Novel GPCR paradigms at the μ-opioid receptor (Q26864286)

G protein-coupled receptor

main subject

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M Canals

4

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Arthur Christopoulos

object named as

A Christopoulos

series ordinal

3

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author name string

G L Thompson

series ordinal

1

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E Kelly

series ordinal

2

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language of work or name

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January 2015

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British Journal of Pharmacology

published in

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volume

172

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issue

2

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page(s)

287-96

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Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor

cites work

1 reference

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Clinically employed opioid analgesics produce antinociception via μ-δ opioid receptor heteromers in Rhesus monkeys

21 March 2017

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The δ opioid receptor agonist SNC80 selectively activates heteromeric μ-δ opioid receptors

21 March 2017

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G-protein-coupled receptor heterodimerization modulates receptor function

21 March 2017

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Crystal structure of the µ-opioid receptor bound to a morphinan antagonist

21 March 2017

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

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ON THE NATURE OF ALLOSTERIC TRANSITIONS: A PLAUSIBLE MODEL

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Mediation of adenylyl cyclase sensitization by PTX-insensitive GalphaoA, Galphai1, Galphai2 or Galphai3.

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Lipo-endomorphin-1 derivatives with systemic activity against neuropathic pain without producing constipation

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ADP-ribosylation factor-dependent phospholipase D2 activation is required for agonist-induced mu-opioid receptor endocytosis

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

28 September 2017

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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.

28 September 2017

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Ligands that interact with putative MOR-mGluR5 heteromer in mice with inflammatory pain produce potent antinociception.

28 September 2017

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Bivalent ligands that target μ opioid (MOP) and cannabinoid1 (CB1) receptors are potent analgesics devoid of tolerance

28 September 2017

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

28 September 2017

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A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine

28 September 2017

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Differentiation of opioid drug effects by hierarchical multi-site phosphorylation

28 September 2017

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

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28 September 2017

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Cardiorenal actions of TRV120027, a novel ß-arrestin-biased ligand at the angiotensin II type I receptor, in healthy and heart failure canines: a novel therapeutic strategy for acute heart failure

28 September 2017

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The other side of opioid receptor signalling: regulation by protein-protein interaction

28 September 2017

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28 September 2017

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Agonist-selective patterns of µ-opioid receptor phosphorylation revealed by phosphosite-specific antibodies

28 September 2017

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N-naphthoyl-beta-naltrexamine (NNTA), a highly selective and potent activator of μ/kappa-opioid heteromers

28 September 2017

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

28 September 2017

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

28 September 2017

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μ-opioid receptors: correlation of agonist efficacy for signalling with ability to activate internalization

28 September 2017

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28 September 2017

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

28 September 2017

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GRIN1 regulates micro-opioid receptor activities by tethering the receptor and G protein in the lipid raft

28 September 2017

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A G protein-coupled receptor at work: the rhodopsin model.

28 September 2017

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G protein-coupled receptor hetero-dimerization: contribution to pharmacology and function

28 September 2017

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Agonist-selective, receptor-specific interaction of human P2Y receptors with beta-arrestin-1 and -2

28 September 2017

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

28 September 2017

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The evasive nature of drug efficacy: implications for drug discovery

28 September 2017

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

28 September 2017

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

28 September 2017

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Differential activation of G-proteins by mu-opioid receptor agonists

28 September 2017

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Opioid receptor homo- and heterodimerization in living cells by quantitative bioluminescence resonance energy transfer

28 September 2017

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Agonists activate Gi1 alpha or Gi2 alpha fused to the human mu opioid receptor differently

28 September 2017

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28 September 2017

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

28 September 2017

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28 September 2017

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Opioid agonists have different efficacy profiles for G protein activation, rapid desensitization, and endocytosis of mu-opioid receptors

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Distinct pharmacological properties of morphine metabolites at G(i)-protein and β-arrestin signaling pathways activated by the human μ-opioid receptor

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Functional selectivity and biased receptor signaling.

21 January 2018

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21 January 2018

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Overview of Receptor Allosterism

21 January 2018

1 reference

https://pubmed.ncbi.nlm.nih.gov/24460711

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

0 references

1 reference

PubMed publication ID

24460711

1 reference