Emerging paradigms in GPCR allostery: implications for drug discovery (Q38125563)

29 August 2017

title

Emerging paradigms in GPCR allostery: implications for drug discovery (English)

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G protein-coupled receptor

29 August 2017

main subject

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Denise Wootten

1

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29 August 2017

Arthur Christopoulos

series ordinal

2

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29 August 2017

Patrick M Sexton

series ordinal

3

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29 August 2017

publication date

1 August 2013

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Nature Reviews Drug Discovery

29 August 2017

published in

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29 August 2017

volume

12

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29 August 2017

issue

8

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29 August 2017

page(s)

630-644

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The 7 TM G-protein-coupled receptor target family

29 August 2017

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A novel multivalent ligand that bridges the allosteric and orthosteric binding sites of the M2 muscarinic receptor

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31 March 2020

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

31 March 2020

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Probing the molecular mechanism of interaction between 4-n-butyl-1-[4-(2-methylphenyl)-4-oxo-1-butyl]-piperidine (AC-42) and the muscarinic M(1) receptor: direct pharmacological evidence that AC-42 is an allosteric agonist

31 March 2020

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31 March 2020

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Mutagenic mapping suggests a novel binding mode for selective agonists of M1 muscarinic acetylcholine receptors

31 March 2020

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

31 March 2020

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Design, synthesis, and action of oxotremorine-related hybrid-type allosteric modulators of muscarinic acetylcholine receptors

31 March 2020

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31 March 2020

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Two-point kinetic experiments to quantify allosteric effects on radioligand dissociation

31 March 2020

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The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor

31 March 2020

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Ivermectin: a positive allosteric effector of the alpha7 neuronal nicotinic acetylcholine receptor.

31 March 2020

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Impact of species variability and 'probe-dependence' on the detection and in vivo validation of allosteric modulation at the M4 muscarinic acetylcholine receptor.

31 March 2020

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Structural determinants of allosteric agonism and modulation at the M4 muscarinic acetylcholine receptor: identification of ligand-specific and global activation mechanisms.

31 March 2020

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

31 March 2020

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Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophrenia

31 March 2020

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The many roles of chemokines and chemokine receptors in inflammation

31 March 2020

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The melanocortin-4 receptor: physiology, pharmacology, and pathophysiology.

31 March 2020

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Interaction of PTH and PTHrP with their receptors

31 March 2020

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Relaxin family peptide receptors--former orphans reunite with their parent ligands to activate multiple signalling pathways

31 March 2020

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International Union of Pharmacology. XXXII. The mammalian calcitonin gene-related peptides, adrenomedullin, amylin, and calcitonin receptors

31 March 2020

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Glucagon and glucagon-like peptide receptors as drug targets.

31 March 2020

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Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology.

31 March 2020

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Agonist and inverse agonist actions of beta-blockers at the human beta 2-adrenoceptor provide evidence for agonist-directed signaling

31 March 2020

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

31 March 2020

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A novel biased allosteric compound inhibitor of parturition selectively impedes the prostaglandin F2alpha-mediated Rho/ROCK signaling pathway

31 March 2020

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An acquired hypocalciuric hypercalcemia autoantibody induces allosteric transition among active human Ca-sensing receptor conformations.

31 March 2020

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Allostery in GPCRs: 'MWC' revisited.

31 March 2020

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31 March 2020

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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.

31 March 2020

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31 March 2020

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31 March 2020

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31 March 2020

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31 March 2020

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The relative activity of "function sparing" HIV-1 entry inhibitors on viral entry and CCR5 internalization: is allosteric functional selectivity a valuable therapeutic property?

