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Search results for: AMIDE RECEPTORS
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Both activating and inhibitory Fc gamma receptors mediate rituximab-induced trogocytosis of CD20 in mice
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Molecular dynamics simulation of human neurohypophyseal hormone receptors complexed with oxytocin—modeling of an activated state
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Evaluation of Receptor Affinity, Analgesic Activity and Cytotoxicity of a Hybrid Peptide, AWL3020
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The FMO analysis of the molecular interaction of fentanyl derivatives with the μ-opioid receptor
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Receptor for advanced glycation end‐products: Biological significance and imaging applications
PublicationThe receptor for advanced glycation end-products (RAGE or AGER) is a transmembrane, immunoglobulin-like receptor that, due to its multiple isoform structures, binds to a diverse range of endo- and exogenous ligands. RAGE activation caused by the ligand binding initiates a cascade of complex pathways associated with producing free radicals, such as reactive nitric oxide and oxygen species, cell proliferation, and immunoinflammatory...
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Salicylaldimine-based receptor as a material for iron(III) selective optical sensing
Publicationα,α-Bis(salicylimino)-m-xylene (L) was prepared using both conventional and microwave-assisted procedure. The compound exhibits ability to colorimetric recognition of iron(III) ions in aqueous environment, what is shown by significant color change from yellow to purple. In DMSO : water (9:1 v/v) solvent system receptor creates with iron(III) cations complexes of 2:1 stoichiometry (L:Fe3+) with stability constant (log K) 7.54±0.21....
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Genes involved in glucocorticoid receptor signalling affect susceptibility to mood disorders
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Expression of ghrelin and ghrelin functional receptor GHSR1a in human pituitary adenomas
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Angiotensin II receptor blocker combinations: From guidelines to clinical practice
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The surge of Japanese studies supporting the use of angiotensin receptor blockers in hypertension
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Discovery of the First Highly Selective Antagonist of the GluK3 Kainate Receptor Subtype
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Computational methods for calculation of binding free energy for ligand-receptor complexes
PublicationAccurate description of the molecular complexes energetic influence is required for understanding of many biological functions carried out by proteins. Therefore, estimation of binding free energy for ligand-receptor complexes is of highest importance for structure-based ligand design and drug discovery approaches.Experimental methods of determination of difference in Gibbs'es free energy have many limitations. Thus, computational...
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Olfactory receptor-based biosensors as potential future tools in medical diagnosis
PublicationThe detection of biomarkers is the future of non-invasive medical diagnosis and screening. Discovery and identification of reliable disease specific volatile organic compounds is dependent on repeatable, accurate analysis of trace level gaseous analytes mainly in breath samples. Natural variety of the olfactory systems and the compounds capable of gas molecules binding creates wide possibilities of acquisition and implementation...
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Amides as models to study the hydration of proteins and peptides — spectroscopic and theoretical approach on hydration in various temperatures
PublicationInteractions with water are one of the key factors which determine protein stability and activity in aqueous solutions. However, the protein hydration is still insufficiently understood. N-methylacetamide (NMA) is regarded as a minimal part of the peptide backbone and the relative simplicity of its structure makes it a good model for studies on protein–water interactions. In this paper, the influence of NMA and N,N-dimethylacetamide...
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Cubane Like Structure of a Silanethiol Primary Amine Assembly a Novel, Unusual Hydrogen Bond Pattern.
PublicationMetodą rentgenowskiej analizy strukturalnej wyznaczono struktury krystaliczne i cząsteczkowe trzech soli amoniowych: (t-BuO)3SiS(-)H3N(+)Bu-t, (i-PrO)3SiS(-)H3N(+)Bu-t i (t-BuO)3SiS(-)H3N(+)(CH2)2CH(CH3)2. Wszystkie trzy związki w ciele stałym tworzą tetramery w których atomy S i N wyznaczają w przybliżeniu naroża sześcianu. Trwałość tych agregatów, oprócz sił elektrostatycznego przyciągania, zapewnia sieć wiązań wodorowych N-H
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Influence of Illite and Its Amine Modifications on the Self-Adhesive Properties of Silicone Pressure-Sensitive Adhesives
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Electromodulation and magnetomodulation of exciton dissociation in electron donor (starburst amine) : electron acceptor (bathocuproine) system
PublicationElectric field dependencies of electromodulated photoluminescence and photocurrents as well as the magnetic field effects on photocurrents, photovoltaic characteristics, electromodulated photoluminescence and photoluminescence have been investigated in vacuum evaporated films of m-MTDATA:BCP (4,4',4''-tris(N-(3-methylphenyl)-N-phenylamino)triphenylamine and bathocuproine) system. The electromodulation processes do remain in accordance...
