Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias
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Activation and allosteric modulation of a muscarinic acetylcholine receptorNovel GPCR paradigms at the μ-opioid receptorFunctional studies cast light on receptor statesBinding of N-methylscopolamine to the extracellular domain of muscarinic acetylcholine receptorsA dynamic view of molecular switch behavior at serotonin receptors: implications for functional selectivityA simple method for quantifying functional selectivity and agonist biasInvited review: GPCR structural characterization: Using fragments as building blocks to determine a complete structure.Exploring the mechanism of F282L mutation-caused constitutive activity of GPCR by a computational study.Divergent transducer-specific molecular efficacies generate biased agonism at a G protein-coupled receptor (GPCR)Estimation of ligand affinity constants for receptor states in functional studies involving the allosteric modulation of G protein-coupled receptors: implications for ligand bias.Structural determinants of allosteric agonism and modulation at the M4 muscarinic acetylcholine receptor: identification of ligand-specific and global activation mechanisms.Molecular mechanisms of bitopic ligand engagement with the M1 muscarinic acetylcholine receptorThe allosteric vestibule of a seven transmembrane helical receptor controls G-protein couplingQuantifying ligand bias at seven-transmembrane receptors.Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: implications for drug screening.A Monod-Wyman-Changeux mechanism can explain G protein-coupled receptor (GPCR) allosteric modulationDepolarization induces a conformational change in the binding site region of the M2 muscarinic receptorSecond extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) has a critical role in GLP-1 peptide binding and receptor activationSecond extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) differentially regulates orthosteric but not allosteric agonist binding and function.Allosteric modulator ORG27569 induces CB1 cannabinoid receptor high affinity agonist binding state, receptor internalization, and Gi protein-independent ERK1/2 kinase activationStimulus bias provides evidence for conformational constraints in the structure of a G protein-coupled receptorHuman Neuropeptide S Receptor Is Activated via a Gαq Protein-biased Signaling Cascade by a Human Neuropeptide S Analog Lacking the C-terminal 10 Residues.Therapeutic potential of β-arrestin- and G protein-biased agonists.Agonists with supraphysiological efficacy at the muscarinic M2 ACh receptor.Molecular properties of muscarinic acetylcholine receptors.Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 5 Based on Select Acetylenic Negative Allosteric Modulators.Muscarinic receptors as model targets and antitargets for structure-based ligand discovery.The pharmacology of TUG-891, a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), demonstrates both potential opportunity and possible challenges to therapeutic agonismFunctionally biased signalling properties of 7TM receptors - opportunities for drug development for the ghrelin receptor.Biased agonism as a mechanism for differential signaling by chemokine receptors.Orthosteric- and allosteric-induced ligand-directed trafficking at GPCRs.Challenges and advances in computational docking: 2009 in review.Ligand functional selectivity and quantitative pharmacology at G protein-coupled receptors.Molecular alliance-from orthosteric and allosteric ligands to dualsteric/bitopic agonists at G protein coupled receptors.Approaches for probing allosteric interactions at 7 transmembrane spanning receptors.Biased agonism at G protein-coupled receptors: the promise and the challenges--a medicinal chemistry perspective.Muscarinic acetylcholine receptors: novel opportunities for drug development.Structure-activity relationship studies of functionally selective kappa opioid receptor agonists that modulate ERK 1/2 phosphorylation while preserving G protein over βarrestin2 signaling bias.Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators.Ligand-Independent Adenosine A2B Receptor Constitutive Activity as a Promoter of Prostate Cancer Cell Proliferation.
P2860
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P2860
Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias
description
2010 nî lūn-bûn
@nan
2010 թուականի Յունուարին հրատարակուած գիտական յօդուած
@hyw
2010 թվականի հունվարին հրատարակված գիտական հոդված
@hy
2010年の論文
@ja
2010年論文
@yue
2010年論文
@zh-hant
2010年論文
@zh-hk
2010年論文
@zh-mo
2010年論文
@zh-tw
2010年论文
@wuu
name
Identification of orthosteric ...... igand-selective signaling bias
@ast
Identification of orthosteric ...... igand-selective signaling bias
@en
type
label
Identification of orthosteric ...... igand-selective signaling bias
@ast
Identification of orthosteric ...... igand-selective signaling bias
@en
prefLabel
Identification of orthosteric ...... igand-selective signaling bias
@ast
Identification of orthosteric ...... igand-selective signaling bias
@en
P2093
P2860
P356
P1476
Identification of orthosteric ...... igand-selective signaling bias
@en
P2093
Andrew B Tobin
Arthur Christopoulos
Karen J Gregory
Nathan E Hall
Patrick M Sexton
P2860
P304
P356
10.1074/JBC.M109.094011
P407
P577
2010-01-05T00:00:00Z