transporter (NET) knock-out leads to the increase in the NET mRNA in brain regions rich in norepinephrine terminals
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Molecular Umbrella as A Nanocarrier for Antifungals
PublicationA molecular umbrella composed of two O‐sulfated cholic acid residues was applied for the construction of conjugates with cispentacin, containing a “trimethyl lock” (TML) or o‐dithiobenzylcarbamoyl moiety as a cleavable linker. Three out of five conjugates demonstrated antifungal in vitro activity against C. albicans and C. glabrata but not against C. krusei, with MIC90 values in the 0.22–0.99 mM range and were not hemolytic. Antifungal...
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Peptide conjugates of lactoferricin analogues and antimicrobials—Design, chemical synthesis, evaluation of antimicrobial activity and mammalian cytotoxicity
PublicationEight new peptide conjugates composed of modified bovine lactoferricin truncated analogues (LFcinB) and oneof the three antimicrobials — ciprofloxacin (CIP), levofloxacin (LVX), and fluconazole (FLC) — were synthesized. Four different linkers were applied to connect a peptide and an antimicrobial agent. The FLC-containing peptidic conjugates were synthesized using the “click chemistry” method. This novel approach is reported here...
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Folic acid-conjugated mesoporous silica particles as nanocarriers of natural prodrugs for cancer targeting and antioxidant action
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Peptydowe koniugaty antrachinonów i ich aktywność biologiczna = Peptidyl anthraquinone conjugates and its biological activity
PublicationW artykule opisano syntezę i aktywność biologiczną peptydowych koniugatów antrachinonów. Koniugaty takie są nie tylko potencjalnymi chemoterapeutykami, ale także odgrywają rolę barwnych ligandów w metodach oczyszczania białek, technikach histochemicznych i badaniu helikalnej struktury DNA z zastosowaniem spektroskopii UV i UV-Vis.
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Synthesis and biological activity of tuftsin, its analogues and conjugates containing muramyl dipeptides of nor-muramyl dipeptides
PublicationOpisano syntezę koniugatów MDP oraz nor-MDP modyfikowanych w części peptydowej tuftsyną oraz pochodną tuftsyny zawierającą grupę nitrową. Zsyntetyzowane związki zostały przebadane in vitro na ludzkich monocytach i limfocytach w Akademii Medycznej w Gdańsku. Niektóre z nich wykazały szybsze i skuteczniejsze działanie w porównaniu z tuftsyną.
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Photodynamic inactivation of Enterococcus faecalis by conjugates of zinc(II) phthalocyanines with thymol and carvacrol loaded into lipid vesicles
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Numerical model for thin liquid film with evaporation and condensation on solid surfaces in systems with conjugated heat transfer
PublicationCondensation and evaporation processes from wetted surfaces are of utmost importance in many technological or industrial applications. In many devices such as home-appliances and air conditioning systems just to name a few, condensation and evaporation processes greatly impact their performance and energy efficiency; The physics of these processes is quite complex, involving conjugate heat transfer among solid–liquid film-gaseous...
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TRANSPORTER Wydziałowe Targi Pracy
EventsBiuro Karier, Wydział OiO, studenci kierunku Transport oraz WRS OiO serdecznie zapraszają na Targi Pracy TRANSPORTER.
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Molecular Umbrellas Modulate the Selective Toxicity of Polyene Macrolide Antifungals
PublicationAntifungal polyene macrolide antibiotics Amphotericin B (AmB) and Nystatin (NYS) were conjugated through the ω-amino acid linkers with diwalled “molecular umbrellas” composed of spermidine-linked deoxycholic or cholic acids. The presence of “umbrella” substituents modulated biological properties of the antibiotics, especially their selective toxicity. Some of the AmB-umbrella conjugates demonstrated antifungal in vitro activity...
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Efficient Gradient-Based Algorithm with Numerical Derivatives for Expedited Optimization of Multi-Parameter Miniaturized Impedance Matching Transformers
PublicationFull-wave electromagnetic (EM) simulation tools have become ubiquitous in the design of microwave components. In some cases, e.g., miniaturized microstrip components, EM analysis is mandatory due to considera¬ble cross-coupling effects that cannot be accounted for otherwise (e.g., by means of equivalent circuits). These effects are particularly pronounced in the structures in¬volving slow-wave compact cells and their numerical...