31 March 2020

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The influence of CCL3L1 gene-containing segmental duplications on HIV-1/AIDS susceptibility

31 March 2020

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Functionally biased modulation of A(3) adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers

31 March 2020

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Acetylcholine metabolism at nerve-endings

31 March 2020

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Adenosine uptake, transport, and metabolism in human erythrocytes

31 March 2020

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The concentration of choline and the activities of cholinesterases, creatine kinase and lactate dehydrogenase in the blood plasma of piglets with the syndrome of splayleg (congenital myofibrillar hypoplasia)

31 March 2020

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Cardiac outflow of amino acids and purines during myocardial ischemia and reperfusion

31 March 2020

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GLP-1 (9-36) amide metabolite suppression of glucose production in isolated mouse hepatocytes

31 March 2020

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A Monod-Wyman-Changeux mechanism can explain G protein-coupled receptor (GPCR) allosteric modulation

31 March 2020

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Re-exploration of the PHCCC Scaffold: Discovery of Improved Positive Allosteric Modulators of mGluR4

31 March 2020

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Chemical switch of a metabotropic glutamate receptor 2 silent allosteric modulator into dual metabotropic glutamate receptor 2/3 negative/positive allosteric modulators

31 March 2020

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Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM.

31 March 2020

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

31 March 2020

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Crystal structure of rhodopsin: A G protein-coupled receptor

31 March 2020

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Crystal structure of the β2 adrenergic receptor-Gs protein complex

31 March 2020

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

31 March 2020

1 reference

Structure and dynamics of the M3 muscarinic acetylcholine receptor

31 March 2020

1 reference

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

31 March 2020

1 reference

Structure of the δ-opioid receptor bound to naltrindole

31 March 2020

1 reference

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

31 March 2020

1 reference

Structure of an agonist-bound human A2A adenosine receptor

31 March 2020

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

31 March 2020

1 reference

High-resolution crystal structure of human protease-activated receptor 1

31 March 2020

1 reference

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

31 March 2020

1 reference

Structure of the human histamine H1 receptor complex with doxepin

31 March 2020

1 reference

Crystal structure of the ligand-bound glucagon-like peptide-1 receptor extracellular domain

31 March 2020

1 reference

Molecular recognition of corticotropin-releasing factor by its G-protein-coupled receptor CRFR1

31 March 2020

1 reference

Structural views of the ligand-binding cores of a metabotropic glutamate receptor complexed with an antagonist and both glutamate and Gd3+.

31 March 2020

1 reference

Structures of the extracellular regions of the group II/III metabotropic glutamate receptors

31 March 2020

1 reference

Interactions of orthosteric and allosteric ligands with [3H]dimethyl-W84 at the common allosteric site of muscarinic M2 receptors

31 March 2020

1 reference

Allosteric interactions with muscarinic acetylcholine receptors: complex role of the conserved tryptophan M2422Trp in a critical cluster of amino acids for baseline affinity, subtype selectivity, and cooperativity

31 March 2020

1 reference

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

31 March 2020

1 reference

A binding pocket for a small molecule inhibitor of HIV-1 entry within the transmembrane helices of CCR5

31 March 2020

1 reference

Molecular interactions of cyclam and bicyclam non-peptide antagonists with the CXCR4 chemokine receptor

31 March 2020

1 reference

Structural and molecular interactions of CCR5 inhibitors with CCR5.

31 March 2020

1 reference

Identification of a putative intracellular allosteric antagonist binding-site in the CXC chemokine receptors 1 and 2.

31 March 2020

1 reference

An intracellular allosteric site for a specific class of antagonists of the CC chemokine G protein-coupled receptors CCR4 and CCR5.

31 March 2020

1 reference

Localization of agonist- and antagonist-binding domains of human corticotropin-releasing factor receptors

31 March 2020

1 reference

Point mutations in the transmembrane region of GABAB2 facilitate activation by the positive modulator N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) in the absence of the GABAB1 subunit.

31 March 2020

1 reference

The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxyiminocyclopropan[b]chromen-1a-carboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group I metabotropic glutamate recepto

31 March 2020

1 reference

Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site

31 March 2020

1 reference

Modeling and Mutagenesis of the Binding Site of Calhex 231, a Novel Negative Allosteric Modulator of the Extracellular Ca2+-sensing Receptor

31 March 2020

1 reference

Mutational analysis and molecular modeling of the allosteric binding site of a novel, selective, noncompetitive antagonist of the metabotropic glutamate 1 receptor

31 March 2020

1 reference

Homology modeling of the transmembrane domain of the human calcium sensing receptor and localization of an allosteric binding site

31 March 2020

1 reference

Targeting protease-activated receptor-1 with cell-penetrating pepducins in lung cancer

31 March 2020

1 reference

Pharmacology, biodistribution, and efficacy of GPCR-based pepducins in disease models.

