Search Results - "Doležal, Vladimír"

The operational model of allosteric modulation of pharmacological agonism by Jakubík, Jan, Randáková, Alena, Chetverikov, Nikolai, El-Fakahany, Esam E., Doležal, Vladimír

“…Proper determination of agonist efficacy is indispensable in the evaluation of agonist selectivity and bias to activation of specific signalling pathways. The…”
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Agonist-Specific Conformations of the M2 Muscarinic Acetylcholine Receptor Assessed by Molecular Dynamics by Randáková, Alena, Nelic, Dominik, Doležal, Vladimír, El-Fakahany, Esam E, Boulos, John, Jakubík, Jan

“…Binding of muscarinic ligands, both antagonists and agonists, and their effects on the conformation of the M2 acetylcholine receptor were modeled in silico and…”
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Agonist-Specific Conformations of the M 2 Muscarinic Acetylcholine Receptor Assessed by Molecular Dynamics by Randáková, Alena, Nelic, Dominik, Doležal, Vladimír, El-Fakahany, Esam E, Boulos, John, Jakubík, Jan

“…Binding of muscarinic ligands, both antagonists and agonists, and their effects on the conformation of the M acetylcholine receptor were modeled and compared…”
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Novel long‐acting antagonists of muscarinic ACh receptors by Randáková, Alena, Rudajev, Vladimír, Doležal, Vladimír, Boulos, John, Jakubík, Jan

“…Background and Purpose The aim of this study was to develop potent and long‐acting antagonists of muscarinic ACh receptors. The 4‐hexyloxy and 4‐butyloxy…”
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Towards predictive docking at aminergic G-protein coupled receptors by Jakubík, Jan, El-Fakahany, Esam E., Doležal, Vladimír

“…G protein-coupled receptors (GPCRs) are hard to crystallize. However, attempts to predict their structure have boomed as a result of advancements in…”
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Molecular mechanisms of methoctramine binding and selectivity at muscarinic acetylcholine receptors by Jakubík, Jan, Zimčík, Pavel, Randáková, Alena, Fuksová, Květoslava, El-Fakahany, Esam E, Doležal, Vladimír

“…Methoctramine (N,N'-bis[6-[[(2-methoxyphenyl)-methyl]hexyl]-1,8-octane] diamine) is an M(2)-selective competitive antagonist of muscarinic acetylcholine…”
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Membrane cholesterol content influences binding properties of muscarinic M 2 receptors and differentially impacts activation of second messenger pathways by Michal, Pavel, Rudajev, Vladimír, El-Fakahany, Esam E., Doležal, Vladimír

“…We investigated the influence of membrane cholesterol content on preferential and non-preferential signaling through the M 2 muscarinic acetylcholine receptor…”
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Long-term activation upon brief exposure to xanomleline is unique to M1 and M4 subtypes of muscarinic acetylcholine receptors by Šantrůčková, Eva, Doležal, Vladimír, El-Fakahany, Esam E, Jakubík, Jan

“…Xanomeline is an agonist endowed with functional preference for M1/M4 muscarinic acetylcholine receptors. It also exhibits both reversible and wash-resistant…”
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Detection of choline transporter‐like 1 protein CTL1 in neuroblastoma × glioma cells and in the CNS, and its role in choline uptake by Machová, Eva, O’Regan, Seana, Newcombe, Jia, Meunier, François‐Marie, Prentice, Joanna, Dove, Rosamund, Lisá, Věra, Doležal, Vladimír

“…Choline is an essential nutrient necessary for synthesis of membrane phospholipids, cell signalling molecules and acetylcholine. The aim of this study was to…”
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Analysis of equilibrium binding of an orthosteric tracer and two allosteric modulators by Dolezal, Vladimír, Jakubík, Jan, El-Fakahany, Esam E, Randáková, Alena

“…Allosteric ligands bind to receptors at sites that are distinct from those endogenous agonists and orthosteric pharmacological agents interact with. Both an…”
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Apolipoprotein E4 reduces evoked hippocampal acetylcholine release in adult mice by Dolejší, Eva, Liraz, Ori, Rudajev, Vladimír, Zimčík, Pavel, Doležal, Vladimír, Michaelson, Daniel M.

