Wyniki wyszukiwania dla: RECEPTORY IMIDAZOLINOWE
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Safety and efficacy of P2X3 receptor antagonist for the treatment of refractory or unexplained chronic cough: A systematic review and meta-analysis of 11 randomized controlled trials
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Prenatal stress affects insulin-like growth factor-1 (IGF-1) level and IGF-1 receptor phosphorylation in the brain of adult rats
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The novel cannabinoid CB1 receptor neutral antagonist AM4113 suppresses ood intake and food-reinforced behavior but does not induce signs of nausea in rats
PublikacjaPrzeprowadzone badania biochemiczne wykazują, że związek AM4113 wiąże się z receptorem kanabinoidowym CB1, ale nie wykazuje właściwości odwrotnego agonisty (między innymi nie wpływa na powstawanie cyklicznego AMP). W testach na swobodne przemieszczanie się szczurów i znieczulenie związek AM4113 osłabia wpływ agonisty AM411 na receptor CB1. AM4113 wpływa na zachowanie szczurów związane z karmieniem oraz powoduje spadek łaknienia...
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Enhanced susceptibility of SARS-CoV-2 spike RBD protein assay targeted by cellular receptors ACE2 and CD147: Multivariate data analysis of multisine impedimetric response
PublikacjaSevere acute respiratory syndrome coronavirus 2 (SARS-CoV-2) enters the cells through the binding of spike protein to the host cell surface-expressing angiotensin-converting enzyme 2 (ACE2) or by endocytosis mediated by extracellular matrix metalloproteinase inducer (CD147). We present extended statistical studies of the multisine dynamic electrochemical impedance spectroscopy (DEIS) revealing interactions between Spike RBD and...
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The PolarScreen™ Estrogen Receptor Competitor Assays for determination of estradiol equivalent concentrations (EEQs) in sewage and drinking water samples.
Dane BadawczeMunicipal waste waters are one of the main sources of estrogenic compounds in aquatic environments. Feminization of fish downstream of Waste Water Treatment Plants (WWTPs) discharges has been observed worldwide. Some estrogenic chemicals, particularly steroid estrogens, are known to cause disruption of the endocrine system of fishes and abnormalities...
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Serotonergic–Muscarinic Interaction within the Prefrontal Cortex as a Novel Target to Reverse Schizophrenia-Related Cognitive Symptoms
PublikacjaRecent studies revealed that the activation of serotonergic 5-HT1A and muscarinic M1, M4, or M5 receptors prevent MK-801-induced cognitive impairments in animal models. In the present study, the effectiveness of the simultaneous activation of 5-HT1A and muscarinic receptors at preventing MK-801-induced cognitive deficits in novel object recognition (NOR) or Y-maze tests was investigated. Activators of 5-HT1A (F15599), M1 (VU0357017),...
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The PARAGON Heart Failure trial – ongoing investigation of the angiotensin receptor antagonist/neprilysin inhibitor sacubitril/valsartan in heart failure patients with hypertension and preserved ejection fraction
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Phytochemical screening and effect of Viscum album L. on monoamine oxidase A and B activity and serotonin, dopamine and serotonin receptor 5-HTR1A levels in Galleria mellonealla (Lepidoptera)
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Molecular cloning and initial characterization of African green monkey (Cercopithecus aethiops) corticotropin releasing factor receptor type 1 (CRF1) from COS-7 cells
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Influence of Estradiol-17beta on Progesterone and Estrogen Receptor mRNA Expression in Porcine Follicular Granulosa Cells during Short-Term, In Vitro Real-Time Cell Proliferation
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Efficacy and safety of B-cell receptor signaling pathway inhibitors in relapsed/refractory chronic lymphocytic leukemia: a systematic review and meta-analysis of randomized clinical trials
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Differential and Overlapping Effects of 20,23(OH)2D3 and 1,25(OH)2D3 on Gene Expression in Human Epidermal Keratinocytes: Identification of AhR as an Alternative Receptor for 20,23(OH)2D3
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Germline DNA Retention in Murine and Human Rearranged T Cell Receptor Gene Coding Joints: Alternative Recombination Signal Sequences and V(D)J Recombinase Errors
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Pregnane X receptor dependent up-regulation of CYP2C9 and CYP3A4 in tumor cells by antitumor acridine agents, C-1748 and C-1305, selectively diminished under hypoxia
PublikacjaInduction of proteins involved in drug metabolism and in drug delivery has a significant impact on drug-drug interactions and on the final therapeutic effects. Two antitumor acridine derivatives selected for present studies, C-1748 (9-(2’-hydroxyethylamino)-4-methyl-1-nitroacridine) and C-1305 (5-dimethylaminopropylamino-8-hydroxy-triazoloacridinone), expressed high and low susceptibility to metabolic transformations with liver...