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

Allosteric modulation of A2A adenosine receptors by amiloride analogues and sodium ions

31 March 2020

1 reference

Induced effects of sodium ions on dopaminergic G-protein coupled receptors

31 March 2020

1 reference

An ion-responsive motif in the second transmembrane segment of rhodopsin-like receptors

31 March 2020

1 reference

GPCRDB: information system for G protein-coupled receptors

31 March 2020

1 reference

Structural Basis for Allosteric Regulation of GPCRs by Sodium Ions

31 March 2020

1 reference

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

31 March 2020

1 reference

Receptors for dopamine and somatostatin: formation of hetero-oligomers with enhanced functional activity

31 March 2020

1 reference

Evidence for negative binding cooperativity within CCR5-CCR2b heterodimers.

31 March 2020

1 reference

Orexin-1 receptor-cannabinoid CB1 receptor heterodimerization results in both ligand-dependent and -independent coordinated alterations of receptor localization and function

31 March 2020

1 reference

Glucagon-like peptide-1 receptor dimerization differentially regulates agonist signaling but does not affect small molecule allostery.

31 March 2020

1 reference

Importance of lipid-exposed residues in transmembrane segment four for family B calcitonin receptor homo-dimerization

31 March 2020

1 reference

Dimerization in the absence of higher-order oligomerization of the G protein-coupled secretin receptor

31 March 2020

1 reference

Transmembrane segment IV contributes a functionally important interface for oligomerization of the Class II G protein-coupled secretin receptor.

31 March 2020

1 reference

Functional importance of a structurally distinct homodimeric complex of the family B G protein-coupled secretin receptor

31 March 2020

1 reference

Distinct roles of metabotropic glutamate receptor dimerization in agonist activation and G-protein coupling

31 March 2020

1 reference

Cinacalcet for secondary hyperparathyroidism in patients receiving hemodialysis

31 March 2020

1 reference

Clinical lessons from the calcium-sensing receptor

31 March 2020

1 reference

Efficacy of short-term monotherapy with maraviroc, a new CCR5 antagonist, in patients infected with HIV-1.

31 March 2020

1 reference

The discovery of the CCR5 receptor antagonist, UK-427,857, a new agent for the treatment of HIV infection and AIDS.

31 March 2020

1 reference

Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods.

31 March 2020

1 reference

12 December 2020

Modeling and mutational analysis of a putative sodium-binding pocket on the dopamine D2 receptor

1 reference

12 December 2020

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

1 reference

12 December 2020

Deal watch: Valuation benefits of structure-enabled drug discovery

1 reference

12 December 2020

Operational models of pharmacological agonism.

1 reference

12 December 2020

Probing of the location of the allosteric site on m1 muscarinic receptors by site-directed mutagenesis

1 reference

12 December 2020

Allosteric Modulation of G Protein–Coupled Receptors

1 reference

12 December 2020

An aspartate conserved among G-protein receptors confers allosteric regulation of alpha 2-adrenergic receptors by sodium

1 reference

12 December 2020

Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery

1 reference

12 December 2020

L-amino acid sensing by the extracellular Ca2+-sensing receptor

1 reference

12 December 2020

Spontaneous association between opioid receptors and GTP-binding regulatory proteins in native membranes: specific regulation by antagonists and sodium ions

1 reference

12 December 2020

Degradation of glucagon-like peptide-1 by human plasma in vitro yields an N-terminally truncated peptide that is a major endogenous metabolite in vivo

1 reference

12 December 2020

Identifiers

DOI

10.1038/NRD4052

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29 August 2017

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