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Search results for: receptor tyrosine kinase flt3
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Antitumor triazoloacridinone C-1305 as a potent FLT3 tyrosine kinase inhibitor in human acute myeloid leukemia (AML) cells.
PublicationJednym z defektów molekularnych u pacjentów z ostrą białaczką szpikową (AML) jest konstytutywna aktywacja receptoroweej kinazy tyrozynowj FLT3.Najczęstszą mutacją genu kodującego FLT3 jest wewnętrzna tandemowa duplikacja ITD we fragmencie okołobłonowym receptora. W pracy zbadano, czy przeciwnowotworowy triazoloakrydon C-1305 może być inhibitorem kinazy tyrozynowej FLT3. Badania przeprowadzono na dwóch liniach komórkowych białaczek...
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The Role of FLT3 Kinase as an AML Therapy Target
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Targeting of FLT3-ITD kinase contributes to high selectivity of imidazoacridinone C-1311 against FLT3-activated leukemia cells
PublicationDrugs targeting receptor tyrosine kinase FLT3 are of particular interest since activating FLT3-internal tandem duplication (ITD) mutations abundantly occur in fatal acute myeloid leukemias (AMLs). Imidazoacridinone C-1311, a DNA-reactive inhibitor of topoisomerase II, has been previously shown to be a potent and selective inhibitor of recombinant FLT3. Here, we expand those findings by studying its effect on leukemia cells with...
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The antitumor compound triazoloacridinone C-1305 inhibits FLT3 kinase activity and potentiates apoptosis in mutant FLT3-ITD leukemia cells.
PublicationAim: FMS-like receptor tyrosine kinase (FLT3) is expressed in some normal hematopoietic cell types and plays an important role in the pathogenesis of acute myeloid leukemia (AML). In this study, we examined the effects of triazoloacridinone C-1305, an antitumor compound, on AML cells with different FLT3 status in vitro. Methods: A panel of human leukemic cell lines with different FLT3 status was used, including FLT3 internal tandem...
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The Kinetics of FMS-Related Tyrosine Kinase 3 Ligand (Flt-3L) during Chemoradiotherapy Suggests a Potential Gain from the Earlier Initiation of Immunotherapy
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Structural and Pharmacological Characterization of Phenylalanine-Based AMPA Receptor Antagonists at Kainate Receptors
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9,10-Dioxoanthracenyldithiocarbamates effectively inhibit the proliferation of non-small cell lung cancer by targeting multiple protein tyrosine kinases
PublicationAnthraquinones have attracted considerable interest in the realm of cancer treatment owing to their potent anticancer properties. This study evaluates the potential of a series of new anthraquinone derivatives as anticancer agents for non-small-cell lung cancer (NSCLC). The compounds were subjected to a range of tests to assess their cytotoxic and apoptotic properties, ability to inhibit colony formation, pro-DNA damage functions,...
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3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands
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Role of Src Kinases in Neu-Induced Tumorigenesis: Challenging the Paradigm Using Csk Homologous Kinase Transgenic Mice
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Discovery of the First Highly Selective Antagonist of the GluK3 Kainate Receptor Subtype
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The photophysics of β-homo-tyrosine and its simple derivatives
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Design, synthesis and structure–activity relationships of novel phenylalanine-based amino acids as kainate receptors ligands
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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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L-tyrosine and L-dihydroxyphenylalanine as hormone-like regulators of melanocyte functions
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A convenient synthesis of (S)-O-benzyl-N-tert-butoxycarbonyl-beta-tyrosine.
PublicationOpracowano dogodną metodę syntezy tytułowego aminokwasu z aldehydu 4-benzyloksybenzoesowego, kwasu malonowego i octanu amonu. Otrzymany aminokwasu rozdzielono na enancjomery poprzez krystalizację soli diastereoizomerycznej z kwasem L-winowym.
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Synthesis of novel, peptidic kinase inhibitors with cytostatic/cytotoxic activity
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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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Influence of the substituent on amide nitrogen atom of N-acetyl tyrosine on interactions with β-cyclodextrin
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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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Molecular features of thymidine analogues governing the activity of human thymidine kinase
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Vasopressin V2 receptor/bioligand interactions
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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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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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Germline mutations in theCHEK2 kinase gene are associated with an increased risk of bladder cancer
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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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PELP1 and SRC kinase as important molecules in the estrogen-mediated pathway in human testis and epididymis
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Cofka w kanale
PublicationHydraulika sieci grawitacyjnych. Problemy spiętrzeń w przewodach kanalizacyjnych. Zasięg cofki. Przeciwdziałanie
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Fermentacja w kanale
PublicationKonsekwencje zmian jakościowych i ilościowych przepływu ścieków. Sammooczyszczanie, wtórne zmiany jakościowe
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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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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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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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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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Mitogen activated protein kinase 4 (MPK4) influences growth in Populus tremula L.×tremuloides
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Novel biocatalytic systems for maintaining the nucleotide balance based on adenylate kinase immobilized on carbon nanostructures
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Assessing the Interactions of Statins with Human Adenylate Kinase Isoenzyme 1: Fluorescence and Enzyme Kinetic Studies
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TLC-based detection of methylated cytosine: application to aging epigenetics
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Adenylate kinases of thermophilesAquifex aeolicusandGeobacillus stearothermophilus: biochemical and kinetic studies
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Human adenylate kinases – classification, structure, physiological and pathological importance
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MITOGEN-ACTIVATED PROTEIN KINASE 4 impacts leaf development, temperature, and stomatal movement in hybrid aspen
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