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Self-assembly of secondary aryl amides in cocrystals with perfluoroaryl coformers: structural analysis and synthon preferences
PublicationCooperation of aryl⋯perfluoroaryl stacking interactions and hydrogen bonds was utilized in the construction of six novel cocrystals of aromatic cis-amides with pentafluorobenzoic acid (pfba) and pentafluorophenol (pfp). They were obtained by crystallization from solution and structurally characterized. In four instances, the components form heterotetrameric motifs, in which amide:amide homodimer interacts symmetrically on two sides...
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Stromal Derived Factor-1 (SDF-1) and Its Receptors CXCR4 and CXCR7 in Endometrial Cancer Patients
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Clinical and Biological Significance of ESR1 Gene Alteration and Estrogen Receptors Isoforms Expression in Breast Cancer Patients
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The expression of Platelet-derived Growth factor receptors (PDGFRs) and their correlation with overall survival of patients with ovarian cancer
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A Potential Relationship Between Estrogen Receptors Polymorphisms, Sperm Function and in vitro Fertilization Success: A Preliminary Study*
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Novel anion receptors: hybrid materials based on quaternary ammonium salts for selective extraction of dichromate ions
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Design, synthesis and structure–activity relationships of novel phenylalanine-based amino acids as kainate receptors ligands
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Pharmacological characterization and binding modes of novel racemic and optically active phenylalanine-based antagonists of AMPA receptors
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Fosfonowe pochodne kaliks[4]arenów jako receptory w środowisku wodnym
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Rola polimorfizmu i zróżnicowanej ekspresji genów cytochromu P450 w metabolizmie ksenobiotyków.
PublicationZdolność do metabolizmu ksenobiotyków przez cytochromy P450 (CYP) określona jest przez polimorfizm i poziom ekspresji genów tych białek. Najwięcej, 40 odmian polimorficznych o zróżnicowanej aktywności enzymatycznej, poznano dla CYP2D6, natomiast tylko dwie w przypadku CYP2C9, których obecność powoduje zahamowanie metabolizmu wielu leków. Z kolei polimorfizm genu CYP3A4 nie miał istotnego wpływu na aktywność metaboliczną jego produktu...
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NK1 receptor binding of a few low molecular weight 3,5-bistrifluoromethylbenzene derivatives
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Structural Insights into σ1 Receptor Interactions with Opioid Ligands by Molecular Dynamics Simulations
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Fentanyl Family at the Mu-Opioid Receptor: Uniform Assessment of Binding and Computational Analysis
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Dysfunctional prefrontal cortical network activity and interactions following cannabinoid receptor activation.
PublicationCoordinated activity spanning anatomically distributed neuronal networks underpins cognition and mediates limbic-cortical interactions during learning, memory, and decision-making. We used CP55940, a potent agonist of brain cannabinoid receptors known to disrupt coordinated activity in hippocampus, to investigate the roles of network oscillations during hippocampal and medial prefrontal cortical (mPFC) interactions in rats. During...
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Genetic Determinants of Vitamin D-Related Disorders; Focus on Vitamin D Receptor
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CRF1 receptor splicing in epidermal keratinocytes: Potential biological role and environmental regulations
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Hormonal Receptor Status Determines Prognostic Significance of FGFR2 in Invasive Breast Carcinoma
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Will we ever use angiotensin receptor neprilysin inhibition (ARNi) for the treatment of hypertension?
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Imidazo-thiazine, -diazinone and -diazepinone derivatives. Synthesis, structure and benzodiazepine receptor binding
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Molecular insights into receptor binding energetics and neutralization of SARS-CoV-2 variants
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In vivoevaluation of the CB1allosteric modulator LDK1258 reveals CB1-receptor independent behavioral effects
PublicationIn the present study, we examined whether LDK1258, which produces strong CB1receptor allosteric effects ininvitroassays, would elicitin vivoeffects consistent with allosteric activity. In initial studies, LDK1258 reducedfood consumption and elicited delayed antinociceptive effects in the chronic constrictive injury of the sciaticnerve (CCI) model of neuropathic pain, which unexpectedly emerged 4 h post-injection. UPLC-MS/MS analysisquantified...
