Pepducin targeting the C-X-C chemokine receptor type 4 acts as a biased agonist favoring activation of the inhibitory G protein.
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Allosteric Modulation of Chemoattractant ReceptorsBiased and g protein-independent signaling of chemokine receptorsMonitoring G protein-coupled receptor and β-arrestin trafficking in live cells using enhanced bystander BRETData on human neutrophil activation induced by pepducins with amino acid sequences derived from β2AR and CXCR4Minireview: Spatial Programming of G Protein-Coupled Receptor Activity: Decoding Signaling in Health and DiseaseA Pluridimensional View of Biased Agonism.Development and characterization of pepducins as Gs-biased allosteric agonists.A pepducin derived from the third intracellular loop of FPR2 is a partial agonist for direct activation of this receptor in neutrophils but a full agonist for cross-talk triggered reactivation of FPR2.Allosteric Activation of a G Protein-coupled Receptor with Cell-penetrating Receptor MimeticsReceptor sequestration in response to β-arrestin-2 phosphorylation by ERK1/2 governs steady-state levels of GPCR cell-surface expression.β-arrestin-biased signaling through the β2-adrenergic receptor promotes cardiomyocyte contraction.Discovery and characterization of novel small-molecule CXCR4 receptor agonists and antagonistsBiasing GPCR signaling from inside.Harnessing allostery: a novel approach to drug discovery.Allosteric and biased g protein-coupled receptor signaling regulation: potentials for new therapeutics.Multiple functions of G protein-coupled receptor kinasesFunctional New World monkey oxytocin forms elicit an altered signaling profile and promotes parental care in rats.Signaling bias in drug discovery.Pepducins and Other Lipidated Peptides as Mechanistic Probes and Therapeutics.Targeting Liver Fibrosis with a Cell-penetrating Protease-activated Receptor-2 (PAR2) Pepducin.Evolutionary action and structural basis of the allosteric switch controlling β2AR functional selectivity.Biased signalling: from simple switches to allosteric microprocessors.A synthetic intrabody-based selective and generic inhibitor of GPCR endocytosis.Design, synthesis, and biological evaluation of CXCR4 ligands.G Protein-Coupled Receptor Kinase 3 and Protein Kinase C Phosphorylate the Distal C-Terminal Tail of the Chemokine Receptor CXCR4 and Mediate Recruitment of β-Arrestin.CXCL14 is no direct modulator of CXCR4.A single amino acid substitution in CXCL12 confers functional selectivity at the beta-arrestin level.Bioluminescence resonance energy transfer-based biosensors allow monitoring of ligand- and transducer-mediated GPCR conformational changesSpatiotemporal regulation of the GPCR activity of BAI3 by C1qL4 and Stabilin-2 controls myoblast fusion
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Pepducin targeting the C-X-C chemokine receptor type 4 acts as a biased agonist favoring activation of the inhibitory G protein.
description
article científic
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article scientifique
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articolo scientifico
@it
artigo científico
@pt
bilimsel makale
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scientific article published on 05 December 2013
@en
vedecký článok
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vetenskaplig artikel
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videnskabelig artikel
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vědecký článek
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name
Pepducin targeting the C-X-C c ...... n of the inhibitory G protein.
@en
Pepducin targeting the C-X-C c ...... n of the inhibitory G protein.
@nl
type
label
Pepducin targeting the C-X-C c ...... n of the inhibitory G protein.
@en
Pepducin targeting the C-X-C c ...... n of the inhibitory G protein.
@nl
prefLabel
Pepducin targeting the C-X-C c ...... n of the inhibitory G protein.
@en
Pepducin targeting the C-X-C c ...... n of the inhibitory G protein.
@nl
P2093
P2860
P356
P1476
Pepducin targeting the C-X-C c ...... n of the inhibitory G protein.
@en
P2093
Jay M Janz
Jeffrey L Benovic
Jiansong Luo
Julie Quoyer
Kenneth E Carlson
Stephen W Hunt
Sylvain Armando
Viktoria Lukashova
P2860
P304
P356
10.1073/PNAS.1312515110
P407
P577
2013-12-05T00:00:00Z