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Search results for: DRUG IMPURITIES
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Molecular mechanism of proton-coupled ligand translocation by the bacterial efflux pump EmrE
PublicationThe current surge in bacterial multi-drug resistance (MDR) is one of the largest challenges to public health, threatening to render ineffective many therapies we rely on for treatment of serious infections. Understanding different factors that contribute to MDR is hence crucial from the global “one health” perspective. In this contribution, we focus on the prototypical broad-selectivity proton-coupled antiporter EmrE, one of the...
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Foliate-Targeting Quantum Dots-β-Cyclodextrin Nanocarrier for Efficient Delivery of Unsymmetrical Bisacridines to Lung and Prostate Cancer Cells
PublicationTargeted drug delivery by nanocarriers molecules can increase the efficiency of cancer treatment. One of the targeting ligands is folic acid (FA), which has a high affinity for the folic acid receptors, which are overexpressed in many cancers. Herein, we describe the preparation of the nanoconjugates containing quantum dots (QDs) and β-cyclodextrin (β-CD) with foliate-targeting properties for the delivery of anticancer compound...
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Organic solvents aggregating and shaping structural folding of protein, a case study of the protease enzyme
PublicationLow solubility of reactants or products in aqueous solutions can result in the enzymatic catalytic reactions that can occur in non-aqueous solutions. In current study we investigated aqueous solutions containing different organic solvents / deep eutectic solvents (DESs) that can influence the protease enzyme's activity, structural, and thermal stabilities. Retroviral aspartic protease enzyme is responsible for the cleavage of the...
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Marcin Stienss dr inż.
PeopleMarcin Stienss (urodzony w 1982 r. w Malborku) specjalizuje się w tematyce infrastruktury drogowej. Jego główne obszary badawcze dotyczą mieszanek mineralno-asfaltowych, badań i diagnostyki nawierzchni oraz szeroko pojętego procesu projektowania dróg. W roku 2006 roku uzyskał na Wydziale Inżynierii Lądowej i Środowiska Politechniki Gdańskiej stopień magistra inżyniera na kierunku Budownictwo Lądowe w specjalności Inżynieria Transportowa,...
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A System for Cooling Electronic Elements with EHD Coolant Flow
PublicationA system for cooling electronic components where the liquid coolant flow is forced with ion-drag type EHD micropumps was tested.
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Zur Ahnlichkeit der Drill- und Biegetrager-Formeln fur dunnwandige Stabe - Stellungsnahme zur Zuschrift.
PublicationPrzedstawiono stanowisko odnośnie uwag dyskutanta, stwierdzające możliwości przyjęcia różnych dróg przejścia granicznego w analizie problemu.
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Projektowanie Dróg i Autostrad - (Budownictwo, 1 st., 6. sem., 2021-2022) - Przedmiot obieralny
e-Learning CoursesKurs przeznaczony dla studentów I stopnia studiów dziennych na kierunku Budownictwo, którzy wybrali przedmiot obieralny "Projektowanie Dróg i Autostrad".
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Projektowanie Dróg i Autostrad - (Budownictwo, 1 st., 6. sem., 2022-2023) - Przedmiot obieralny
e-Learning CoursesKurs przeznaczony dla studentów I stopnia studiów dziennych na kierunku Budownictwo, którzy wybrali przedmiot obieralny "Projektowanie Dróg i Autostrad".
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Projektowanie Dróg i Autostrad - (Budownictwo, 1 st., 6. sem., 2023-2024) - Przedmiot obieralny
e-Learning CoursesKurs przeznaczony dla studentów I stopnia studiów dziennych na kierunku Budownictwo, którzy wybrali przedmiot obieralny "Projektowanie Dróg i Autostrad".
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Mesh dependence study for numerical assessment of hydrodynamic characteristics of windsurfing fin
PublicationThe presented research aims to assess the drag coefficient and lift coefficient versus angle of attack curves for windsurfing fin. Special attention in the research was being paid to the evaluation of the stall angle value. The angle of incidence for which the stall occurs was searched, and the sensitivity of the solution for the mesh resolution was studied. The mesh resolution sensitivity analysis was done by systematically decreasing...
