Biased agonism at G protein-coupled receptors: the promise and the challenges--a medicinal chemistry perspective. (Q38209355)

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24796277%20AND%20SRC:MED&resulttype=core&format=json

17 March 2020

title

Biased agonism at G protein-coupled receptors: the promise and the challenges--a medicinal chemistry perspective (English)

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G protein-coupled receptor

17 March 2020

main subject

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1

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17 March 2020

Peter J. Scammells

3

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17 March 2020

Arthur Christopoulos

4

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17 March 2020

J. Robert Lane

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17 March 2020

author name string

Laura Lopez

2

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17 March 2020

Ben Capuano

5

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17 March 2020

publication date

5 May 2014

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Medicinal Research Reviews

17 March 2020

published in

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17 March 2020

volume

34

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17 March 2020

issue

6

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17 March 2020

page(s)

1286-1330

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24796277%20AND%20SRC:MED&resulttype=core&format=json

17 March 2020

1 reference

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

21 January 2018

1 reference

The GPCR Network: a large-scale collaboration to determine human GPCR structure and function

21 January 2018

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The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints

21 January 2018

1 reference

Allosteric binding sites on cell-surface receptors: novel targets for drug discovery

21 January 2018

1 reference

Allosteric Modulation of G Protein–Coupled Receptors

21 January 2018

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Allosteric modulation of G protein-coupled receptors: a pharmacological perspective.

21 January 2018

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Functional Selectivity and Biased Receptor Signaling

21 January 2018

1 reference

A simple method for quantifying functional selectivity and agonist bias

21 January 2018

1 reference

Collateral efficacy in drug discovery: taking advantage of the good (allosteric) nature of 7TM receptors

21 January 2018

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Beta-arrestin-biased ligands at seven-transmembrane receptors

21 January 2018

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Functional Selectivity and Classical Concepts of Quantitative Pharmacology

21 January 2018

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

21 January 2018

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G-protein-coupled receptors and signaling networks: emerging paradigms.

21 January 2018

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Efficacy at G-protein-coupled receptors

21 January 2018

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Conformational complexity of G-protein-coupled receptors

21 January 2018

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Activation of G protein-coupled receptors: beyond two-state models and tertiary conformational changes.

21 January 2018

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Constitutive activity and inverse agonists of G protein-coupled receptors: a current perspective

21 January 2018

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Structure-activity relationships of inverse agonists for G-protein-coupled receptors

21 January 2018

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

21 January 2018

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Inverse, protean, and ligand-selective agonism: matters of receptor conformation

21 January 2018

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

21 January 2018

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Agonist binding, agonist affinity and agonist efficacy at G protein-coupled receptors

21 January 2018

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Drug efficacy at G protein-coupled receptors

21 January 2018

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Emerging paradigms of β-arrestin-dependent seven transmembrane receptor signaling

21 January 2018

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Agonist efficacy and allosteric models of receptor action.

21 January 2018

1 reference

Signal transduction and functional selectivity of F15599, a preferential post-synaptic 5-HT1A receptor agonist

21 January 2018

1 reference

Agonist-selective endocytosis of mu opioid receptor by neurons in vivo

21 January 2018

1 reference

Morphine activates opioid receptors without causing their rapid internalization

21 January 2018

1 reference

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

21 January 2018

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Impedance responses reveal β₂-adrenergic receptor signaling pluridimensionality and allow classification of ligands with distinct signaling profiles

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

21 January 2018

1 reference

Functional selectivity of D2 receptor ligands in a Chinese hamster ovary hD2L cell line: evidence for induction of ligand-specific receptor states

21 January 2018

1 reference

Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists

21 January 2018

1 reference

Aripiprazole has functionally selective actions at dopamine D2 receptor-mediated signaling pathways.

