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Search results for: ESTROGEN RECEPTOR-BENZO[B]NAPHTHO[1
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Towards β-selectivity in functional estrogen receptor antagonists
PublicationBased on the benzo[b]naphtho[1,2-d]furan and benzo[b]naphtho[1,2-d]thiophene frameworks, a series of ligands with different basic side chains (BSCs) has been synthesized and pharmacologically evaluated. Also, their binding modes have been modelled using docking techniques. It was found that the introduction of a BSC in these systems brings about a decrease of affinity for both estrogen receptors α and β in an in vitro competitive...
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Phosphate tricyclic coumarin analogs as steroid sulfatase inhibitors: synthesis and biological activity.
PublicationIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate tricyclic coumarin derivatives as potential steroid sulfatase inhibitors. The described synthesis includes the straightforward preparation of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c]chromen-6-one modified...
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New clicked full agonists of the estrogen receptor β
PublicationA click chemistry approach was used to synthesize a series of 1,4-diaryl-substituted 1,2,3-triazoles designed to behave as estrogen receptor (ER) ligands. We studied their affinities for both receptors α and β, their agonist activities in a cell-based luciferase reporter assay and their effect on the proliferation of the hormone-dependent MCF-7 cell line. We found two compounds (3a and 3c) that behave as selective full agonists...
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Estrogen receptor 2 polymorphism in idiopathic scoliosis
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Replication study of estrogen receptor 1 XbaI polymorphism in adolescent idiopathic scoliosis (AIS) Caucasian population
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Estrogen Receptor 2 Gene Polymorphism in Idiopathic Scoliosis
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XbaI and PvuII Polymorphisms of Estrogen Receptor 1 Gene in Females with Idiopathic Scoliosis: No Association with Occurrence or Clinical Form
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Methylation level of the regulatory regions of the estrogen receptor type 1 gene in paravertebral muscles of girls with idiopathic scoliosis
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Methylation of Estrogen Receptor 1 Gene in the Paraspinal Muscles of Girls with Idiopathic Scoliosis and Its Association with Disease Severity
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Optimization of Chemical Functionalities of Indole-2-carboxamides To Improve Allosteric Parameters for the Cannabinoid Receptor 1 (CB1)
Publication5-Chloro-3-ethyl-N-(4-(piperidin-1-yl)phenethyl)-1H-indole-2-carboxamide (1; ORG27569) is a prototypical allosteric modulator for the cannabinoid type 1 receptor (CB1). Here, we reveal key structural requirements of indole-2-carboxamides for allosteric modulation of CB1: a critical chain length at the C3-position, an electron withdrawing group at the C5-position, the length of the linker between the amide bond and the phenyl ring...
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Oxidative stress induced by 4-methyl-1-nitroacridine derivative C-1748 (Capridine B) in human colon cancer cells
PublicationZbadano wpływ pochodnej C-1748 (Capridine B) na indukcję stresu oksydacyjnego w komórkach ludzkich raków jelita grubego HCT-8 i HT29. W tym celu wykorzystano technikę cytometrii przepływowej z zastosowaniem barwników fluorescencyjnych H2DCFDA i DHR 123. W komórkach traktowanych pochodną C-1748 dochodziło do generowania reaktywnych form tlenu. Ponadto, pochodna C-1748 nie indukowała znaczącego spadku zawartości zredukowanej formy...
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Estrogen Receptor Type 1 and Type 2 Presence in Paravertebral Skeletal Muscles: Expression Level and Relation to Phenotype in Children with Idiopathic Scoliosis
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Expression of Estrogen Receptor Coactivator Proline-, Glutamic Acid- and Leucine-Rich Protein 1 within Paraspinal Muscles in Adolescents with Idiopathic Scoliosis
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Rozstaw rys według PN-EN 1992-1-1:2008 oraz PN-B 03264:2002
PublicationW pracy opisano mechanizm powstawania rys dla osiowo rozciąganego pręta żelbetowego. Na tej podstawie określono maksymalny i minimalny rozstaw rys, konfrontując otrzymane wyniki z procedurami podanymi w normie europejskiej PN-EN 1992-1-1:2008 oraz w normie polskiej PN-B 03264:2002. Przedstawiono praktyczne wnioski do projektowania, wynikajace z przeprowadzonej analizy.