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Effects of Addictive Substances During Pregnancy and Infancy and Their Analysis in Biological Materials
PublicationThe use of addictive substances during pregnancy is a serious social problem, not only because of effects on the health of the woman and child, but also because drug or alcohol dependency it detracts from childcare and enhances the prospect of child neglect and family breakdown. Developing additive substance abuse treatment programs for pregnant women is socially important and can help ensure the health of babies, prevent subsequent...
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Projektowanie technologii wzmocnień nawierzchni ulic
PublicationMetody obliczania obciążenia dróg ruchem.Ocena stanu istniejącej nawierzchni. Przyjęcie technologii napraw ulic. Obliczenia wzmocnień konstrukcji nawierzchni.
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Tailoring the electrochemical degradation of iron protected with polypyrrole films for biodegradable cardiovascular stents
PublicationThe degradation of polypyrrole (PPy) coated iron is studied in phosphate buffer saline solution at 37 °C by odd random phase multisine electrochemical impedance spectroscopy (ORP-EIS). PPy is electropolymerized with anti-inflammatory salicylates incorporated in the film, as a drug release system. The modelling of EIS over time provides the quantitative description of the corrosion behaviour of the material. Thus, the reliable...
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Diagnostyka i niezawodność dróg szynowych 2023/24
e-Learning CoursesKurs diagnostyka i niezawodność dróg szynowych prowadzony jest w ramach specjalności drogi szynowe na studiach II stopnia na kierunku budownictwo
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Diagnostyka i niezawodność dróg szynowych 2022/23
e-Learning CoursesKurs diagnostyka i niezawodność dróg szynowych prowadzony jest w ramach specjalności drogi szynowe na studiach II stopnia na kierunku budownictwo
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Wody opadowe - aspekty prawne, ekonomiczne i techniczne
PublicationProblemy zagospodarowania wód opadowych. Zagadnienia formalne i techniczne, trudności, poszukiwanie dróg rozwiązania. Konflikty. Rezultaty branżowego spotkania włocławskiego.
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Badanie znaczenia atrybutów bazy wiedzy.
PublicationW pracy przedstawiono dwie metody umożliwiające wyznaczanie miary znaczenia wybranych atrybutów bazy wiedzy. W pierwszej metodzie wykorzystano teorię zbiorów przybliżonych i podano definicje miary znaczenia atrybutów oparte na liczbie reguł sprzecznych. Druga metoda wykorzystująca teorię zbiorów rozmytych pozawala na zdefiniowanie dwóch sposobów oceny miary znaczenia. Pierwsza miara opiera się na liczbie reguł sprzecznych,...
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ANALIZA PORÓWNAWCZA METOD WYZNACZANIA SZEROKOŚCI PASA RUCHU STATKU ŚRÓDLĄDOWEGO
PublicationŻegluga śródlądowa w Polsce stanowi niewykorzystany potencjał. Możliwości przewozowe jakie posiadają rzeki są olbrzymie. Kluczowy problem stanowią parametry eksploatacyjne poszczególnych odcinków, które w znacznym stopniu ograniczają żeglowność szlaku. W związku z powyższym istotnego znaczenia nabiera wyznaczanie parametrów eksploatacyjnych śródlądowych dróg wodnych. W artykule dokonano charakterystyki śródlądowych dróg w Polsce....
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Cele, koncepcja i założenia Krajowego Systemu Zarządzania Ruchem
PublicationW pracy przedstawiono historię prac zmierzających do opracowania jednolitego standardu FRAME. Opisano założenia i cele Krajowego Systemu Zarządzania Ruchem. Przedstawiono 17 modułów wdrożeniowych, które będą wdrażane na drogach sieci TEN-T, sieci dróg krajowych nie należących do tej sieci i na nowo - budowanych odcinkach dróg, w zakresie kontraktów budowlanych. W artykule przedstawiono obszary funkcjonalne KSZR i bazy danych, które...
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Design and characteristics of gellan gum beads for modified release of meloxicam
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Aryl- and heteroaryl-substituted phenylalanines as AMPA receptor ligands
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Short Term Monitor of Photodegradation Processes in Ranitidine Hydrochloride Observed by FTIR and ATR FTIR
PublicationThe effects of degradation of ranitidine hydrochloride exposed to UVB radiation (l = 310 nm) and oxygen in a weathering chamber were studied by Fourier Transform Infrared spectroscopy (FTIR) and Attenuated Total Reflectance Fourier Transform Infrared spectroscopy (ATR-FTIR). ATR-FTIR profile indicated that the degradation was spatially heterogeneous. Significant amounts of photoproducts were detected only in a directly...