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

21 January 2018

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

21 January 2018

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Differential kinetic and spatial patterns of beta-arrestin and G protein-mediated ERK activation by the angiotensin II receptor

21 January 2018

1 reference

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

21 January 2018

1 reference

Gonadotropin-releasing hormone receptor signaling: biased and unbiased

21 January 2018

1 reference

Biased agonism at the parathyroid hormone receptor: a demonstration of functional selectivity in bone metabolism

21 January 2018

1 reference

Independent beta-arrestin2 and Gq/protein kinase Czeta pathways for ERK stimulated by angiotensin type 1A receptors in vascular smooth muscle cells converge on transactivation of the epidermal growth factor receptor

21 January 2018

1 reference

Beta-arrestin2-mediated inotropic effects of the angiotensin II type 1A receptor in isolated cardiac myocytes

21 January 2018

1 reference

beta-Arrestin1 mediates nicotinic acid-induced flushing, but not its antilipolytic effect, in mice

21 January 2018

1 reference

Nicotinic acid receptor agonists differentially activate downstream effectors

21 January 2018

1 reference

Structure of the human κ-opioid receptor in complex with JDTic

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

Crystal structure of the β2 adrenergic receptor-Gs protein complex

21 January 2018

1 reference

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

21 January 2018

1 reference

Structure of the Adenosine A2A Receptor in Complex with ZM241385 and the Xanthines XAC and Caffeine

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

Structure of an agonist-bound human A2A adenosine receptor

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

Structure of the agonist-bound neurotensin receptor

21 January 2018

1 reference

Structural Features for Functional Selectivity at Serotonin Receptors

21 January 2018

1 reference

Structural Basis for Molecular Recognition at Serotonin Receptors

21 January 2018

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Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation

21 January 2018

1 reference

Activation and allosteric modulation of a muscarinic acetylcholine receptor

21 January 2018

1 reference

Molecular signatures of G-protein-coupled receptors

21 January 2018

1 reference

Inactive-state preassembly of G(q)-coupled receptors and G(q) heterotrimers

21 January 2018

1 reference

Differential G-protein-coupled receptor phosphorylation provides evidence for a signaling bar code.

21 January 2018

1 reference

Location, location, location...site-specific GPCR phosphorylation offers a mechanism for cell-type-specific signalling

21 January 2018

1 reference

Distinct phosphorylation sites on the β(2)-adrenergic receptor establish a barcode that encodes differential functions of β-arrestin.

21 January 2018

1 reference

Activation mechanism of the β2-adrenergic receptor

21 January 2018

1 reference

GPCR engineering yields high-resolution structural insights into beta2-adrenergic receptor function

21 January 2018

1 reference

Structural insights into agonist-induced activation of G-protein-coupled receptors

21 January 2018

1 reference

The structural basis of agonist-induced activation in constitutively active rhodopsin

21 January 2018

1 reference

Structure-function of the G protein-coupled receptor superfamily

21 January 2018

1 reference

The structure and function of G-protein-coupled receptors

21 January 2018

1 reference

Crystal structure of metarhodopsin II

21 January 2018

1 reference

Location of the retinal chromophore in the activated state of rhodopsin*.

21 January 2018

1 reference

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

21 January 2018

1 reference

Beta2 adrenergic receptor activation. Modulation of the proline kink in transmembrane 6 by a rotamer toggle switch

21 January 2018

1 reference

Involvement of Asn-293 in stereospecific agonist recognition and in activation of the beta 2-adrenergic receptor

21 January 2018

1 reference

The forgotten serine. A critical role for Ser-2035.42 in ligand binding to and activation of the beta 2-adrenergic receptor.

21 January 2018

1 reference

Ser203 as well as Ser204 and Ser207 in fifth transmembrane domain of the human beta2-adrenoceptor contributes to agonist binding and receptor activation

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

Structural insights into biased G protein-coupled receptor signaling revealed by fluorescence spectroscopy

21 January 2018

1 reference

Structure and conformational changes in the C-terminal domain of the beta2-adrenoceptor: insights from fluorescence resonance energy transfer studies

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

High-resolution distance mapping in rhodopsin reveals the pattern of helix movement due to activation

21 January 2018

1 reference

Conformational Changes in the G Protein-Coupled Receptor Rhodopsin Revealed by Histidine Hydrogen−Deuterium Exchange

21 January 2018

1 reference

Ligand-dependent perturbation of the conformational ensemble for the GPCR β2 adrenergic receptor revealed by HDX.