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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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Methylation of estrogen receptor 2 (ESR2) in deep paravertebral muscles and its association with idiopathic scoliosis
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N-(1-Piperidinepropionyl)amphotericin B methyl ester (PAME) - a new derivative of the antifungal antibiotic amphotericin B: Searching for the mechanism of its reduced
PublicationZ zastosowaniem techniki monowarstw Langmuira zbadano naturę oddziaływań pochodnej antybiotyku przeciwgrzybowego amfoterycyny B o obniżonej toksyczności tj. estru metylowego N-(1-piperydynopropionylo)amfoterycyny B (PAME) z komponentami błon biologicznych takich jak: ergosterol, cholesterol i modelowy fosfolipid DPPC i stwierdzono, że zróżnicowanie tych oddziaływań jest podstawą obniżonej toksyczności związku.
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Naphtho[1′,2′:4,5]imidazo[1,2-a]pyridine-5,6-diones: Synthesis, enzymatic reduction and cytotoxic activity
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Estrogen receptors 1 and 2 genotypes and age at menarche in idiopathic scoliosis
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Synthesis of disubstituted 1,3,4,9-tetrahydropyrano-[3,4-b]indole-1-acetic acids derivatives
Publication1,3,4,9-tetrahydropyrano[3,4-b ]indole-1-acetic acid derivatives are of interest for pharmaceutical research as a core structure for synthesis of biological active substance - Etodolac (selective Cyclooxygenase-2 inhibitor, which belongs to the Non-steroidal Anti-inflammatory Drug, NSAID, that shows a clin-ically effective analgesic and anti-inflammatory activity). Here the way of synthesis of two 1,3,4,9-tetrahydropyrano[3,4-b...
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Szerokość rozwarcia rys w konstrukcjach żelbetowych według PN-EN 1992-1-1:2008 oraz PN-B 03264:2002
PublicationW referacie przedstawiono zalecenia normowe związane z ograniczeniem szerokości rozwarcia rys w konstrukcjach żelbetowych. Przeanalizowano wytyczne projektowe podane w PN-EN 1992-1-1:2008 [1] oraz PN-B 03264:2002 [2]. W przykładzie obliczeniowym dołączonym do referatu sprawdzono rozwarcie rys w płycie żelbetowej pod obciążeniem długotrwałym dla różnych wariantów: obliczeń elementu według założeń PN-EN 1992-1-1:2008 – m. in. z...
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Szerokość rozwarcia rys w konstrukcjach żelbetowych według PN-EN 1992-1-1:2008 oraz PN-B 03264:2002
PublicationW referacie przedstawiono zalecenia normowe związane z ograniczeniem szerokości rozwarcia rys w konstrukcjach żelbetowych. Przeanalizowano wytyczne projektowe podane w PN-EN 1992-1-1:2008 [1] oraz PN-B 03264:2002 [2]. W przykładzie obliczeniowym dołączonym do referatu sprawdzono rozwarcie rys w płycie żelbetowej pod obciążeniem długotrwałym dla różnych wariantów: obliczeń elementu według założeń PN-EN 1992-1-1:2008 – m. in. z...
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Targeting melanocortin receptor type 1 with small peptides
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Mechanism of Isomerization and Acid-Induced Transformations of 3-Hydroxy-4,4'-dimethoxy-3'-methyl-3-oxo-7,7'-bis(piperidino-carbonyloxy)-2,2'-spirobi-[2H,2'H,3H,3'H-benzo[b]thiophene]. Unusual Equilibrium between the Spiro and 3-Hydroxy-benzothiophene Systems.
PublicationStwierdzono, że 3'-hydroksy-4,4'-dimetoksy-3'-metylo-3-okso-7,7'-bis(piperydynokarbonyloksy)-2,2'-spirobi[2H,2'H,3H,3'H-benzo[b]tiofen] występuje w roztworach postaci mieszaniny dwóch diastereoizomerów pozostających w dynamicznej równowadze. Mechanizm tej równowagi oparty jest na odwracalnym otwarciu pierścienia z 1,5 przeniesieniem protonu i utworzeniu przjściowej formy 3-hydroksybenzotiofenu.