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Elastic multi-layer resilient IP-over-Flexgrid networking: Detailed cost analysis with bandwidth-variable transponders
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Multi-objective optimization of compact UWB impedance matching transformers using Pareto front exploration and adjoint sensitivities
PublicationIn this paper, a technique for fast multi-objective optimization of impedance matching transformers has been presented. In our approach, a set of alternative designs that represent the best possible trade-offs between conflicting objectives (here, the maximum reflection level within a frequency band of interest and the circuit size) is identified by directly exploring the Pareto front. More specifically, the subsequent Pareto-optimal...
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Measurements of no-load and short-circuit parameters of power transformers with taps
Open Research Data1) The Laboratory LINTE^2 is a large research infrastructure operated by the Faculty of Electrical and Control Engineering at Gdańsk University of Technology, to be found in Gdańsk, Poland (54.3690 N, 18.6130 E).
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Electrochemical detection of bacterial endotoxin lipopolysaccharide (LPS) on gold electrode modified with DAL-PEG-DK5-PEG-OH - Antimicrobial peptide conjugate
PublicationThis work describes fabrication of gold electrodes modified with peptide conjugate DAL-PEG-DK5-PEG-OH that enables ultra-sensitive detection of lipopolysaccharide (LPS) isolated from the reference strain of Escherichia coli O26:B6. The initial step of the established procedure implies immobilization of the fully protected DAL-PEG-DK5-PEG-OH peptide on the surface of the gold electrode previously modified by cysteamine. Then side...
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Immunosuppressive properties of amino acid and peptide derivatives of mycophenolic acid
PublicationMycophenolic acid (MPA) was coupled with amino acids and biologically active peptides including derivatives of tuftsin to modify its immunosuppressive properties. Both amino acid unit in the case of simple MPA amides and modifications within peptide moiety of MPA - tuftsin conjugates influenced the observed activity. Antiproliferative potential of the obtained conjugates was investigated in vitro and MPA amides with threonine methyl...
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Cytocompatibility of stabilized black phosphorus nanosheets tailored by directly conjugated polymeric micelles for human breast cancer therapy
PublicationThe 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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Synthesis and Characterization of New Conjugated Azomethines End-Capped with Amino-thiophene-3,4-dicarboxylic Acid Diethyl Ester
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Dual-Activity Fluoroquinolone-Transportan 10 Conjugates offer alternative Leukemia therapy during Hematopoietic Cell Transplantation
PublicationHematopoietic cell transplantation (HCT) is often considered a last resort leukemia treatment, fraught with limited success due to microbial infections, a leading cause of mortality in leukemia patients. To address this critical issue, we explored a novel approach by synthesizing antileukemic agents containing antibacterial substances. This innovative strategy involves conjugating fluoroquinolone antibiotics, such as ciprofloxacin...
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The Product of Matrix Metalloproteinase Cleavage of Doxorubicin Conjugate for Anticancer Drug Delivery: Calorimetric, Spectroscopic, and Molecular Dynamics Studies on Peptide–Doxorubicin Binding to DNA
PublicationMatrix metalloproteinases (MMPs) are extracellular matrix degradation factors, promoting cancer progression. Hence, they could provide an enzyme-assisted delivery of doxorubicin (DOX) in cancer treatment. In the current study, the intercalation process of DOX and tetrapeptide-DOX, the product of the MMPs' cleavage of carrier-linked DOX, into dsDNA was investigated using stationary and time-resolved fluorescence spectroscopy, UV-Vis...
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Cations of amino acid alkyl esters conjugated with an anion from the group of NSAIDs – As tunable pharmaceutical active ionic liquids
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Synthesis of conjugates of muramyl dipeptide and nor-muramyl dipeptide with retro-tuftsin (Arg-Pro-Lys-ThrOMe) as potential immunostimulants.
PublicationOpisano syntezę nowych koniugatów muramylodipeptydu i nor-muramylo-dipeptydu z estrem metylowym tuftsyny o odwróconej sekwencji (Arg-Pro-Lys-Thr-OMe)jako potencjalnych immunostymulantów. Synteza tych połączeń została przeprowadzona zgodnie z zasadami chemii peptydów.
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Surface Site Modulations by Conjugated Organic Molecules To Enhance Visible Light Activity of ZnO Nanostructures in Photocatalytic Water Splitting
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In vitro studies of antimicrobial activity of Gly-His-Lys conjugates as potential and promising candidates for therapeutics in skin and tissue infections
PublicationWe presented in vitro studies of antimicrobial activity of Gly-His-Lys conjugates that are important point in preliminary biological evaluation of their potential application in skin and tissue therapy. The novel compounds include the conjugation of fatty acids with a modification of the amino acid sequence in the primary structure of Gly-His-Lys.
