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

scientific article

A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand. is …
instance of (P31):
scholarly articleQ13442814

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P356DOI10.1074/JBC.M803801200
P932PMC publication ID2662018
P698PubMed publication ID18723515

P50authorCeline ValantQ56938593
Michael LewQ67255069
Patrick M. SextonQ39936838
P2093author name stringNathan E Hall
Karen J Gregory
Arthur Christopoulos
Peter J Scammells
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Qualitative and quantitative assessment of relative agonist efficacyQ28142282
Dimethylsulfonium analogues of the muscarinic agent McN-A-343: [4-[[N-(3- or 4-halophenyl)carbamoyl]oxy]-2-butynyl] dimethylsulfonium perchloratesQ28339969
Structural diversity of G protein-coupled receptors and significance for drug discoveryQ29616716
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G protein-coupled receptor allosterism and complexingQ34523552
Seven-transmembrane receptors: crystals clarifyQ34552623
The effect of McN-A-343 on muscarinic receptors in the cerebral cortex and heartQ36097563
Allosteric agonists of 7TM receptors: expanding the pharmacological toolboxQ36556801
Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology.Q36880915
N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl- d -aspartate receptor activityQ37089832
Drugs from emasculated hormones: the principle of syntopic antagonismQ38360052
Estimation of agonist activity at G protein-coupled receptors: analysis of M2 muscarinic receptor signaling through Gi/o,Gs, and G15.Q40152913
Site-directed mutagenesis of the putative human muscarinic M2 receptor binding siteQ40924610
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.Q42277559
Estimation of partial agonist affinity by interaction with a full agonist: a direct operational model-fitting approachQ42920913
International Union of Pharmacology. XVII. Classification of muscarinic acetylcholine receptors.Q45345827
Probing the beta2 adrenoceptor binding site with catechol reveals differences in binding and activation by agonists and partial agonistsQ46427567
Allosteric binding sites on muscarinic acetylcholine receptorsQ46720566
Pharmacological analysis of the mode of interaction of McN-A-343 at atrial muscarinic M2 receptorsQ46887583
Structure-function studies of allosteric agonism at M2 muscarinic acetylcholine receptors.Q51797215
Assessing the distribution of parameters in models of ligand-receptor interaction: to log or not to log.Q52233618
Allosteric Modulation of G Protein–Coupled ReceptorsQ56115675
P433issue43
P407language of work or nameEnglishQ1860
P921main subjectG protein-coupled receptorQ38173
P1104number of pages10
P304page(s)29312-29321
P577publication date2008-08-22
P1433published inJournal of Biological ChemistryQ867727
P1476titleA novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand
P478volume283

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