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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
PublicationSome 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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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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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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Ambulatory Blood Pressure Adds to Explaining Benefits of AT‐1 Receptor Blockade in the Treatment of Left Ventricular Hypertrophy
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Docking is not enough: 17-trifluoromethylphenyl trinor PGF2α is only a very weak ligand of neurokinin-1 receptor
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Correcting a widespread error: Neuroprotectant N-acetyl-L-tryptophan does not bind to the neurokinin-1 receptor
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Efficacy of high-dose corticosteroid-based treatment for chronic lymphocytic leukemia patients with p53 abnormalities in the era of B-cell receptor inhibitors
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Radiochemical Synthesis and Evaluation of Novel Radioconjugates of Neurokinin 1 Receptor Antagonist Aprepitant Dedicated for NK1R-Positive Tumors
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Ocena wskaźnika wykorzystania nośności wybranych elementów stalowej konstrukcji wiaty wg PN-90/B-03200 i PN-EN 1993-1-1
PublicationPrzedstawiono wyniki analizy nośności wybranych elementów konstrukcji stalowej, z uwzględnieniem przepisów normy polskiej i Eurokodu 3 oraz obciążenia śniegiem wg normy PN-80/B-0210 i jej zmian z 2006 roku. Wyrażono pogląd o potrzebie opracowania wytycznych dotyczących postępowania w przypadku oceny nośności obiektów eksploatowanych.
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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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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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Transcriptomic Effects of Estrogen Starvation and Induction in the MCF7 Cells. The Meta-analysis of Microarray Results
PublicationEstrogen is one of the most important signaling molecules which targets a number of genes. Estrogen levels regulate cell proliferation and a plethora of metabolic processes, which may interfere with a range of medical conditions and drug metabolism. The MCF7 breast cancer cell line, expressing the estrogen receptor α, is a well-studied model of cellular answer to estrogen. The aim of this study was to characterize transcriptomic...
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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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Comparative field test for measurement of PM10 dust in atmospheric air using gravimetric (reference) method and b-absorption method (Eberline FH 62-1)
PublicationThe paper presents the results of a field test carried out in Gdansk region between 01-01-2010 and 31-12-2010 in order to demonstrate equivalence of the Eberline FH 62-1 sampler to the reference gravimetric method of suspended PM10 dust measurement. The differences in PM10 dust concentration provided by both methods have been discussed for different seasons of the year. A method of estimation of the correction factors/correction...
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Spectrofluorometrical Determination of Vitamin B 1 in Different Matrices Using Box‐Behnken Designed Pipette Tip Solid Phase Extraction by a Carbon Nanotube Sorbent
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Luminescent properties of Tb and Eu activated AxB1-xAlO3 (A = Y, Lu, Gd; B = Lu; x = 0, 0.5, 1) mixed oxides crystals prepared by micro-pulling-down method
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Karaś P., Kochanowicz K., Pitek M., Domański P., Obuchowski I., Tomiczek B., Liberek K.: Evolution towards simplicity in bacterial small heat shock protein system// eLife -, (2023), s.1-21
PublicationEvolution can tinker with multi-protein machines and replace them with simpler single-protein systems performing equivalent functions in an equally efficient manner. It is unclear how, on a molecular level, such simplification can arise. With ancestral reconstruction and biochemical analysis, we have traced the evolution of bacterial small heat shock proteins (sHsp), which help to refold proteins from aggregates using either...
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Idea zastosowania sztucznej inteligencji w prognozowaniu wpływu drgań komunikacyjnych na odpowiedź dynamiczną budynków mieszkalnych
PublicationW poniższym artykule autorzy analizują wpływ drgań komunikacyjnych na budynki mieszkalne oraz metodykę pomiarową według PN-85 B-02170 [1]. Problemem badawczym jest opracowanie prostej metody prognozowania wpływu drgań na budynki mieszkalne w taki sposób, aby nie było konieczne przeprowadzanie pracochłonnych i kosztownych pomiarów polowych. W tym celu wykonano analizę przy użyciu algorytmów opartych na sztucznej inteligencji oraz...
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Comparison of PCBs and PAHs levels in European coastal waters using mussels from the Mytilus edulis complex as biomonitors
PublicationMussels from the Mytilus edulis complex were used as biomonitors for two groups of organic pollutants: polychlorinated biphenyls (PCBs, congeners: 28, 52, 101, 118, 138, 153 and 180) and polycyclic aromatic hydrocarbons (PAHs, naphthalene, acenaphthylene, acenaphthene, fluorene, phenanthrene, anthracene, fluoranthene, pyrene, benz(a)anthracene, chrysene, benzo(b)fluoranthene, benzo(k)fluoranthene, benzo(a)pyrene, indeno(1,2,3-cd)pyrene,...