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Application of Alanine Scanning to Determination of Amino Acids Essential for Peptide Adsorption at the Solid/Solution Interface and Binding to the Receptor: Surface-Enhanced Raman/Infrared Spectroscopy versus Bioactivity Assays
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In vitro biological evaluation of a novel folic acid-targeted receptor quantum dot−β−cyclodextrin carrier for C-2028 unsymmetrical bisacridine in the treatment of human lung and prostate cancers
PublikacjaTraditional small-molecule chemotherapeutics usually do not distinguish tumors from healthy tissues. However, nanotechnology creates nanocarriers that selectively deliver drugs to their site of action. This work is the next step in the development of the quantum dot−β−cyclodextrin−folic acid (QD−β−CD−FA) platform for targeted and selected delivery of C−2028 unsymmetrical bisacridine in cancer therapy.Herein, we report an initial...
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Teresa Olszewska dr hab. inż.
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(4-(Bis(4-Fluorophenyl)Methyl)Piperazin-1-yl)(Cyclohexyl)Methanone Hydrochloride (LDK1229): A New Cannabinoid CB1 Receptor Inverse Agonist from the Class of Benzhydryl Piperazine Analogs
PublikacjaSome inverse agonists of cannabinoid receptor type 1 (CB1) have been demonstrated to be anorectic antiobesity drug candidates. However, the first generation of CB1 inverse agonists, represented by rimonabant (SR141716A), otenabant, and taranabant, are centrally active, with a high level of psychiatric side effects. Hence, the discovery of CB1 inverse agonists with a chemical scaffold distinct from these holds promise for developing...
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The role of glucuronidation in drug resistance
PublikacjaThe final therapeutic effect of a drug candidate, which is directed to a specific molecular target strongly depends on its absorption, distribution, metabolism and excretion (ADME). The disruption of at least one element of ADME may result in serious drug resistance. In this work we described the role of one element of this resistance: phase II metabolism with UDP-glucuronosyltransferases (UGTs). UGT function is the transformation...
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Investigation on the behaviour of imidazolium ionic liquids in the environment
PublikacjaCiecze jonowe są solami o niskiej temperaturze topnienia, które mogą zrewolucjonizować przemysł chemiczny ponieważ w wielu przypadkach oferują zarówno ekonomiczny jak i ekologiczny zysk w porównaniu z dotychczas stosowanymi technologiami. Imidazoliowe cieczejonowe należą do najczęściej stosowanych co sprawia, że mogą stanowić źródło zanieczyszczenia środowiska glebowego i wodnego. Niektóre parametry środowiskowe (np. biodegradowalność,...
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Bioelectronic tongue: Current status and perspectives
PublikacjaIn the course of evolution, nature has endowed humans with systems for the recognition of a wide range of tastes with a sensitivity and selectivity which are indispensable for the evaluation of edibility and flavour attributes. Inspiration by a biological sense of taste has become a basis for the design of instruments, operation principles and parameters enabling to mimic the unique properties of their biological precursors. In...
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Dibutyl phthalate disrupts conserved circadian rhythm in Drosophila and human cells
PublikacjaPeople are constantly exposed to phthalates, due to their common use in the production of plastics, pharmaceuticals, cosmetics and skin care products. The ability of phthalates to disrupt endocrine signaling, leading to developmental, reproductive and metabolic defects, has been studied, yet how phthalates interfere with these biological functions is still unclear. To uncover DBP interacting molecular pathways, we raised Drosophila...
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Self-organization of imidazolium ionic liquids in aqueous solution
PublikacjaW pracy przeanalizowano i podsumowano wyniki badań nad samoorganizacją oraz tworzeniem micel cieczy jonowych w roztworach wodnych otrzymane przez wiele zespołów badawczych. Średnio i długołańcuchowe imidazoliowe ciecze jonowe wykazują aktywność powierzchniową zależną od długości łańcucha alkilowego w kationie, analogicznie do kationowych surfaktantów. Wskazano na liczne zagadnienia, które wymagają dalszych systematycznych badań
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Synthesis and properties of new 'N,'N-phenyltetrazole podand
PublikacjaThe synthesis of a new chromogenic N,N-phenyltetrazole receptor is reported here. The cationbinding properties of this receptor in solution were investigated by naked-eye colour change, electrochemical methods and UV-Vis spectroscopy in various solvents (CH3CN, dimethylsulphoxide (DMSO), DMSO/H2O, CH3CN/H2O and CH3CN/MeOH). In addition, the receptor was used as a sensing material in ion-selective membrane electrodes. The selectivity...
