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Search results for: RECEPTOR
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The PARAGON Heart Failure trial – ongoing investigation of the angiotensin receptor antagonist/neprilysin inhibitor sacubitril/valsartan in heart failure patients with hypertension and preserved ejection fraction
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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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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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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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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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Pregnane X receptor dependent up-regulation of CYP2C9 and CYP3A4 in tumor cells by antitumor acridine agents, C-1748 and C-1305, selectively diminished under hypoxia
PublicationInduction of proteins involved in drug metabolism and in drug delivery has a significant impact on drug-drug interactions and on the final therapeutic effects. Two antitumor acridine derivatives selected for present studies, C-1748 (9-(2’-hydroxyethylamino)-4-methyl-1-nitroacridine) and C-1305 (5-dimethylaminopropylamino-8-hydroxy-triazoloacridinone), expressed high and low susceptibility to metabolic transformations with liver...
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Differential and Overlapping Effects of 20,23(OH)2D3 and 1,25(OH)2D3 on Gene Expression in Human Epidermal Keratinocytes: Identification of AhR as an Alternative Receptor for 20,23(OH)2D3
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Germline DNA Retention in Murine and Human Rearranged T Cell Receptor Gene Coding Joints: Alternative Recombination Signal Sequences and V(D)J Recombinase Errors
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In vitro biological evaluation of a novel folic acid-targeted receptor quantum dot−β−cyclodextrin carrier for C-2028 unsymmetrical bisacridine in the treatment of human lung and prostate cancers
PublicationTraditional small-molecule chemotherapeutics usually do not distinguish tumors from healthy tissues. However, nanotechnology creates nanocarriers that selectively deliver drugs to their site of action. This work is the next step in the development of the quantum dot−β−cyclodextrin−folic acid (QD−β−CD−FA) platform for targeted and selected delivery of C−2028 unsymmetrical bisacridine in cancer therapy.Herein, we report an initial...
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Application of Alanine Scanning to Determination of Amino Acids Essential for Peptide Adsorption at the Solid/Solution Interface and Binding to the Receptor: Surface-Enhanced Raman/Infrared Spectroscopy versus Bioactivity Assays
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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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Fosfonowe pochodne kaliks[4]arenów jako receptory w środowisku wodnym
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Pyridylmethylsilanes as dicarboxyacid receptors: Experimental and theoretical study
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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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Expression of hCG and GnRHs and Their Receptors in Endometrial Carcinoma and Hyperplasia
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new analogues of agmatine with higher activity to imidazoline receptors
PublicationOpracowano syntezę nowych pochodnych imidazoliny, będących kompilacją struktury agmatyny i imidazoliny w wyniku zaprojektowanej przez nas drogi syntezy. Kluczowymi substratami w syntezie były pochodne 1,2,4 -triaminobutanu, otrzymane z chronionego kwasu glutaminowego. Otrzymane nowe pochodne imidazoliny wykazywały zróżnicowane powinowactwo do receptorów imidazolinowych I1, I2 oraz do receptorów alfa -adrenergicznych.
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QSPR analysis of some agonists and antagonists of α-adrenergic receptors
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Estrogen receptors genes polymorphisms and age at menarche in idiopathic scoliosis
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Molecular Modeling of Interaction of the Vasopressin Analogs with Vasopressin and Oxytocin Receptors
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Neurotrophin serum concentrations and polymorphisms of neurotrophins and their receptors in children with asthma
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Chromogenic amides of pyridine-2,6-dicarboxylic acid as anion receptors
PublicationThe synthesis of simple, chromogenic pyridine-2,6-dicarboxylic acid amides, derivates of isomeric nitroanilines and aminonitrophenols, and their ion binding properties are described. The ligands' response to ionic species was examined by naked eye and was studied with the use of UV-Vis spectroscopy in DMSO and its mixture with water. The effect of the localisation and the type of the substituents in aromatic rings were discussed....
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DAF - and collagen-binding properties of chimeric Dr fimbriae
PublicationEkspozycja białek heterologicznych na powierzchni mikroorganizmów jest jedną z nowych strategii stosowanych w mikrobiologii, biotechnologii oraz projektowaniu nowoczesnych szczepionek. W niniejszej pracy zbadano możliwość wykorzystania białka podjednostkowego DraE fimbrii Dr uropatogennych szczepów Escherichia coli jako nośnika heterologicznych sekwencji. W rejon odpowiadający N-terminalnej domenie 2 białka DraE wprowadzono epitopową...
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Estrogen receptors 1 and 2 genotypes and age at menarche in idiopathic scoliosis
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Molecular Dynamics Study of the Internal Water Molecules in Vasopressin and Oxytocin Receptors
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Synthesis of Fentanyl Triazole Derivatives and their Affinity for Mu-Opioid and Sigma-1 Receptors
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Theoretical Study on Interactions of Bicyclic Vasopressin Analogues with Human Neurohypophyseal Hormone Receptors
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Expression of estrogen receptors, PELP1, and SRC in human spermatozoa and their associations with semen quality
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Neurohypophyseal Receptors-Ligands: Where We Are After the Landmark Rhodopsin Structure Determination
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Molecular Dynamics of Complexes of Atosiban with Neurohypophyseal Receptors in the Fully Hydrated Phospholipid Bilayer
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Studies on Aryl-Substituted Phenylalanines: Synthesis, Activity, and Different Binding Modes at AMPA Receptors
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Similarities and differences in affinity and binding modes of tricyclic pyrimido- and pyrazinoxanthines at human and rat adenosine 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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Vitamin D signaling and melanoma: role of vitamin D and its receptors in melanoma progression and management
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Expression and cellular distribution of estrogen and progesterone receptors and the real-time proliferation of porcine cumulus cells
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Novel anion receptors: hybrid materials based on quaternary ammonium salts for selective extraction of dichromate ions
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Stromal Derived Factor-1 (SDF-1) and Its Receptors CXCR4 and CXCR7 in Endometrial Cancer Patients
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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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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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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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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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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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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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Phenylalanine derivatives with modulating effects on human α1-glycine receptors and anticonvulsant activity in strychnine-induced seizure model in male adult rats
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Pharmacophore models based studies on the affinity and selectivity toward 5-HT1A with reference to α1-adrenergic receptors among arylpiperazine derivatives of phenytoin
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Can cornelian cherry mask bitter taste of probiotic chocolate? Human TAS2R receptors and a sensory study with comprehensive characterisation of new functional product
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Enhanced susceptibility of SARS-CoV-2 spike RBD protein assay targeted by cellular receptors ACE2 and CD147: Multivariate data analysis of multisine impedimetric response
PublicationSevere acute respiratory syndrome coronavirus 2 (SARS-CoV-2) enters the cells through the binding of spike protein to the host cell surface-expressing angiotensin-converting enzyme 2 (ACE2) or by endocytosis mediated by extracellular matrix metalloproteinase inducer (CD147). We present extended statistical studies of the multisine dynamic electrochemical impedance spectroscopy (DEIS) revealing interactions between Spike RBD and...