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Resistance of human prostate carcinoma cells to a new antitumor compound capridine beta is associated with changed drug metabolism combined with both inherent and drug-induced overexpression of ABC transporters
PublicationW pracy charakteryzujemy mechanizm oporności na nową pochodną 1-nitroakrydyny, związku capridine beta (C-1748) o wysokiej aktywności przeciwnowotworowej, znajdującego się w badaniach klinicznych. Nasze dane wskazują, że oporność na ten związek jest wynikiem zmienionego metabolizmu inaktywującego C-1748 oraz wzrostem ekspresji pompy błonowej ABCG2 a także innych białek transportowych typu ABC.
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Characteristics of the Conjugative Transfer System of the IncM Plasmid pCTX-M3 and Identification of Its Putative Regulators
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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
PublicationSamples 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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Synthesis of π-extended and bowl-shaped sumanene–ferrocene conjugates and their application in highly selective and sensitive cesium cations electrochemical sensors
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New conjugates of muramyl dipeptide and nor-muramyl dipeptide linked to tuftsin and retro-tuftsin derivatives significantly influence their biological activity
PublicationOpisano syntezę nowych koniugatów MDP i nor-MDP z pochodnymi tuftsyny i retro-tuftsyny zawierającymi wiązanie izopeptydowe pomiędzy epsilon-aminową grupą lizyny, a karboksylową grupą Ala, Gly czy Val. Zbadano ich aktywność biologiczną, m.in. profil cytokinowy.
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Novel insights into conjugation of antitumor-active unsymmetrical bisacridine C-2028 with glutathione: characteristics of non-enzymatic and glutathione S-transferase-mediated reactions
PublicationUnsymmetrical bisacridines (UAs) are a novel potent class of antitumor-active therapeutics. A significant route of phase II drug metabolism is conjugation with glutathione (GSH), which can be non-enzymatic and/or catalyzed by GSH-dependent enzymes. The aim of this work was to investigate the GSH-mediated metabolic pathway of a representative UA, C 2028. GSH supplemented incubations of C-2028 with rat, but not with human, liver...
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Quantum dots conjugates with unsymmetrical bisacridines enhance cytotoxicity of these antitumor compounds in lung cancer cells and have protecting effects on normal cells
PublicationBackground: In recent years, with the rapid development of nanotechnology and its extensive applications in the medicine, nanocarriers for anticancer drug delivery have gained a great importance. Spherical semiconductor nanocrystals, frequently called quantum dots (QDs) are very attractive nanomaterials for bioimaging applications and they possess properties as potential candidates for drug carrier. Unsymmetrical bisacridines (UAs),...
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Genetic characterization of the CcpA-dependent, cellobiose-specific PTS system comprising CelB, PtcB and PtcA that transports lactose in Lactococcus lactis IL1403
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Poly(amic acid)s vs. polyimides with π-conjugated –N N- units: Cis-trans isomerization reaction and kinetics of thermal imidization
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The synthesis and biological activity of lipophilic derivatives of bicine conjugated with n3-(4-methoxyfumaroyl)-l-2,3-diaminopropanoic acid(fmdp) - an inhibitor of glucosamine-6-phosphate synthase
PublicationOtrzymano serię pochodnych bicyny połączonych z inhibitorem syntazy glukozamino-6-fosforanu (fmdp)oraz zbadano ich właściwości lipofilowe i aktywność przeciwgrzybową. otrzymane związki charakteryzowały się wyższą llipofilowością niż fmdp. wszystkie otrzymane związki wykazywały także wyższą aktywność przeciwgrzybową niż fmdp.
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Analytical data on molecular umbrella: cispentacin and molecular umbrella: fluorescent probe conjugates
Open Research DataAnalytical data (NMR, MS, FTIR) for nine conjugates of molecular umbrella with cispentacin, Lys(Mca) or Nap-NH2. The conjugates have been rationally designed as potential antifungal agents. 1H NMR and 13C NMR spectra were obtained at 500 MHz Varian Unity Plus spectrometer and the deuterated solvents were used as internal locks. High-resolution mass...
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Sławomir Milewski prof. dr hab. inż.
PeopleSławomir Milewski, born in 1955 in Puck, Poland, graduated in 1979 in Chemistry from the Faculty of Chemistry, Gdańsk University of Technology (GUT). In 1984 was employed at the Department of Pharmaceutical Technology and Biochemistry. In 1985 he got his PhD, in 1994 became a DSc (habilitation) and in 2002 got the professorship in chemical sciences. Currently he is a full professor and Head of the Department of Pharmaceutical Technology...
