Ligand functional selectivity and quantitative pharmacology at G protein-coupled receptors (Q38014954)

27 August 2017

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Ligand functional selectivity and quantitative pharmacology at G protein-coupled receptors (English)

1 reference

G protein-coupled receptor

27 August 2017

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1 reference

Michel Bouvier

3

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author name string

Wayne Stallaert

series ordinal

1

1 reference

PubMed ID

22651124

27 August 2017

Arthur Christopoulos

series ordinal

2

1 reference

PubMed ID

22651124

27 August 2017

language of work or name

English

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publication date

24 May 2011

1 reference

Expert Opinion on Drug Discovery

27 August 2017

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27 August 2017

6

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27 August 2017

8

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27 August 2017

811-825

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G protein-coupled receptors: novel targets for drug discovery in cancer

27 August 2017

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Seven-transmembrane receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

A modification of receptor theory

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Efficacy as a vector: the relative prevalence and paucity of inverse agonism

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the beta 2-adrenoceptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Biochemical and pharmacological control of the multiplicity of coupling at G-protein-coupled receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

GPCR interacting proteins (GIP).

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

G protein-coupled receptor interacting proteins: emerging roles in localization and signal transduction

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Agonist-receptor efficacy. II. Agonist trafficking of receptor signals

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Differential signal transduction by five splice variants of the PACAP receptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Functional selectivity of dopamine receptor agonists. I. Selective activation of postsynaptic dopamine D2 receptors linked to adenylate cyclase

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Functional selectivity of dopamine receptor agonists. II. Actions of dihydrexidine in D2L receptor-transfected MN9D cells and pituitary lactotrophs

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Ligand-directed signaling at the beta3-adrenoceptor produced by 3-(2-Ethylphenoxy)-1-[(1,S)-1,2,3,4-tetrahydronapth-1-ylamino]-2S-2-propanol oxalate (SR59230A) relative to receptor agonists.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Constitutive activity of the serotonin2C receptor inhibits in vivo dopamine release in the rat striatum and nucleus accumbens.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Differential signaling of the endogenous agonists at the beta2-adrenergic receptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Differential desensitization, receptor phosphorylation, beta-arrestin recruitment, and ERK1/2 activation by the two endogenous ligands for the CC chemokine receptor 7.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Functional selectivity of melanocortin 4 receptor peptide and nonpeptide agonists: evidence for ligand-specific conformational states.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Teaching old receptors new tricks: biasing seven-transmembrane receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Beyond desensitization: physiological relevance of arrestin-dependent signaling.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Selectively engaging β-arrestins at the angiotensin II type 1 receptor reduces blood pressure and increases cardiac performance.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Beta-arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G protein-coupled receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Characterization of serotonin 5-HT2C receptor signaling to extracellular signal-regulated kinases 1 and 2.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Internalization and Src activity regulate the time course of ERK activation by delta opioid receptor ligands.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Distinct signaling profiles of beta1 and beta2 adrenergic receptor ligands toward adenylyl cyclase and mitogen-activated protein kinase reveals the pluridimensionality of efficacy

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

A unique mechanism of beta-blocker action: carvedilol stimulates beta-arrestin signaling

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Beta-blockers in heart failure: are pharmacological differences clinically important?

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Desensitization of G protein-coupled receptors and neuronal functions

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Clathrin-dependent mechanisms of G protein-coupled receptor endocytosis

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Agonist-selective mechanisms of GPCR desensitization

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Mass spectrometric analysis of agonist effects on posttranslational modifications of the beta-2 adrenoceptor in mammalian cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Identification of a potent and highly efficacious, yet slowly desensitizing CB1 cannabinoid receptor agonist

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Rapid desensitization of the serotonin(2C) receptor system: effector pathway and agonist dependence

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Agonist- and antagonist-induced sequestration/internalization of neuropeptide Y Y1 receptors in HEK293 cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Activation-independent parathyroid hormone receptor internalization is regulated by NHERF1 (EBP50).

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

The endothelin subtype A receptor undergoes agonist- and antagonist-mediated internalization in the absence of signaling

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Paradoxical trafficking and regulation of 5-HT(2A) receptors by agonists and antagonists

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Ligand-directed trafficking of the δ-opioid receptor in vivo: two paths toward analgesic tolerance

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

New concepts in drug discovery: collateral efficacy and permissive antagonism

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Agonist-induced phosphorylation of the angiotensin II (AT(1A)) receptor requires generation of a conformation that is distinct from the inositol phosphate-signaling state

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Selective engagement of G protein coupled receptor kinases (GRKs) encodes distinct functions of biased ligands

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Agonist-selective mechanisms of mu-opioid receptor desensitization in human embryonic kidney 293 cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Morphine-activated opioid receptors elude desensitization by beta-arrestin

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Morphine-induced mu-opioid receptor rapid desensitization is independent of receptor phosphorylation and beta-arrestins

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Reduced development of tolerance to the analgesic effects of morphine and clonidine in PKC gamma mutant mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Determination of the role of conventional, novel and atypical PKC isoforms in the expression of morphine tolerance in mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

