Accès ouvert
2023
letter
OpenAlex
Evi Kostenis, Jesús Gomeza, Elke Miess-Tanneberg, Nina Kathleen Blum et autres
We thank Dr. Robert Lefkowitz and co-authors for their comments on our article “How carvedilol activates β 2 -adrenoceptors” 1 . In their critique 2 , they state that our study concludes that intrinsic sympathomimetic activity (ISA) is the mechanism responsible for …
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Accès ouvert
2022
article
OpenAlex
Tobias Benkel, Mirjam Zimmermann, Julian Zeiner, Sergi Bravo et autres
Abstract 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 blockade of β1-adrenoceptors, arrestin-biased signalling via β2-adrenoceptors is a molecular mechanism proposed to …
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Accès ouvert
2022
article
OpenAlex
Johanna Kaufmann, Nina Kathleen Blum, Falko Nagel, Anna Schuler et autres
Analysis of agonist-driven phosphorylation of G protein-coupled receptors (GPCRs) can provide valuable insights into the receptor activation state and ligand pharmacology. However, to date, assessment of GPCR phosphorylation using high-throughput applications has been challenging. We have developed and validated a bead-based immunoassay …
de, at
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Accès ouvert
2022
preprint
OpenAlex
Johanna Kaufmann, Nina Kathleen Blum, Falko Nagel, Anna Schuler et autres
Abstract Analysis of agonist-driven phosphorylation of G protein-coupled receptors (GPCRs) can provide valuable insights into the receptor activation state and ligand pharmacology. However, to date, assessment of GPCR phosphorylation using high-throughput applications has been challenging. We have developed and validated a bead-based …
de, at
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Accès ouvert
2022
article
OpenAlex
Julia Drube, Raphael S. Haider, Edda S. F. Matthees, Mona Reichel et autres
G protein-coupled receptors (GPCRs) activate G proteins and undergo a complex regulation by interaction with GPCR kinases (GRKs) and the formation of receptor-arrestin complexes. However, the impact of individual GRKs on arrestin binding is not clear. We report the creation of eleven …
de
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