21 January 2018

1 reference

Dynamics of the beta2-adrenergic G-protein coupled receptor revealed by hydrogen-deuterium exchange

21 January 2018

1 reference

Multiple ligand-specific conformations of the β2-adrenergic receptor

21 January 2018

1 reference

Biased signaling pathways in β2-adrenergic receptor characterized by 19F-NMR.

21 January 2018

1 reference

Crystal Structures of a Stabilized β1-Adrenoceptor Bound to the Biased Agonists Bucindolol and Carvedilol

21 January 2018

1 reference

Morphine side effects in beta-arrestin 2 knockout mice

21 January 2018

1 reference

Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain.

21 January 2018

1 reference

Discovery of β-arrestin-biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy

21 January 2018

1 reference

Antagonism of dopamine D2 receptor/beta-arrestin 2 interaction is a common property of clinically effective antipsychotics.

21 January 2018

1 reference

Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes

21 January 2018

1 reference

An Akt/beta-arrestin 2/PP2A signaling complex mediates dopaminergic neurotransmission and behavior

21 January 2018

1 reference

Convergent evidence for impaired AKT1-GSK3beta signaling in schizophrenia

21 January 2018

1 reference

Lithium antagonizes dopamine-dependent behaviors mediated by an AKT/glycogen synthase kinase 3 signaling cascade

21 January 2018

1 reference

The Akt-GSK-3 signaling cascade in the actions of dopamine

21 January 2018

1 reference

Novel antipsychotic agents with dopamine autoreceptor agonist properties: synthesis and pharmacology of 7-[4-(4-phenyl-1-piperazinyl)butoxy]-3,4-dihydro-2(1H)-quinolinone derivatives

21 January 2018

1 reference

Structure-functional selectivity relationship studies of β-arrestin-biased dopamine D₂ receptor agonists

21 January 2018

1 reference

Advancing schizophrenia drug discovery: optimizing rodent models to bridge the translational gap.

21 January 2018

1 reference

An operational model of pharmacological agonism: the effect of E/[A] curve shape on agonist dissociation constant estimation. 1985.

21 January 2018

1 reference

A structure-activity analysis of biased agonism at the dopamine D2 receptor

21 January 2018

1 reference

Histidine 6.55 is a major determinant of ligand-biased signaling in dopamine D2L receptor.

21 January 2018

1 reference

Highly potent 5-aminotetrahydropyrazolopyridines: enantioselective dopamine D3 receptor binding, functional selectivity, and analysis of receptor-ligand interactions

21 January 2018

1 reference

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

21 January 2018

1 reference

Receptor conformations involved in dopamine D(2L) receptor functional selectivity induced by selected transmembrane-5 serine mutations

21 January 2018

1 reference

On the analysis of ligand-directed signaling at G protein-coupled receptors

21 January 2018

1 reference

Quantifying ligand bias at seven-transmembrane receptors.

21 January 2018

1 reference

Measurements of ligand bias and functional affinity.

21 January 2018

1 reference

Quantifying biased agonism: understanding the links between affinity and efficacy.

21 January 2018

1 reference

Signalling bias in new drug discovery: detection, quantification and therapeutic impact.

21 January 2018

1 reference

The role of histamine H4 receptor in immune and inflammatory disorders

21 January 2018

1 reference

Agonist-biased signaling at the histamine H4 receptor: JNJ7777120 recruits β-arrestin without activating G proteins.

21 January 2018

1 reference

Analysis of multiple histamine H₄ receptor compound classes uncovers Gαi protein- and β-arrestin2-biased ligands

21 January 2018

1 reference

G protein-coupled receptor allosterism and complexing

21 January 2018

1 reference

Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology.

