Inverse agonism at G protein-coupled receptors: (patho)physiological relevance and implications for drug discovery (Q33898777)

29 July 2017

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title

Inverse agonism at G protein-coupled receptors: (patho)physiological relevance and implications for drug discovery (English)

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G protein-coupled receptor

29 July 2017

main subject

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1 reference

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R A de Ligt

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29 July 2017

A P Kourounakis

series ordinal

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29 July 2017

A P IJzerman

series ordinal

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29 July 2017

language of work or name

English

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publication date

1 May 2000

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British Journal of Pharmacology

29 July 2017

published in

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29 July 2017

volume

130

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29 July 2017

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29 July 2017

page(s)

1-12

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ON THE NATURE OF ALLOSTERIC TRANSITIONS: A PLAUSIBLE MODEL

29 July 2017

cites work

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5 July 2018

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5 July 2018

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5 July 2018

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5 July 2018

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Ligand-induced overexpression of a constitutively active beta2-adrenergic receptor: pharmacological creation of a phenotype in transgenic mice

5 July 2018

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5 July 2018

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Inverse agonist-induced up-regulation of the human beta2-adrenoceptor in transfected neuroblastoma X glioma hybrid cells.

5 July 2018

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5 July 2018

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Functional evidence of inverse agonism in vascular smooth muscle

5 July 2018

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Defects in G protein-coupled signal transduction in human disease

5 July 2018

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Inverse agonism of amino-terminally truncated parathyroid hormone (PTH) and PTH-related peptide (PTHrP) analogs revealed with constitutively active mutant PTH/PTHrP receptors

5 July 2018

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Constitutively activated receptors for parathyroid hormone and parathyroid hormone-related peptide in Jansen's metaphyseal chondrodysplasia

5 July 2018

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Inverse agonism of histamine H2 antagonist accounts for upregulation of spontaneously active histamine H2 receptors

5 July 2018

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5 July 2018

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5 July 2018

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5 July 2018

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Antagonists of bradykinin that stabilize a G-protein-uncoupled state of the B2 receptor act as inverse agonists in rat myometrial cells.

5 July 2018

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5 July 2018

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5 July 2018

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5 July 2018

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5 July 2018

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5 July 2018

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A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor

5 July 2018

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Effects of drugs on beta-adrenergic receptors on human lymphocytes

5 July 2018

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Reciprocal modulation of agonist and antagonist binding to inhibitory adenosine receptors by 5'-guanylylimidodiphosphate and monovalent cations

5 July 2018

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The relationship between muscarinic receptor occupancy and adenylate cyclase inhibition in the rabbit myocardium

5 July 2018

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A1 adenosine receptor-G protein coupling in bovine brain membranes: effects of guanine nucleotides, salt, and solubilization

5 July 2018

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Regulation of porcine brain alpha 2-adrenergic receptors by Na+,H+ and inhibitors of Na+/H+ exchange

5 July 2018

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Sodium ions increase the binding of the antagonist peptide ICI 174864 to the delta-opiate receptor

5 July 2018

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Certain beta-blockers can decrease beta-adrenergic receptor number: II. Down-regulation of receptor number by alprenolol and propranolol in cultured lymphoma and muscle cells

5 July 2018

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Antagonist-induced opioid receptor up-regulation. II. Regionally specific modulation of mu, delta and kappa binding sites in rat brain revealed by quantitative autoradiography

5 July 2018

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Differences in the GTP-regulation of membrane-bound and solubilized A1-adenosine receptors

5 July 2018

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

5 July 2018

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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=1572052

Na+ regulation of formyl peptide receptor-mediated signal transduction in HL 60 cells. Evidence that the cation prevents activation of the G-protein by unoccupied receptors

5 July 2018

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Regions of the alpha 1-adrenergic receptor involved in coupling to phosphatidylinositol hydrolysis and enhanced sensitivity of biological function

5 July 2018

1 reference

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

5 July 2018

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Sodium-dependent isomerization of dopamine D-2 receptors characterized using [125I]epidepride, a high-affinity substituted benzamide ligand.

5 July 2018

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Mapping of a functional autoimmune epitope on the beta 1-adrenergic receptor in patients with idiopathic dilated cardiomyopathy

5 July 2018

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Beta 2-adrenergic receptor antibodies in myasthenia gravis

5 July 2018

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Guanine nucleotides modulate muscarinic receptor binding in the heart

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=1572052

Agonist-specific effects of monovalent and divalent cations on adenylate cyclase-coupled alpha adrenergic receptors in rabbit platelets

5 July 2018

1 reference

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SR 141716A, a cannabinoid receptor antagonist, produces hyperalgesia in untreated mice

5 July 2018

1 reference

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Agonist-independent effects of muscarinic antagonists on Ca2+ and K+ currents in frog and rat cardiac cells

29 October 2018

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Histamine H1-receptor binding sites in guinea pig brain membranes: regulation of agonist interactions by guanine nucleotides and cations

29 October 2018

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29 October 2018

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The ternary complex model. Its properties and application to ligand interactions with the D2-dopamine receptor of the anterior pituitary gland

29 October 2018

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Two affinity states of Ri adenosine receptors in brain membranes. Analysis of guanine nucleotide and temperature effects on radioligand binding.

29 October 2018

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Interaction at End-Plate Receptors between Different Choline Derivatives

29 October 2018

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Reciprocal modulation of agonist and antagonist binding to A1 adenosine receptors by guanine nucleotides is mediated via a pertussis toxin-sensitive G protein

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Induction of a pharmacologically active clonotypic B cell response directed to an immunogenic region of the human beta 2-adrenergic receptor

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Agonist-independent inhibition of G protein activation by muscarinic acetylcholine receptor antagonists in cardiac membranes

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Activation of calcium currents in cardiac myocytes by empty beta-adrenoceptors

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Autoantibodies against cardiac G-protein-coupled receptors define different populations with cardiomyopathies but not with hypertension

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Unoccupied beta-adrenoceptor-induced adenylyl cyclase stimulation in turkey erythrocyte membranes

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

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Human calcitonin receptors exhibit agonist-independent (constitutive) signaling activity

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Pharmacology of muscarinic receptor subtypes constitutively activated by G proteins

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A Selective Inverse Agonist for Central Cannabinoid Receptor Inhibits Mitogen-activated Protein Kinase Activation Stimulated by Insulin or Insulin-like Growth Factor 1

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Protean agonism at alpha2A-adrenoceptors

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Agonist-independent regulation of constitutively active G-protein-coupled receptors

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SR 141716A acts as an inverse agonist to increase neuronal voltage-dependent Ca2+ currents by reversal of tonic CB1 cannabinoid receptor activity

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12 December 2020

Modulation of CB1 cannabinoid receptor functions after a long-term exposure to agonist or inverse agonist in the Chinese hamster ovary cell expression system

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Identifiers

DOI

10.1038/SJ.BJP.0703311

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29 July 2017

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29 July 2017

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