“…Apolipoprotein E4 (apoE4) is the most prevalent genetic risk factor for Alzheimer's disease. We utilized apoE4‐targeted replacement mice (approved by the Tel…”
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Changes in Membrane Cholesterol Differentially Influence Preferential and Non-preferential Signaling of the M1 and M3 Muscarinic Acetylcholine Receptors by Michal, Pavel, El-Fakahany, Esam E., Doležal, Vladimír

“…We have found earlier that changes in membrane cholesterol content have distinct impact on signaling via the M1, M2, or M3 receptors expressed in CHO cells…”
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Chronic treatment with amyloid β1-42 inhibits non-cholinergic high-affinity choline transport in NG108-15 cells through protein kinase C signaling by NOVAKOVA, Jana, MIKASOVA, Lenka, MACHOVA, Eva, LISA, Vera, DOLEZAL, Vladimir

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Binding of N-methylscopolamine to the extracellular domain of muscarinic acetylcholine receptors by Jakubík, Jan, Randáková, Alena, Zimčík, Pavel, El-Fakahany, Esam E., Doležal, Vladimír

“…Interaction of orthosteric ligands with extracellular domain was described at several aminergic G protein-coupled receptors, including muscarinic acetylcholine…”
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Functional cholinergic damage develops with amyloid accumulation in young adult APPswe/PS1dE9 transgenic mice by Machová, Eva, Rudajev, Vladimír, Smyčková, Helena, Koivisto, Henna, Tanila, Heikki, Doležal, Vladimír

“…Abstract We investigated the functional characteristics of pre- and postsynaptic cholinergic transmission in APPswe/PS1dE9 double transgenic mice at a young…”
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The effects of brucine and alcuronium on the inhibition of [3H]acetylcholine release from rat striatum by muscarinic receptor agonists by DOLEZAL, V, TUCEK, S

“…1 Radioligand binding experiments indicate that the affinity of muscarinic receptors for their agonists may be enhanced by allosteric modulators. We have now…”
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Subtype differences in pre-coupling of muscarinic acetylcholine receptors by Dolezal, Vladimír, Jakubík, Jan, El-Fakahany, Esam E, Janícková, Helena, Randáková, Alena

“…Based on the kinetics of interaction between a receptor and G-protein, a myriad of possibilities may result. Two extreme cases are represented by: 1/Collision…”
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Membrane cholesterol content influences binding properties of muscarinic M2 receptors and differentially impacts activation of second messenger pathways by MICHAL, Pavel, RUDAJEV, Vladimir, EL-FAKAHANY, Esam E, DOLEZAL, Vladimir

“…We investigated the influence of membrane cholesterol content on preferential and non-preferential signaling through the M(2) muscarinic acetylcholine receptor…”
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Detection of choline transporter-like 1 protein CTL1 in neuroblastoma x glioma cells and in the CNS, and its role in choline uptake by Machová, Eva, O'Regan, Seana, Newcombe, Jia, Meunier, François-Marie, Prentice, Joanna, Dove, Rosamund, Lisá, Věra, Doležal, Vladimír

“…Choline is an essential nutrient necessary for synthesis of membrane phospholipids, cell signalling molecules and acetylcholine. The aim of this study was to…”
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Pharmacological evaluation of the long-term effects of xanomeline on the M(1) muscarinic acetylcholine receptor by Grant, Marianne K O, Noetzel, Meredith J, De Lorme, Kayla C, Jakubík, Jan, Doležal, Vladimír, El-Fakahany, Esam E

“…Xanomeline is a unique agonist of muscarinic receptors that possesses functional selectivity at the M(1) and M(4) receptor subtypes. It also exhibits…”
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