G-protein receptor kinase 3 (GRK3) influences opioid analgesic tolerance but not opioid withdrawal

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Endocytosis of the mu opioid receptor reduces tolerance and a cellular hallmark of opiate withdrawal

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

The role of conformational ensembles of seven transmembrane receptors in functional selectivity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Conformational complexity of G-protein-coupled receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Differential transcriptional activation in vitro by NF-kappa B/Rel proteins

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Sequential binding of agonists to the beta2 adrenoceptor. Kinetic evidence for intermediate conformational states

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Functionally different agonists induce distinct conformations in the G protein coupling domain of the beta 2 adrenergic receptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Coupling ligand structure to specific conformational switches in the beta2-adrenoceptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Molecular basis of inverse agonism in a G protein-coupled receptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Distinct structural changes in a G protein-coupled receptor caused by different classes of agonist ligands

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Ligand-specific changes in M3 muscarinic acetylcholine receptor structure detected by a disulfide scanning strategy

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Bioluminescence resonance energy transfer assays reveal ligand-specific conformational changes within preformed signaling complexes containing delta-opioid receptors and heterotrimeric G proteins.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Direct Observation of G-protein Binding to the Human δ-Opioid Receptor Using Plasmon-Waveguide Resonance Spectroscopy

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

The effect of ligand efficacy on the formation and stability of a GPCR-G protein complex

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Probing the activation-promoted structural rearrangements in preassembled receptor-G protein complexes.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Independent beta-arrestin 2 and G protein-mediated pathways for angiotensin II activation of extracellular signal-regulated kinases 1 and 2.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Conformational rearrangements and signaling cascades involved in ligand-biased mitogen-activated protein kinase signaling through the beta1-adrenergic receptor.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

The structure and function of G-protein-coupled receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Structure of the Human Dopamine D3 Receptor in Complex with a D2/D3 Selective Antagonist

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Crystal structure of the human beta2 adrenergic G-protein-coupled receptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Structure of a beta1-adrenergic G-protein-coupled receptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Structure of a nanobody-stabilized active state of the β(2) adrenoceptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Structure and function of an irreversible agonist-β(2) adrenoceptor complex

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

The structural basis for agonist and partial agonist action on a β(1)-adrenergic receptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Highly conserved tyrosine stabilizes the active state of rhodopsin

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Prediction of functionally selective allosteric interactions at an M3 muscarinic acetylcholine receptor mutant using Saccharomyces cerevisiae

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Detection of novel functional selectivity at M3 muscarinic acetylcholine receptors using a Saccharomyces cerevisiae platform

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Determination of adenosine A1 receptor agonist and antagonist pharmacology using Saccharomyces cerevisiae: implications for ligand screening and functional selectivity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Use of a cAMP BRET sensor to characterize a novel regulation of cAMP by the sphingosine 1-phosphate/G13 pathway

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Monitoring agonist-promoted conformational changes of beta-arrestin in living cells by intramolecular BRET.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Combining resonance energy transfer methods reveals a complex between the alpha2A-adrenergic receptor, Galphai1beta1gamma2, and GRK2.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Fusion of Aequorea victoria GFP and aequorin provides their Ca(2+)-induced interaction that results in red shift of GFP absorption and efficient bioluminescence energy transfer.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Characterization of serotonin 5-hydroxytryptamine-1A receptor activation using a phospho-extracellular-signal regulated kinase 2 sensor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Visualization of JNK activity dynamics with a genetically encoded fluorescent biosensor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Visualization of PKA activity in plasma membrane microdomains

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Heterogeneity of phosphatidic acid levels and distribution at the plasma membrane in living cells as visualized by a Föster resonance energy transfer (FRET) biosensor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Imaging in real-time with FRET the redox response of tumorigenic cells to glutathione perturbations in a microscale flow.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

A genetically encoded fluorescent sensor of ERK activity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Multiplexing of multicolor bioluminescence resonance energy transfer

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Label-free whole-cell assays: expanding the scope of GPCR screening

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Real-time monitoring of morphological changes in living cells by electronic cell sensor arrays: an approach to study G protein-coupled receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Non-invasive optical biosensor for assaying endogenous G protein-coupled receptors in adherent cells.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Deconvolution of complex G protein-coupled receptor signaling in live cells using dynamic mass redistribution measurements.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Evaluating cellular impedance assays for detection of GPCR pleiotropic signaling and functional selectivity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

A 100K well screen for a muscarinic receptor using the Epic label-free system--a reflection on the benefits of the label-free approach to screening seven-transmembrane receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Enhanced selectivity screening of GPCR ligands using a label-free cell based assay technology

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Delineating the mode of action of adenosine A1 receptor allosteric modulators

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

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.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Quantification of functional selectivity at the human α(1A)-adrenoceptor.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Selectivity of agonists for the active state of M1 to M4 muscarinic receptor subtypes

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

Assessing the distribution of parameters in models of ligand-receptor interaction: to log or not to log.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2011.586691

10.1517/17460441.2011.586691

21 January 2018

Identifiers

DOI

1 reference

27 August 2017

1 reference

PubMed ID

22651124