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Wyniki wyszukiwania dla: RECEPTOR
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Nuclear Receptor Signaling
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Journal of Receptor Ligand and Channel Research
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Angiotensin receptor blockers and endpoint protection
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Quantitative chirality in the binding of androgens to their receptor
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Vasopressin V2 receptor/bioligand interactions
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Structural and Pharmacological Characterization of Phenylalanine-Based AMPA Receptor Antagonists at Kainate Receptors
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Selective detection of F- by chromogenic tetrazole receptor
PublikacjaA 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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Molecular Modeling of the Neurohypophyseal Receptor/Atosiban Complexes
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Affinity of fentanyl and its derivatives for the σ1-receptor
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Estrogen receptor 2 polymorphism in idiopathic scoliosis
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Moving out of CF3‐Land: Synthesis, Receptor Affinity, and in silico Studies of NK1 Receptor Ligands Containing a Pentafluorosulfanyl (SF5) Group
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Towards β-selectivity in functional estrogen receptor antagonists
PublikacjaBased 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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New clicked full agonists of the estrogen receptor β
PublikacjaA 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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Targeting melanocortin receptor type 1 with small peptides
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Vitamin D receptor(s): In the nucleus but also at membranes?
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Gαi-derived peptide binds the µ-opioid receptor
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Molecular dynamics of fentanyl bound to μ-opioid receptor
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Estrogen Receptor 2 Gene Polymorphism in Idiopathic Scoliosis
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Aryl- and heteroaryl-substituted phenylalanines as AMPA receptor ligands
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Trend research of vitamin D receptor: Bibliometric analysis
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RORα is not a receptor for melatonin (response to DOI 10.1002/bies.201600018)
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Tuning the sumanene receptor structure towards the development of potentiometric sensors
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Vitamin D receptor gene polymorphisms in Alzheimer's disease patients
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The neuroprotective activity of new phenylalanine-based AMPA receptor antagonists
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3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands
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Molecular Dynamics of a Vasopressin V2 Receptor in a Phospholipid Bilayer Membrane
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Receptor for advanced glycation end‐products: Biological significance and imaging applications
PublikacjaThe 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
Publikacjaα,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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Computational methods for calculation of binding free energy for ligand-receptor complexes
PublikacjaAccurate 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
PublikacjaThe 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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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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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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Expression of ghrelin and ghrelin functional receptor GHSR1a in human pituitary adenomas
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Discovery of the First Highly Selective Antagonist of the GluK3 Kainate Receptor Subtype
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Genes involved in glucocorticoid receptor signalling affect susceptibility to mood disorders
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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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Molecular insights into receptor binding energetics and neutralization of SARS-CoV-2 variants
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Will we ever use angiotensin receptor neprilysin inhibition (ARNi) for the treatment of hypertension?
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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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Imidazo-thiazine, -diazinone and -diazepinone derivatives. Synthesis, structure and benzodiazepine receptor binding
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Hormonal Receptor Status Determines Prognostic Significance of FGFR2 in Invasive Breast Carcinoma
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Dysfunctional prefrontal cortical network activity and interactions following cannabinoid receptor activation.
PublikacjaCoordinated 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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In vivoevaluation of the CB1allosteric modulator LDK1258 reveals CB1-receptor independent behavioral effects
PublikacjaIn 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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The electrochemical response to BDD electrode functionalization with CD147 receptor
Dane BadawczeThis dataset contains the results of the electrochemical impedance spectroscopy (EIS) measurements of the boron-doped diamond (BDD) electrode functionalization with CD147 receptor. The functionalized electrode was then used for the electrochemical detection of the SARS-CoV-2 virus S1 protein.
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The electrochemical response to BDD electrode functionalization with ACE2 receptor
Dane BadawczeThis dataset contains the results of the electrochemical impedance spectroscopy (EIS) measurements of the boron-doped diamond (BDD) electrode functionalization with ACE2 receptor. The functionalized electrode was then used for the electrochemical detection of the SARS-CoV-2 virus S1 protein.