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Wyznaczanie współczynników dyfuzji tlenku węgla (IV) przez membrany wysycone cieczą jonową = Determination of carbon dioxide diffusion coefficients in supported ionic liquids membranes
PublikacjaWykazano możliwość zastosowania imidazoliowych cieczy jonowych osadzonych na nośnikach polimerowych SILM (supported ionic liquids membranes) do absorpcji CO2. W badaniach wykorzystano sole imidazoliowe posiadające w strukturze aniony fluoroalkilowe typu [Tf2N] i [TfO], które selektywnie separują tlenek węgla (IV). Wyznaczono współczynniki dyfuzji CO2 przez poszczególne SILM na podstawie ilości dyfundującego CO2 przez powierzchnię...
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Zastosowanie unieruchomionych ciekłych membran z cieczami jonowymi w procesach separacji CO2
PublikacjaPrzedmiotem pracy jest efektywność przenikania CO2 i CH4 przez ciekłe membrany z cieczami jonowymi osadzonymi na nośnika polimerowych. Jako fazę membranową zastosowano imidazoliowe ciecz jonowe będące kombinacją kationu o różnej długości podstawnika alkilowego oraz różnych anionów [Tf2N][, [TfO],[BF4] i [PF6]. Porównano szybkość permeacji obu gazów w układzie laboratoryjnym, gdzie powierzchnia membrany wynosiła 13cm2.
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Bioelectronic nose: Current status and perspectives
PublikacjaA characteristic feature of human and animal organs of smell is the ability to identify hundreds of thousands of odours. It is accompanied by particular smell sensations, which are a basic source of information about odour mixture. The main structural elements of biological smell systems are the olfactory receptors. Small differences in a structure of odorous molecules (odorants) can lead to significant change of odour, which is...
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Selective transport of Pb(II) across polymer inclusion membrane using imidazole azocrown ethers as carriers.
PublikacjaZbadano selektywność transportu jonów ołowiu(II) z równomolowych roztworów jonów Zn(II), Cd(II) i Pb(II) przez polimerowe membrany inkluzyjne (PIM) zawierające imidazolowe etery azokoronowe.Wykazano, że polimerowe membrany inkluzyjne z imidazolowymi azokoronami wykazują dużą stabilność, zależną w dużym stopniu od rodzaju jonoforu.
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Elżbieta Luboch prof. dr hab. inż.
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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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Badania możliwości wykorzystania cieczy jonowych w procesach oczyszczania biogazu
PublikacjaCelem pracy było lepsze zrozumienie mechanizmu przenikania metanu i tlenku węgla(IV) przez imidazoliowe, amoniowe oraz fosfoniowe ciecze jonowe osadzone na nośniku polimerowym, jak również opracowanie nowych procedur badawczych, przygotowania i użycia immobilizowanych membran ciekłych w procesach separacji gazów. Przeprowadzono badania przenikanie CO2 oraz CH4 przez ciecz jonowe unieruchomione w porach porowatego nośnika polimerowego...
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The estrogenicity of wastewater samples.
Dane BadawczeThe principle of operation of the kit is based on the fact that the tested sample with endocrine activity (containing compounds capable of binding to the human estrogen receptor α, hERα) releases the fluorescently labeled ligand (FluormoneTM ES2) from the receptor-ligand complex, which results in a reduction of the polarization value fluorescence. The...
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Adolfo Poma
OsobyDr. Adolfo Poma (see my biosketch) is the group leader of the Multiscale Modelling of Complex Systems divison. In 2008, he got a MSc. degree in computational physics from the State University of Campinas (Brazil). Then he moved to Germany and under the supervision of Prof. Kurt Kremer (head of the polymer theory group, Max Planck Institute for Polymer Research) and Prof. Luigi Delle Site (Frei University of Berlin) got a PhD degree...
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Biologically active compounds based on the carbazole scaffold - synthetic and mechanistic aspects
PublikacjaDoctoral dissertation is divided into three main parts: introduction, results and discussion and experimental. The introduction is divided into four main parts which describe: 5-hydroxytryptamine receptors, the most popular antidepressants, new compounds based on the carbazole structure with affinity for serotonin receptors, telomeres and telomerase with their functions, telomerase inhibition strategies, carbazoles approved in...
