A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand. (Q39947679)

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English	A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand.	scientific article

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12 January 2020

A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand (English)

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12 January 2020

G protein-coupled receptor

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Patrick M. Sexton

6

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12 January 2020

1

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12 January 2020

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12 January 2020

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Karen J Gregory

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12 January 2020

Nathan E Hall

3

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12 January 2020

Peter J Scammells

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12 January 2020

Arthur Christopoulos

7

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12 January 2020

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22 August 2008

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12 January 2020

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10

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Journal of Biological Chemistry

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12 January 2020

283

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12 January 2020

43

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12 January 2020

29312-29321

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12 January 2020

Structural diversity of G protein-coupled receptors and significance for drug discovery

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High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor

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Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology.

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22 September 2017

Estimation of agonist activity at G protein-coupled receptors: analysis of M2 muscarinic receptor signaling through Gi/o,Gs, and G15.

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Allosteric agonists of 7TM receptors: expanding the pharmacological toolbox

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22 September 2017

Functional Selectivity and Classical Concepts of Quantitative Pharmacology

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22 September 2017

Molecular mechanisms of ligand binding, signaling, and regulation within the superfamily of G-protein-coupled receptors: molecular modeling and mutagenesis approaches to receptor structure and function

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22 September 2017

N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl- d -aspartate receptor activity

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22 September 2017

G protein-coupled receptor allosterism and complexing

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Seven-transmembrane receptors: crystals clarify

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Crystal structure of rhodopsin: A G protein-coupled receptor

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22 September 2017

Qualitative and quantitative assessment of relative agonist efficacy

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Biased probability Monte Carlo conformational searches and electrostatic calculations for peptides and proteins

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22 September 2017

The effect of McN-A-343 on muscarinic receptors in the cerebral cortex and heart

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22 September 2017

Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction

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Drugs from emasculated hormones: the principle of syntopic antagonism

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22 September 2017

Dimethylsulfonium analogues of the muscarinic agent McN-A-343: [4-[[N-(3- or 4-halophenyl)carbamoyl]oxy]-2-butynyl] dimethylsulfonium perchlorates

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A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding

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22 September 2017

Site-directed mutagenesis of the putative human muscarinic M2 receptor binding site

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25 September 2017

International Union of Pharmacology. XVII. Classification of muscarinic acetylcholine receptors.

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15 June 2018

Estimation of partial agonist affinity by interaction with a full agonist: a direct operational model-fitting approach

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Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: interactions of strychnine and acetylcholine at muscarinic receptors

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Allosteric binding sites on muscarinic acetylcholine receptors

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Probing the beta2 adrenoceptor binding site with catechol reveals differences in binding and activation by agonists and partial agonists

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Pharmacological analysis of the mode of interaction of McN-A-343 at atrial muscarinic M2 receptors

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Allosteric Modulation of G Protein–Coupled Receptors

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21 January 2018

Critical Role for the Second Extracellular Loop in the Binding of Both Orthosteric and Allosteric G Protein-coupled Receptor Ligands

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21 January 2018

Evidence for a multiple binding mode of bispyridinium-type allosteric modulators of muscarinic receptors

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Transducer abstraction: a novel approach to the detection of partial agonist efficacy in radioligand binding studies

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Structure-activity relationships among a series of acetylenic carbamates related to McN-A343

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Identification of drugs competing with d-tubocurarine for an allosteric site on cardiac muscarinic receptors

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Subtype selectivity of the positive allosteric action of alcuronium at cloned M1-M5 muscarinic acetylcholine receptors

1 reference

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12 December 2020

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Mutations of aspartate 103 in the Hm2 receptor and alterations in receptor binding properties of muscarinic agonists

1 reference

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An unusual type of sympathetic ganglionic stimulant

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10.1074/JBC.M803801200

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12 January 2020

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12 January 2020

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