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CDK9: Therapeutic Perspective in HCC Therapy
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Current Challenges in Targeting Tumor Desmoplasia to Improve the Efficacy of Immunotherapy
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Investigating the disease‐modifying properties of sclerotiorin in Alzheimer's therapy using acetylcholinesterase inhibition
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Current state of a dual behaviour of antimicrobial peptides-Therapeutic agents and promising delivery vectors
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The Chemometric Evaluation of Antitumor Activity of Novel Benzensulfonamide Derivatives Based on their Physiochemical Properties
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QSAR Analysis of Compounds Exhibiting General Anesthetics’ Properties
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QSAR Analysis of Selected Antimicrobial Structures Belonging to Nitro-derivatives of Heterocyclic Compounds
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Differential scanning calorimetry for authentication of edible fats and oils - What can we learn from the past to face the current challenges?
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Conformational Preferences of Proline Derivatives Incorporated into Vasopressin Analogues: NMR and Molecular Modelling Studies
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Highly Potent Antidiuretic Antagonists: Conformational Studies of Vasopressin Analogues Modified with 1-Naphthylalanine Enantiomers at Position 2
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Structure–activity relationships study on biological activity of peptides as dipeptidyl peptidase IV inhibitors by chemometric modeling
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Preliminary antifungal activity assay of selected chlorine-containing derivatives of xanthone and phenoxyethyl amines
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Simplified, serine‐rich theta‐defensin analogues as antitumour peptides
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Solubility advantage of sulfanilamide and sulfacetamide in natural deep eutectic systems: experimental and theoretical investigations
PublicationObjective: The aim of this study was to explore the possibility of using natural deep eutectic solvents (NADES) as solvation media for enhancement of solubility of sulfonamides, as well as gaining some thermodynamic characteristics of the analyzed systems. Significance: Low solubility of many active pharmaceutical ingredients is a well-recognized difficulty in pharmaceutical industry, hence the need for different strategies addressing...
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Synthesis and biological evaluation of N-acylated tyramine sulfamates containing C-F bonds as steroid sulfatase inhibitors
PublicationSteroid sulfatase (STS) is responsible for the hydrolysis of biologically inactive sulfated steroids into their active un-sulfated forms and promotes the growth of various hormone-dependent cancers (e.g., breast cancer). Therefore, the STS enzyme is a promising therapeutic target for the treatment of steroid-sensitive cancers. Herein, we report the synthesis and biological evaluation of sulfamate analogs as potential STS inhibitors...
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Novel anticancer strategy aimed at targeting shelterin complexes by the induction of structural changes in telomeric DNA: hitting two birds with one stone.
PublicationThe ends of chromosomes in mammals are composed of telomeric DNA containing TTAGGG repeats, which bind specific proteins called shelterins. This telomeric DNA together with shelterins form a cap that protects the ends of chromosomes from being recognized as sites of DNA damage and from chromosomal fusions. Many very successful antitumor drugs used in the treatment of cancer patients bind to DNA, some of them with a prominent sequence...
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Structural Factors Affecting Cytotoxic Activity of (E)-1-(Benzo[d ][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one Derivatives
PublicationDerivatives of (E)-1-(5-alkoxybenzo[d][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one (1) demonstrated exceptionally high in vitro cytotoxic activity, with IC50 values of the most active derivatives in the nanomolar range. To identify structural fragments necessary for the activity, several analogs deprived of selected fragments were prepared, and their cytotoxic activity was tested. It was found that the activity depends on combined effects...
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Effects of an immunosuppressive treatment on the rat prostate
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Influence of S-Oxidation on Cytotoxic Activity of Oxathiole-Fused Chalcones
PublicationSynthesis, in vitro cytotoxic activity, and interaction with tubulin of oxidized, isomeric 1-(5-alkoxybenzo[d] [1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-ones and 1-(6- alkoxybenzo[d][1,3]oxathiol-5-yl)-3-phenylprop-2-en-1- ones are described. Most of the compounds demonstrated cytotoxic activity at submicromolar concentrations. It was found that oxidation of sulfur atom of the oxathiole-fused chalcones strongly influenced activity...