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Lysophosphatidic acid signaling in ovarian cancer
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Structure-function analysis of decay-accelerating factor: identification ofresidues important for binding of the Escherichia coli Dr adhesin and complement regulation
PublikacjaZidentyfikowano ważne dla wiązania adhezyny Dr uropatogennych Escherichiacoli reszty aminokwasowe w ludzkim receptorze DAF SCR-3.
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Predicting the critical micelle concentration of aqueous solutions of ionic liquids and other ionic surfactants
PublikacjaNiektóre ciecze jonowe, szczególnie te będące kombinacją organicznego i nieorganicznego jonu, wykazują strukturalne podobieństwo do surfaktantów. Krytyczne stężenie micelizacji jest podstawowym parametrem w chemii powierzchni i nauce o koloidach. Parametr ten został zmierzony dla wielu cieczy jonowych, jednakże ze względu na ogromną ilość możliwych kombinacji anionów i kationów jego eksperymentalny pomiar dla wszystkich struktur...
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Neurochemical changes underlying cognitive impairment in olfactory bulbectomized rats and the impact of the mGlu5-positive allosteric modulator CDPPB
PublikacjaThe olfactory bulbectomized (OBX) rat model is a well-established model of depression in which antidepressant drugs reverse deficits in the passive avoidance test 14 days after administration. Recently, the olfactory bulbectomized rat model has been proposed to be a model of Alzheimer’s disease (AD), and the available data indicate similarities between the changes that typically occur in AD and those observed in OBX animals. In...
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The potential role of bisphenol A in the pathogenesis of polycystic ovary syndrome
PublikacjaPolycystic ovary syndrome (PCOS) is the most common endocrinopathy in women of reproductive age, that lead to infertility, type 2 diabetes and coronary heart disease. Bisphenol A (BPA) is one of the most abundant chemicals produced worldwide and is used as a plasticizer in daily life. Nowadays it is also well know that it can interact with estrogen receptors, androgen receptors and peroxisome proliferatoractivated receptors g (PPARg)....
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Low-volume label-free SARS-CoV-2 detection with the microcavity-based optical fiber sensor
PublikacjaAccurate and fast detection of viruses is crucial for controlling outbreaks of many diseases; therefore, to date, numerous sensing systems for their detection have been studied. On top of the performance of these sensing systems, the availability of biorecognition elements specific to especially the new etiological agents is an additional fundamental challenge. Therefore, besides high sensitivity and selectivity, such advantages...
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Highly Conserved Homotrimer Cavity Formed by the SARS-CoV-2 Spike Glycoprotein: A Novel Binding Site
PublikacjaAn important stage in severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) life cycle is the binding of the spike (S) protein to the angiotensin converting enzyme-2 (ACE2) host cell receptor. Therefore, to explore conserved features in spike protein dynamics and to identify potentially novel regions for drugging, we measured spike protein variability derived from 791 viral genomes and studied its properties by molecular...
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Mieszanki betonowe stosowane w technologii druku trójwymiarowego
PublikacjaW niniejszej pracy dokonano przeglądu literatury z zakresu mieszanek i zapraw betonowych stosowanych w druku trójwymiarowym. Przegląd literatury przygotowano z zachowaniem chronologii pojawienia się danej publikacji (daty publikacji). Na podstawie przeprowadzonego przeglądu dokonano tabelarycznego zestawienia receptur mieszanek wykorzystywanych w wydrukach trójwymiarowych (3D). Przedstawiony przegląd literatury z zakresu mieszanek...
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Malignant neoplasm of breast - Female, 55 - Tissue image [2270630026302991]
Dane BadawczeThis is the histopathological image of BREAST tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.
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Malignant neoplasm of breast - Female, 39 - Tissue image [2270630026302791]
Dane BadawczeThis is the histopathological image of BREAST tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.
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Malignant neoplasm of breast - Female, 55 - Tissue image [2270630026303201]
Dane BadawczeThis is the histopathological image of BREAST tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.
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Malignant neoplasm of breast - Female, 39 - Tissue image [2270630026307301]
Dane BadawczeThis is the histopathological image of BREAST tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.
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Malignant neoplasm of breast - Female, 54 - Tissue image [2270630026304381]
Dane BadawczeThis is the histopathological image of BREAST tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.
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Malignant neoplasm of breast - Female, 54 - Tissue image [2270630026305081]
Dane BadawczeThis is the histopathological image of BREAST tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.
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Malignant neoplasm of breast - Female, 39 - Tissue image [2270630026301541]
Dane BadawczeThis is the histopathological image of BREAST tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.
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Malignant neoplasm of breast - Female, 54 - Tissue image [227063002630101]
Dane BadawczeThis is the histopathological image of BREAST tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.