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Enzymatic cleavage of specific dipeptide conjugated with ferrocene as a flexible ultra-sensitive and fast voltammetric assay of matrix metalloproteinase-9 considered a prognostic cancer biomarker in plasma samples
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Microorganisms from starter and protective cultures - Occurrence of antibiotic resistance and conjugal transfer of tet genes in vitro and during food fermentation
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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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Marek Adamowicz dr hab. inż.
PeopleStopień naukowy doktora uzyskał w 2008 r. na Wydziale Elektrotechniki i Automatyki Politechniki Gdańskiej. W latach 2005 – 2011 pracował na Akademii Morskiej w Gdyni. W 2010 r. jako laureat programu NCBR LIDER wybrał Wydział Elektrotechniki i Automatyki Politechniki Gdańskiej jako jednostkę realizującą swój projekt z zakresu szerokopasmowych przyrządów półprzewodnikowych i ich zastosowań w elektrowniach wiatrowych. Od 2011 roku...
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The content of conjugated linoleic acid and vaccenic acid in the breast milk of women from Gdansk and the surrounding district, as well as in, infant formulas and follow-up formulas. Nutritional recommendation for nursing women
PublicationFatty acids are some of the most important components of human milk. Polyunsaturated fatty acids (PUFAs) are essential nutrients required for the optimal growth and development of infants, especially the central nervous system, brain and retina. AIM: To determine the conjugated linolenic acid (CLA) and vaccenic acid (VA) content of human breast milk from mothers consuming different diets, and to compare the results with CLA and...
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New Chalcones Derivatives With Potent Antitumor Activity And Their Metabolism In Vitro
PublicationChalcone derivatives exhibit a broad range of biological activities, with antioxidant and cytotoxic properties among the most studied. Despite numerous reports on chalcones as cytotoxic, and potentially anticancer agents, very little is know on their actual mechanism of activity. Generally, chalcones are considered as antimitotic agents, which interfere with tubulin assembly.We have recently developed a new class of chalcones with...
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Anna Lisowska-Oleksiak prof. dr hab.
PeopleAnna Lisowska-Oleksiak, born in 1952, has been working at GUT since 1977. Currently is employed at the Faculty of Chemistry as a full professor. She was employed as a research assistant at the University of St Andrews in the group of C. A. Vincent and P.G. Bruce (1991-1994). She completed a two-month research internship in CEA Grenoble (2011). Anna Lisowska-Oleksiak obtained her MSc in chemistry at Nicolaus Copernicus University...
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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
PublicationA 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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Oligopeptide antifungals are exceptionally active against multidrug-resistant yeast
PublicationPermeazy 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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Nuclear Magnetic Resonance data for the synthesis of esterase cleavable antifungal conjugates containing fatty acids as molecular carriers
Open Research DataNMR data for novel organic compounds - conjugates composed of C2-18 fatty acid (FA) residues as a molecular carrier and 5-fluorocytosine (5-FC) as an active agent, released upon the action of intracellular esterases on the ester bond between FA and “trimethyl lock” intramolecular linker.
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Michał Michna dr hab. inż.
PeopleMichal Michna received the M.Sc. and Ph.D. degrees in electrical engineering from the Gdansk University of Technology (GUT), Gdansk, Poland, in 1998 and 2005, respectively. Since 2004, he was employed at the Department of Power Electronics and Electrical Machines of the Gdańsk University of Technology (assistant, assistant professor, senior lecturer). In 2010-2015 he was a deputy of head of the Department of Power Electronics and...
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‘Acridines’ as New Horizons in Antifungal Treatment
PublicationFrequent fungal infections in immunocompromised patients and mortality due to invasive mycosis are important clinical problems. Opportunistic pathogenic Candida species remain one of the leading causes of systemic mycosis worldwide. The repertoire of antifungal chemotherapeutic agents is very limited. Although new antifungal drugs such as lanosterol 14α-demethylase and β-glucan synthase inhibitors have been introduced into clinical...
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The mechanism of internalization study of QDgreen−CD−FA−C−2028 conjugate at IC80 value to cancer (H460, Du-145, and LNCaP) and normal (MRC-5 and PNT1A) cells
Open Research DataThe influence of different endocytosis inhibitors on the internalization of QDgreen−CD−FA−C−2028 conjugate at IC80 value in cancer (H460, Du-145, and LNCaP) and normal (MRC-5 and PNT1A) cells. First, the cells were preincubated with: drug-free medium (no inhibitor), at 4 °C, 5 µM Cytochalasin D, 30 µM Amiloride, 80 µM Dynasore, 25 µM Pitstop 2 and 1.5...