Search Results - "Jakubík, Jan"

Allosteric Modulation of GPCRs of Class A by Cholesterol by Jakubík, Jan, El-Fakahany, Esam E

“…G-protein coupled receptors (GPCRs) are membrane proteins that convey extracellular signals to the cellular milieu. They represent a target for more than 30%…”
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A critical re-evaluation of the slope factor of the operational model of agonism: When to exponentiate operational efficacy by Randáková, Alena, Nelic, Dominik, Jakubík, Jan

“…Agonist efficacy denoting the “strength” of agonist action is a cornerstone in the proper assessment of agonist selectivity and signalling bias. The simulation…”
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Functionally selective and biased agonists of muscarinic receptors by Randáková, Alena, Jakubík, Jan

“…Disruption of cholinergic signalling via muscarinic receptors is associated with various pathologies, like Alzheimer’s disease or schizophrenia. Selective…”
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Allosteric Modulation of Muscarinic Receptors by Cholesterol, Neurosteroids and Neuroactive Steroids by Szczurowska, Ewa, Szánti-Pintér, Eszter, Randáková, Alena, Jakubík, Jan, Kudova, Eva

“…Muscarinic acetylcholine receptors are membrane receptors involved in many physiological processes. Malfunction of muscarinic signaling is a cause of various…”
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Modulation of Muscarinic Signalling in the Central Nervous System by Steroid Hormones and Neurosteroids by Szczurowska, Ewa, Szánti-Pintér, Eszter, Chetverikov, Nikolai, Randáková, Alena, Kudová, Eva, Jakubík, Jan

“…Muscarinic acetylcholine receptors expressed in the central nervous system mediate various functions, including cognition, memory, or reward. Therefore,…”
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Agonist-selective activation of individual G-proteins by muscarinic receptors by Nelic, Dominik, Chetverikov, Nikolai, Hochmalová, Martina, Diaz, Christina, Doležal, Vladimír, Boulos, John, Jakubík, Jan, Martemyanov, Kirill, Janoušková-Randáková, Alena

“…Selective activation of individual subtypes of muscarinic receptors is a promising way to safely alleviate a wide range of pathological conditions in the…”
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Muscarinic Receptors in Cardioprotection and Vascular Tone Regulation by Dolejší, Eva, Janoušková, Alena, Jakubík, Jan

“…Muscarinic acetylcholine receptors are metabotropic G-protein coupled receptors. Muscarinic receptors in the cardiovascular system play a central role in its…”
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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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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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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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Neurosteroids and steroid hormones are allosteric modulators of muscarinic receptors by Dolejší, Eva, Szánti-Pintér, Eszter, Chetverikov, Nikolai, Nelic, Dominik, Randáková, Alena, Doležal, Vladimír, Kudová, Eva, Jakubík, Jan

“…The membrane cholesterol was found to bind and modulate the function of several G-protein coupled receptors including muscarinic acetylcholine receptors. We…”
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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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Neuroactive steroids, WIN-compounds and cholesterol share a common binding site on muscarinic acetylcholine receptors by Dolejší, Eva, Chetverikov, Nikolai, Szánti-Pintér, Eszter, Nelic, Dominik, Randáková, Alena, Doležal, Vladimír, El-Fakahany, Esam E., Kudová, Eva, Jakubík, Jan

“…[Display omitted] Endogenous neurosteroids and their synthetic analogues-neuroactive steroids-have been found to bind to muscarinic acetylcholine receptors and…”
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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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Novel M2‐selective, Gi‐biased agonists of muscarinic acetylcholine receptors by Randáková, Alena, Nelic, Dominik, Ungerová, Dana, Nwokoye, Peter, Su, Qiwen, Doležal, Vladimír, El‐Fakahany, Esam E., Boulos, John, Jakubík, Jan

“…Background and Purpose More than 30% of currently marketed medications act via GPCRs. Thus, GPCRs represent one of the most important pharmacotherapeutic…”
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Applications and limitations of fitting of the operational model to determine relative efficacies of agonists by Jakubík, Jan, Randáková, Alena, Rudajev, Vladimír, Zimčík, Pavel, El-Fakahany, Esam E., Doležal, Vladimír

“…Proper determination of agonist efficacy is essential in the assessment of agonist selectivity and signalling bias. Agonist efficacy is a relative term that is…”
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Fusion with Promiscuous Gα16 Subunit Reveals Signaling Bias at Muscarinic Receptors by Randáková, Alena, Nelic, Dominik, Hochmalová, Martina, Zimčík, Pavel, Mulenga, Mutale Jane, Boulos, John, Jakubík, Jan

“…A complex evaluation of agonist bias at G-protein coupled receptors at the level of G-protein classes and isoforms including non-preferential ones is essential…”
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Role of membrane cholesterol in differential sensitivity of muscarinic receptor subtypes to persistently bound xanomeline by Randáková, Alena, Dolejší, Eva, Rudajev, Vladimír, Zimčík, Pavel, Doležal, Vladimír, El-Fakahany, Esam E., Jakubík, Jan

“…Xanomeline (3-(Hexyloxy)-4-(1-methyl-1,2,5,6-tetrahydropyridin-3-yl)-1,2,5-thiadiazole) is a muscarinic agonist that is considered to be functionally selective…”
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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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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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