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Search results for: ENZYMATIC RECEPTOR
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Structural and Pharmacological Characterization of Phenylalanine-Based AMPA Receptor Antagonists at Kainate Receptors
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New generation of analytical tests based on the assessment of enzymatic and nuclear receptor activity changes induced by environmental pollutants
PublicationAnalytical methods show great potential in biological tests. The analysis of biological response that results from environmental pollutant exposure allows: (i) prediction of the risk of toxic effects and (ii) provision of the background for the development of markers of the toxicants presence. Bioanalytical tests based on changes in enzymatic activity and nuclear receptor action provide extremely high specificity and sensitivity....
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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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Enzymatic activities behind degradation of glucosinolates
PublicationMyrosinase (thioglucosidase, EC 3.2.1.147) is the enzyme responsible for the hydrolysis of glucosinolates (GLs). In plant tissue, myrosinase and GLs are sequestered in separate cellular compartments. As a result of cell disruption, e.g., after pathogen attack or on chopping or grinding during food preparation, the myrosinase comes into contact with GLs and catalyzes the hydrolysis of thioglucosidic bond in GL structure. Consequently,...
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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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Enantioselective enzymatic desymmetrization of the prochiral pyrimidine acyclonucleoside
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Production of trehalose in a single step enzymatic reaction
PublicationThe aim of this study was isolation and cloning of trehalose synthase gene derived from extremophilic microorganisms Deinoccoci to the expressive E. coli vectors and its biosythesis in different hosts.
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Vasopressin V2 receptor/bioligand interactions
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Quantitative chirality in the binding of androgens to their receptor
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Angiotensin receptor blockers and endpoint protection
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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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Estrogen receptor 2 polymorphism in idiopathic scoliosis
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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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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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Enzymatic Activity as New Moorsh-Forming Process Indicators of Peatlands
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Sandwich Biobattery with Enzymatic Cathode and Zinc Anode Integrated with Sensor
PublicationCarbon paper covered with side-naphthylated multi walled carbon nanotubes was used as the conducting support for the construction of a biocathode in a hybrid biofuel cell. Laccase Carrena unicolor enzyme was employed as the catalyst for the 4e reduction of oxygen and a zinc disc covered with hopeite was used as the anode. Derivatized carbon nanotubes increase the working surface of the electrode and provide direct contact with...
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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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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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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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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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Green chemical and hybrid enzymatic pretreatments for lignocellulosic biorefineries: Mechanism and challenges
PublicationThe greener chemical and enzymatic pretreatments for lignocellulosic biomasses are portraying a crucial role owing to their recalcitrant nature. Traditional pretreatments lead to partial degradation of lignin and hemicellulose moieties from the pretreated biomass. But it still restricts the enzyme accessibility for the digestibility towards the celluloses and the interaction of lignin-enzymes, nonproductively. Moreover, incursion...
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Enzymatic degradation and transport of endothiopeptides into Escherichia coli K12 mutant strains
PublicationZbadano transport trzech otrzymanych na drodze syntezy ditiopeptydów do komórek Escherichia coli K12. Ponadto zbadano szybkość hydrolizy tych związków. Wszystkie peptydy są transportowane przez permeazy, natomiast są bardziej oporne na hydrolizę enzymatyczną w stosunku do naturalnych peptydów.
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Studies on the application of the Passerini reaction and enzymatic procedures to the synthesis of tripeptide mimetics
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Rat cathepsin K: Enzymatic specificity and regulation of its collagenolytic activity
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Effect of pesticides on microorganisms, enzymatic activity and plant in biochar-amended soil
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The role of the enzymatic antioxidant system in cylindrospermopsin-induced toxicity in human lymphocytes
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Electrochemical simulation of enzymatic transformations studied for the selected antitumor acridine derivatives
PublicationThe elucidation of the metabolic pathways and the biotransformation mechanisms of potential drugs is a crucial point in drug development. It allows to know the activation routes of the new biologically active compounds, especially in respect to their possible toxicity. Generally, in vivo or in vitro experiments with liver microsomes or hepatocytes are performed. However, these testing schemes are tedious, time consuming and of...
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Enzymatic electrodes nanostructured with functionalized carbon nanotubes for biofuel cell applications
PublicationNanostructured bioelectrodes were designed and assembled into a biofuel cell with no separating membrane.
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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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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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Molecular Dynamics of a Vasopressin V2 Receptor in a Phospholipid Bilayer Membrane
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RORα is not a receptor for melatonin (response to DOI 10.1002/bies.201600018)
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Membrane Filtration-Assisted Enzymatic Hydrolysis Affects the Biological Activity of Potato Juice
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Nitrobenzimidazoles as Substrates for DT-Diaphorase and Redox Cycling Compounds: Their Enzymatic Reactions and Cytotoxicity
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A Redundant Role of Human Thyroid Peroxidase Propeptide for Cellular, Enzymatic, and Immunological Activity
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The propeptide of human thyroid peroxidase is not required for its cellular, enzymatic or immunological activity
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Materials for Mediator-free Electron Transfer in the Enzymatic Electrodes of Biobatteries and Biofuel Cells
PublicationWe present functionalization of single-walled carbon nanotubes (SWCNTs) and their application in the enzymatic fuel cells construction. SWCNTs were covalently modified with different types of aromatic moieties. Free radical reaction was employed to create direct carbon-carbon bond between moiety and SWCNTs. In second approach functionalization takes place through amide bonding. Functionalized SWCNTs were characterized by spectroscopy...
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Molecular mechanism of the enzymatic oxidation investigated for imidazoacridinone antitumor drug C-1311.
PublicationPraca miala na celu określenie molekularnego mechanizmu enzymatycznej utleniającej aktywacji wymienionego związku przeciwnowotworowego w takim układzie modelowym, w którym wcześniej wykazano jego kowalencyjne wiązanie się do DNA. Badania struktur chemicznych produktów enzymatycznej aktywacji wykazały, że dwa z nich powstają w wyniku dealkilacji łańcucha bocznego cząsteczki, natomiast dwa inne w wyniku aktywacji pierścienia imidazoakrydonu....
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Pyridylmethylsilanes as dicarboxyacid receptors: Experimental and theoretical study
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