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  1. Article

    Open Access

    GRK 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...

    Edda S. F. Matthees, Jenny C. Filor, Natasha Jaiswal in Communications Biology (2024)

  2. Article

    Open Access

    Systematic 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...

    Katrijn Boon, Nathan Vanalken, Martyna Szpakowska in Cell Communication and Signaling (2024)

  3. Article

    Open Access

    Reply to: How carvedilol does not activate β2-adrenoceptors

    Evi Kostenis, Jesus Gomeza, Elke Miess-Tanneberg in Nature Communications (2023)

  4. Article

    Open Access

    How 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...

    Tobias Benkel, Mirjam Zimmermann, Julian Zeiner, Sergi Bravo in Nature Communications (2022)

  5. Article

    Open Access

    Computationally 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...

    Justine S. Paradis, **ang Feng, Brigitte Murat in Nature Communications (2022)

  6. Article

    Open Access

    The natural analgesic conolidine targets the newly identified opioid scavenger ACKR3/CXCR7

    Martyna Szpakowska, Ann M. Decker, Max Meyrath in Signal Transduction and Targeted Therapy (2021)

  7. Article

    Open Access

    The 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...

    Max Meyrath, Martyna Szpakowska, Julian Zeiner, Laurent Massotte in Nature Communications (2020)

  8. Article

    Open Access

    Aurora 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...

    Estelle Willems, Matthias Dedobbeleer, Marina Digregorio, Arnaud Lombard in Oncogene (2019)