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Selective detection of F- by chromogenic tetrazole receptor
PublicationA chromogenic anion host 4, containing two amide functionalities linked to azo dye and tetrazole rings was synthesized and its complexes with various anions were investigated. The results show that receptor 4 can recognize selectively biologically important F- ion. The binding affinity for F- was investigated by naked-eye colour change, UV-Vis and 1H NMR spectroscopy. Addition F- ion in CH3CN and DMSO to receptor 4 cause a colour...
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Synthesis and biological evaluation of fluorinated N-benzoyl and N-phenylacetoyl derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as steroid sulfatase inhibitors
PublicationIn the present work, we report convenient methods for the synthesis of 3-(4-aminophenyl)-coumarin-7-O-sulfamate derivatives N-acylated with fluorinated analogues of benzoic or phenylacetic acid as steroid sulfatase (STS) inhibitors. The design of these potential STS inhibitors was supported by molecular modeling techniques. Additionally, computational docking methods were used to determine the binding modes of the synthesized inhibitors...
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Convenient Synthesis of Functionalized Unsymmetrical Vinyl Disulfides and Their Inverse Electron-Demand Hetero-Diels-Alder Reaction
PublicationThe simple, convenient, and efficient methods for the preparation of unsymmetrical vinyl disulfides with additional functional groups under mild conditions with moderate to high yields were designed. The developed methods include the reaction of S-vinyl phosphorodithioate with thiotosylates or S-vinyl thiotosylate with thiols. The designed methods allow for the synthesis of unsymmetrical vinyl disulfides with additional functionalities...
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Detection and removal of priority substances and emerging pollutants from stormwater: case study of the Kołobrzeska collector, Gdańsk, Poland
PublicationProgressive urban development affects environmental balance and disrupts the hydrologic cycle, in which rainfall plays a significant role. Since rainwater is considered a valuable resource of the environment, many technical solutions are implemented that enable effective rainwater management. On the other hand, stormwater runoff from urban areas contains numerous (also toxic) substances, and therefore should be properly treated....
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Activation of Metabotropic Glutamate Receptor (mGlu2) and Muscarinic Receptors (M1, M4, and M5), Alone or in Combination, and Its Impact on the Acquisition and Retention of Learning in the Morris Water Maze, NMDA Expression and cGMP Synthesis
PublicationThe Morris water maze (MWM) is regarded as one of the most popular tests for detecting spatial memory in rodents. Long-term potentiation and cGMP synthesis seem to be among the crucial factors involved in this type of learning. Muscarinic (M1, M4, and M5 receptors) and metabotropic glutamate (mGlu) receptors are important targets in the search for antipsychotic drugs with the potency to treat cognitive disabilities associated with...
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The Quantum Efficiency Roll-Off Effect in Near-Infrared Organic Electroluminescent Devices with Iridium Complexes Emitters
PublicationThe electroluminescence quantum efficiency roll-off in iridium(III)-based complexes, namely Ir(iqbt)2(dpm) and Ir(iqbt)3(iqbt=1 (benzo[b]thiophen-2-yl)-isoquinolinate, dpm=2,2,6,6-tetramethyl-3,5-heptanedionate) utilized as near-infrared emitters in organic light emitting diodes with remarkable external quantum efficiencies, up to circa 3%, 1.5% and 1%, are measured and analyzed. With a 5–6 weight % of emitters embedded...
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Design, synthesis, and molecular docking of new 5-HT reuptake inhibitors based on modified 1,2-dihydrocyclopenta[b] indol-3(4H)-one scaffold
PublicationA new group of serotonin reuptake inhibitors containing 1,2-dihydrocyclopenta[b]indol-3(4H)-one scaffoldwas synthesized, starting from indole 5-((1H-indol-3-yl)(1,3-dioxane-4,6-diones as a key intermediates. Following three transformations including intramolecular cyclization and formation of imines, a series of new ligand for human serotonin transporter was obtained. The ability of these ligands to inhibit human TS3 serotonin transporter...