Results 21 to 30 of about 131,252 (300)
Molecules, 2022 Allosteric modulation of G protein-coupled receptors (GPCRs) is nowadays a hot topic in medicinal chemistry. Allosteric modulators, i.e., compounds which bind in a receptor site topologically distinct from orthosteric sites, exhibit a number of ...
Agnieszka A. Kaczor +2 more
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Allosteric Modulators of Adenosine Receptors
, 2023 Allosterism occurs when a ligand binds to a receptor on a binding site distinct from the orthosteric one to which endogenous ligand normally binds. Among the G protein-coupled receptors (GPCRs), the adenosine receptors (ARs), classified as A1, A2A, A2B ...
Da Settimo, Federico +5 more
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Pharmacological Research, 2023 Considerable progress has been made in recent years towards the identification and characterisation of novel subtype-selective modulators of nicotinic acetylcholine receptors (nAChRs).
Victoria R. Sanders, Neil S. Millar
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Biochemical pharmacology of the positive allosteric modulation of the GABAb receptor "in Vitro" and "in Vivo" [PDF]
, 2007 Allosteric modulators of G-protein coupled receptors (GPCRs) interact with binding sites on the receptor molecule that are topographically distinct from the classic orthosteric site.
Gjoni, Tina
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Biomolecules, 2021 G-protein-coupled receptors (GPCRs) are the largest and most diverse group of cell surface receptors that respond to various extracellular signals. The allosteric modulation of GPCRs has emerged in recent years as a promising approach for developing ...
Tianling Hou +3 more
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Experimental GABA A Receptor Agonists and Allosteric Modulators for the Treatment of Focal Epilepsy
, 2021 Slobodan M Janković,1 Miralem Dješević,2 Snežana V Janković1 1Faculty of Medical Sciences, University of Kragujevac, Kragujevac, Serbia; 2Cardiology Department, Private Policlinic Center Eurofarm, Sarajevo, Bosnia and HercegovinaCorrespondence ...
Janković SM +5 more
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Allosteric Modulators for mGlu Receptors [PDF]
Current Neuropharmacology, 2007 The metabotropic glutamate receptor family comprises eight subtypes (mGlu1-8) of G-protein coupled receptors. mGlu receptors have a large extracellular domain which acts as recognition domain for the natural agonist glutamate. In contrast to the ionotropic glutamate receptors which mediate the fast excitatory neurotransmission, mGlu receptors have been
Gasparini, F, Spooren, W
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Chemical, target, and bioactive properties of allosteric modulation.
PLoS Computational Biology, 2014 Allosteric modulators are ligands for proteins that exert their effects via a different binding site than the natural (orthosteric) ligand site and hence form a conceptually distinct class of ligands for a target of interest.
Gerard J P van Westen +2 more
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Allosteric modulators targeting GPCRs
, 2020 The remarkable precision of the pharmacological modulation, including high degree of specificity, probe dependence, and signaling bias, confers to GPCR allosteric modulators unique advantages over orthosteric classical ligands.
María L. López-Rodríguez +5 more
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Current Advances in Allosteric Modulation of Muscarinic Receptors
Biomolecules, 2020 Allosteric modulators are ligands that bind to a site on the receptor that is spatially separated from the orthosteric binding site for the endogenous neurotransmitter.
Jan Jakubik, Esam E. El-Fakahany
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