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Search results for: androgen receptor
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INTERNATIONAL JOURNAL OF HYDROGEN ENERGY
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Quantitative chirality in the binding of androgens to their receptor
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Androgens
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Structural and Pharmacological Characterization of Phenylalanine-Based AMPA Receptor Antagonists at Kainate Receptors
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Nuclear Receptor Signaling
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RECEPTORS & CHANNELS
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Analysis of interactions responsible for vasopressin binding to human neurohypophyseal hormone receptors—molecular dynamics study of the activated receptor–vasopressin–Gα systems
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Molecular Docking-Based Study of Vasopressin Analogues Modified at Positions 2 and 3 with N-Methylphenylalanine: Influence on Receptor-Bound Conformations and Interactions with Vasopressin and Oxytocin Receptors
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Investigation of mechanism of desmopressin binding in vasopressin V2 receptor versus vasopressin V1a and oxytocin receptors: Molecular dynamics simulation of the agonist-bound state in the membrane–aqueous system
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Study of New Oxytocin Antagonist Barusiban (Fe200 440) Affinity Toward Human Oxytocin Receptor Versus Vasopressin V1a and V2 Receptors - Molecular Dynamics Simulation in POPC Bilayer
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Angiotensin receptor blockers and endpoint protection
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Vasopressin V2 receptor/bioligand interactions
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Journal of Receptor Ligand and Channel Research
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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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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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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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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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Transfer. Reception studies
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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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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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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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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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Anticancer Imidazoacridinone C-1311 is Effective in Androgen-Dependent and Androgen-Independent Prostate Cancer Cells
PublicationAndrogen receptor (AR) plays a crutial role in prostate cancer (PCa) development and metastasis. Here, we reported potent anti-PCa activity of a small molecule imidazoacridinone C-1311. In AR-positive PCa cells, C-1311 was found to inhibit the transcriptional activity of AR uncovering a novel mechanism that may be relevant for its anticancer effect. Mechanistically, C-1311 decreased AR binding to prostate-specific antigen (PSA)...
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Estrogen Receptors in Cell Membranes: Regulation and Signaling
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Evidence for sex steroid receptors in feline brainstem
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Pyridylmethylsilanes as dicarboxyacid receptors: Experimental and theoretical study
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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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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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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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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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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...