Conformational basis of G protein-coupled receptor signaling versatility
LM Wingler, RJ Lefkowitz - Trends in cell biology, 2020 - cell.com
G protein-coupled receptors (GPCRs) are privileged structural scaffolds in biology that have
the versatility to regulate diverse physiological processes. Interestingly, many GPCR ligands …
the versatility to regulate diverse physiological processes. Interestingly, many GPCR ligands …
Post-translational modifications of G Protein–Coupled receptors control cellular signaling dynamics in space and time
G protein–coupled receptors (GPCRs) are a large family comprising> 800 signaling
receptors that regulate numerous cellular and physiologic responses. GPCRs have been …
receptors that regulate numerous cellular and physiologic responses. GPCRs have been …
Signaling snapshots of a serotonin receptor activated by the prototypical psychedelic LSD
Summary Serotonin (5-hydroxytryptamine [5-HT]) 5-HT2-family receptors represent essential
targets for lysergic acid diethylamide (LSD) and all other psychedelic drugs. Although the …
targets for lysergic acid diethylamide (LSD) and all other psychedelic drugs. Although the …
GPCR kinase knockout cells reveal the impact of individual GRKs on arrestin binding and GPCR regulation
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 …
by interaction with GPCR kinases (GRKs) and the formation of receptor–arrestin complexes …
[HTML][HTML] How GPCR phosphorylation patterns orchestrate arrestin-mediated signaling
Binding of arrestin to phosphorylated G-protein-coupled receptors (GPCRs) controls many
aspects of cell signaling. The number and arrangement of phosphates may vary …
aspects of cell signaling. The number and arrangement of phosphates may vary …
How Carvedilol activates β2-adrenoceptors
T Benkel, M Zimmermann, J Zeiner, S Bravo… - Nature …, 2022 - nature.com
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 …
infarction. Yet the mechanisms by which carvedilol achieves this superior clinical profile are …
Structural snapshots uncover a key phosphorylation motif in GPCRs driving β-arrestin activation
Agonist-induced GPCR phosphorylation is a key determinant for the binding and activation
of β-arrestins (βarrs). However, it is not entirely clear how different GPCRs harboring …
of β-arrestins (βarrs). However, it is not entirely clear how different GPCRs harboring …
β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling to the same GPCR in living cells
Abstract β-arrestins mediate regulatory processes for over 800 different G protein-coupled
receptors (GPCRs) by adopting specific conformations that result from the geometry of the …
receptors (GPCRs) by adopting specific conformations that result from the geometry of the …
Structure of an endosomal signaling GPCR–G protein–β-arrestin megacomplex
AH Nguyen, ARB Thomsen, TJ Cahill III… - Nature structural & …, 2019 - nature.com
Classically, G-protein-coupled receptors (GPCRs) are thought to activate G protein from the
plasma membrane and are subsequently desensitized by β-arrestin (β-arr). However, some …
plasma membrane and are subsequently desensitized by β-arrestin (β-arr). However, some …
Spatial bias in cAMP generation determines biological responses to PTH type 1 receptor activation
The parathyroid hormone (PTH) type 1 receptor (PTHR) is a class BG protein–coupled
receptor (GPCR) that regulates mineral ion, vitamin D, and bone homeostasis. Activation of …
receptor (GPCR) that regulates mineral ion, vitamin D, and bone homeostasis. Activation of …