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Search for new tools to combat Gram-negative resistant bacteria among amine derivatives of 5-arylidenehydantoin
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Photoconduction and magnetic field effect on photoconduction in hole-transporting star-burst amine (m-MTDATA) films
PublicationPhotoconduction and magnetic field effect on photoconduction have been investigated as a function of electric field strength, excitation light intensity and wavelength in vacuum evaporated films of m-MTDATA (4,4′,4″-tris(N-(3-methylphenyl)-N-phenylylamino) triphenylamine), the starburst amine commonly used as hole-transporting material in organic light-emitting diodes. The photocurrent is found to be generated by the singlet exciton...
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Exploring the Reactivity of Unsymmetrical Diphosphanes toward Heterocumulenes: Access to Phosphanyl and Phosphoryl Derivatives of Amides, Imines, and Iminoamides
PublicationWe present a comprehensive study on the diphosphanation of iso(thio)cyanates by unsymmetrical diphosphanes. The reactions involving unsymmetrical diphosphanes and phenyl isocyanate or phenyl thioisocyanate gave rise to phosphanyl, phosphoryl, and thiophosphoryl derivatives of amides, imines, and iminoamides. The structures of the diphosphanation products were confirmed through NMR spectroscopy, IR spectroscopy, and single-crystal...
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Preferential solvation in (amide+alcohol) binary mixtures. Part 2. The N-methylpyrrolidinone+methanol mixture at T = 313.15 K: thermodynamic resultsand molecular dynamics calculations.
PublicationBadano zjawisko preferencyjnej solwatacji amidu (N-metylopyrrolidonu) przez metanol wykorzystując dwie uzupełniające się metody: bezpośrednich pomiarów własności termodynamicznych roztworu oraz symulacji komputerowych. W metodzie pierwszej dokonano pomiarów wielkości termodynamicznych takich jak: nadmiarowa energia swobodna mieszania, nadmiarowa objętość mieszania oraz współczynnika ściśliwości izotermicznej mieszaniny,...
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Preferential solvation in (amide+alcohol) binary mixtures. Part 1. The N- methylpyrrolidinone+ethanol mixture at T = 313.15 K: thermodynamic resultsand molecular dynamics calculations.
PublicationBadano zjawisko preferencyjnej solwatacji amidu (N-metylopyrrolidonu) przez etanol wykorzystując dwie uzupełniające się metody: bezpośrednich pomiarów własności termodynamicznych roztworu oraz symulacji komputerowych. W metodzie pierwszej dokonano pomiarów wielkości termodynamicznych takich jak: nadmiarowa energia swobodna mieszania, nadmiarowa objętość mieszania oraz współczynnika ściśliwości izotermicznej mieszaniny,...
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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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O-substituted tetrahydroxamate derivatives of p-tert-butylcalix[4]arene as receptors for transition and heavy metal cations
PublicationTetrasubstituted O-hydroxamate derivatives of p-tert-butylcalix[4]arene were applied as active materials in ion-selective membrane electrodes and were tested towards Pb-selectivity. The electrodes gave near-Nernstian characteristics for Pb2+ cations. The selectivity coefficients were determined. The influence of plasticizer on the electrode behaviour was studied. The dependence of the chemical structure on selectivity coefficients...
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An Influence of the Aromatic Side Chains Conformations in Positions 2 and 3 of Vasopressin Analogs on Interactions with Vasopressin and Oxytocin Receptors
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Ion recognition properties of new pyridine-2,6-dicarboxamide bearing propeller-like pendant residues: multi-spectroscopic approach
PublicationThe synthesis and ion binding properties of new amide derived from propeller-like tris(2-pyridyl)amine and 2,6-pyridinedicarboxylic acid chloride were described. Amide binds divalent metal cations: copper(II), nickel(II), zinc(II), and lead(II) in acetonitrile. In acetonitrile:water mixture (9:1 v/v) amide interacts only with copper(II) and nickel(II) cations forming complexes of 1:1 stoichiometry. It was found that the introduction...
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Diversity of Students’ Unethical Behaviors in Online Learning Amid COVID-19 Pandemic: An Exploratory Analysis
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Structural studies on radiopharmaceutical DOTA-minigastrin analogue (CP04) complexes and their interaction with CCK2 receptor
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Novel Tools for Comprehensive Functional Analysis of LDLR (Low-Density Lipoprotein Receptor) Variants
PublicationFamilial hypercholesterolemia (FH) is an autosomal-dominant disorder caused mainly by substitutions in the low-density lipoprotein receptor (LDLR) gene, leading to an increased risk of premature cardiovascular diseases. Tremendous advances in sequencing techniques have resulted in the discovery of more than 3000 variants of the LDLR gene, but not all of them are clinically relevant. Therefore, functional studies of selected variants...