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Synthesis and biological evaluation of fluorinated 3-phenylcoumarin-7-O-sulfamate derivatives as steroid sulfatase inhibitors
PublicationIn the present work, we report the initial results of our study on a series of 3-phenylcoumarin sulfamate-based compounds containing C-F bonds as a novel inhibitors of steroid sulfatase (STS). The new compounds are potent STS inhibitors, possessing more than 10 times higher inhibitory potency than coumarin-7-O-sulfamate. In the course of our investigation, compounds 2b and 2c demonstrated the highest inhibitory effect in the enzymatic...
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Debata społeczna "Gospodarka wodna w Poznaniu"
PublicationPrezentacja rezultatów przeprowadzonej w Poznaniu publicznej debaty o wodzie. Przykład współpracy z ludnością - jedna z dróg poszukiwania ''najlepszej praktyki''.
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Wzmacnianie gruntu in situ metodą wgłębnego mieszania.
PublicationOpisano technologie mieszania wgłębnego na sucho i mokro. Przedstawiono przykłady zastosowania przy budowie dróg w Polsce na słabym podłożu.
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Synthesis and biological activity of ester derivatives of mycophenolic acid and acridines/acridones as potential immunosuppressive agents
PublicationImproved derivatives of mycophenolic acid (MPA) are necessary to reduce the frequency of adverse effects, this drug exerts in treated patients. In this study, MPA was coupled with N-(x-hydroxyalkyl)-9-acridone-4-carboxamides or N-(x-hydroxyalkyl)acridine-4-carboxamides to give respective ester conjugates upon Yamaguchi protocol. This esterification required protection of phenol group in MPA. Designed conjugates revealed higher...
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Dietary intervention with beetroot juice during doxorubicin cancer chemotherapy in vivo reduces markers of oxidative stress
PublicationCancer chemotherapy with doxorubicin, despite high antitumor activity and broad spectrum of this drug, is on decline due to toxic side effects. The clinical efficacy of anthracyclines have continuously prompted the search for new adjuvants to alleviate undesirable side toxicity incurred by this group of cytostatics. The recent approaches involve the application of synthetic or purified natural antioxidants in combination with doxorubicin...
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The influence of food phytochemicals on cyclic phosphodiesterase 4 (PDE4) activity
PublicationCyclic phosphodiesterase 4 (PDE4) belongs to family of cyclic phosphodiesterases, which are expressed predominantly in inflammatory cells, airway smooth muscles, cardiovascular tissues and brain. Inhibitors of this family of enzymes found medicinal applications as antidepressants, antiinflamatory drugs (mainly in airway diseases) or antiasthmatics (Ibudilast). PDE4 inhibitors are also being tested for preventing the development...
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Prenatal exposure to substance of abuse: A worldwide problem
PublicationSubstance abuse during pregnancy is an important public health issue affecting the mother and the growing infant. Preterm labor, miscarriage, abruption and postpartum hemorrhage are obstetric complications which have been associated with women who are dependent on abused substances. Moreover, women are also at an increased risk of medical problems such as poor nutrition, anemia, urinary tract infections as well as sexually transmitted...
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Mass spectrometry based identification of geometric isomers during metabolic stability study of a new cytotoxic sulfonamide derivatives supported by quantitative structure-retention relationships
PublicationA set of 15 new sulphonamide derivatives, presenting antitumor activity have been subjected to a metabolic stability study. The results showed that besides products of biotransformation, some additional peaks occurred in chromatograms. Tandem mass spectrometry revealed the same mass and fragmentation pathway, suggesting that geometric isomerization occurred. Thus, to support this hypothesis, quantitative structure-retention relationships...
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Targeting of FLT3-ITD kinase contributes to high selectivity of imidazoacridinone C-1311 against FLT3-activated leukemia cells
PublicationDrugs targeting receptor tyrosine kinase FLT3 are of particular interest since activating FLT3-internal tandem duplication (ITD) mutations abundantly occur in fatal acute myeloid leukemias (AMLs). Imidazoacridinone C-1311, a DNA-reactive inhibitor of topoisomerase II, has been previously shown to be a potent and selective inhibitor of recombinant FLT3. Here, we expand those findings by studying its effect on leukemia cells with...