21 January 2018

1 reference

Probe dependence in the allosteric modulation of a G protein-coupled receptor: implications for detection and validation of allosteric ligand effects

21 January 2018

1 reference

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

Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor.

21 January 2018

1 reference

A novel, conformation-specific allosteric inhibitor of the tachykinin NK2 receptor (NK2R) with functionally selective properties

21 January 2018

1 reference

Bridging the gap: bitopic ligands of G-protein-coupled receptors.

21 January 2018

1 reference

The best of both worlds? Bitopic orthosteric/allosteric ligands of g protein-coupled receptors

21 January 2018

1 reference

Orthosteric/allosteric bitopic ligands: going hybrid at GPCRs.

21 January 2018

1 reference

Rational design of dualsteric GPCR ligands: quests and promise

21 January 2018

1 reference

Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist

21 January 2018

1 reference

Dualsteric GPCR targeting: a novel route to binding and signaling pathway selectivity

21 January 2018

1 reference

An optical dynamic mass redistribution assay reveals biased signaling of dualsteric GPCR activators

21 January 2018

1 reference

Hybrid ortho/allosteric ligands for the adenosine A(1) receptor

21 January 2018

1 reference

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

21 January 2018

1 reference

H2 relaxin is a biased ligand relative to H3 relaxin at the relaxin family peptide receptor 3 (RXFP3).

21 January 2018

1 reference

Quantitative cell-based high-content screening for vasopressin receptor agonists using transfluor technology

21 January 2018

1 reference

Deciphering biased-agonism complexity reveals a new active AT1 receptor entity.

21 January 2018

1 reference

Probing heterotrimeric G protein activation: applications to biased ligands.

21 January 2018

1 reference

Quantification of ligand bias for clinically relevant β2-adrenergic receptor ligands: implications for drug taxonomy.

21 January 2018

1 reference

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

21 January 2018

1 reference

Exploring the mechanism of agonist efficacy: a relationship between efficacy and agonist dissociation rate at the muscarinic M3 receptor.

21 January 2018

1 reference

Functional efficacy of adenosine A₂A receptor agonists is positively correlated to their receptor residence time

21 January 2018

1 reference

Kinetics of 5-HT2B receptor signaling: profound agonist-dependent effects on signaling onset and duration

21 January 2018

1 reference

High-throughput screening of G protein-coupled receptor antagonists using a bioluminescence resonance energy transfer 1-based beta-arrestin2 recruitment assay

21 January 2018

1 reference

Beta galactosidase complementation: a cell-based luminescent assay platform for drug discovery

21 January 2018

1 reference

A homogeneous enzyme fragment complementation-based beta-arrestin translocation assay for high-throughput screening of G-protein-coupled receptors

21 January 2018

1 reference

The genetic design of signaling cascades to record receptor activation

21 January 2018

1 reference

G protein-independent cell-based assays for drug discovery on seven-transmembrane receptors

21 January 2018

1 reference

Impact of clinically relevant mutations on the pharmacoregulation and signaling bias of the calcium-sensing receptor by positive and negative allosteric modulators

21 January 2018

1 reference

Identification of molecular phenotypes and biased signaling induced by naturally occurring mutations of the human calcium-sensing receptor.

21 January 2018

1 reference

Stimulus bias provides evidence for conformational constraints in the structure of a G protein-coupled receptor

21 January 2018

1 reference

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

21 January 2018

1 reference

Functional selectivity of adenosine A1 receptor ligands?

21 January 2018

1 reference

Regulation of μ-opioid receptors: desensitization, phosphorylation, internalization, and tolerance.

21 January 2018

1 reference

Strategies to discover unexpected targets for drugs active at G protein-coupled receptors

21 January 2018

1 reference

Energy landscapes as a tool to integrate GPCR structure, dynamics, and function

21 January 2018

1 reference

21 January 2018

Identifiers

DOI

10.1002/MED.21318

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24796277%20AND%20SRC:MED&resulttype=core&format=json

17 March 2020

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