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Open AccessGRK specificity and Gβγ dependency determines the potential of a GPCR for arrestin-biased agonism
G protein-coupled receptors (GPCRs) are mainly regulated by GPCR kinase (GRK) phosphorylation and subsequent β-arrestin recruitment. The ubiquitously expressed GRKs are classified into cytosolic GRK2/3 and mem...
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Article
Open AccessSystematic assessment of chemokine ligand bias at the human chemokine receptor CXCR2 indicates G protein bias over β-arrestin recruitment and receptor internalization
The human CXC chemokine receptor 2 (CXCR2) is a G protein-coupled receptor (GPCR) interacting with multiple chemokines (i.e., CXC chemokine ligands CXCL1-3 and CXCL5-8). It is involved in inflammatory diseases as...
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Open AccessReply to: How carvedilol does not activate β2-adrenoceptors
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Open AccessHow Carvedilol activates β2-adrenoceptors
Carvedilol is among the most effective β-blockers for improving survival after myocardial infarction. Yet the mechanisms by which carvedilol achieves this superior clinical profile are still unclear. Beyond bl...
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Article
Open AccessComputationally designed GPCR quaternary structures bias signaling pathway activation
Communication across membranes controls critical cellular processes and is achieved by receptors translating extracellular signals into selective cytoplasmic responses. While receptor tertiary structures can b...
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Open AccessThe natural analgesic conolidine targets the newly identified opioid scavenger ACKR3/CXCR7
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Open AccessThe atypical chemokine receptor ACKR3/CXCR7 is a broad-spectrum scavenger for opioid peptides
Endogenous opioid peptides and prescription opioid drugs modulate pain, anxiety and stress by activating opioid receptors, currently classified into four subtypes. Here we demonstrate that ACKR3/CXCR7, hithert...
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Open AccessAurora A plays a dual role in migration and survival of human glioblastoma cells according to the CXCL12 concentration
Primary glioblastoma is the most frequent human brain tumor in adults and is generally fatal due to tumor recurrence. We previously demonstrated that glioblastoma-initiating cells invade the subventricular zon...