Structure and dynamics of GPCR signaling complexes
G-protein-coupled receptors (GPCRs) relay numerous extracellular signals by triggering
intracellular signaling through coupling with G proteins and arrestins. Recent breakthroughs …
intracellular signaling through coupling with G proteins and arrestins. Recent breakthroughs …
G protein-coupled receptor signaling: transducers and effectors
G protein-coupled receptors (GPCRs) are of considerable interest due to their importance in
a wide range of physiological functions and in a large number of Food and Drug …
a wide range of physiological functions and in a large number of Food and Drug …
Structure of the neurotensin receptor 1 in complex with β-arrestin 1
Arrestin proteins bind to active, phosphorylated G-protein-coupled receptors (GPCRs),
thereby preventing G-protein coupling, triggering receptor internalization and affecting …
thereby preventing G-protein coupling, triggering receptor internalization and affecting …
Molecular mechanism of GPCR-mediated arrestin activation
Despite intense interest in discovering drugs that cause G-protein-coupled receptors
(GPCRs) to selectively stimulate or block arrestin signalling, the structural mechanism of …
(GPCRs) to selectively stimulate or block arrestin signalling, the structural mechanism of …
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 …
Catalytic activation of β-arrestin by GPCRs
Abstract β-arrestins are critical regulator and transducer proteins for G-protein-coupled
receptors (GPCRs). β-arrestin is widely believed to be activated by forming a stable and …
receptors (GPCRs). β-arrestin is widely believed to be activated by forming a stable and …
GPCR-mediated β-arrestin activation deconvoluted with single-molecule precision
Summary β-arrestins bind G protein-coupled receptors to terminate G protein signaling and
to facilitate other downstream signaling pathways. Using single-molecule fluorescence …
to facilitate other downstream signaling pathways. Using single-molecule fluorescence …
Distinct G protein-coupled receptor phosphorylation motifs modulate arrestin affinity and activation and global conformation
D Mayer, FF Damberger, M Samarasimhareddy… - Nature …, 2019 - nature.com
Cellular functions of arrestins are determined in part by the pattern of phosphorylation on the
G protein-coupled receptors (GPCRs) to which arrestins bind. Despite high-resolution …
G protein-coupled receptors (GPCRs) to which arrestins bind. Despite high-resolution …
G protein–coupled receptor interactions with arrestins and GPCR kinases: The unresolved issue of signal bias
Q Chen, JJG Tesmer - Journal of Biological Chemistry, 2022 - ASBMB
G protein–coupled receptor (GPCR) kinases (GRKs) and arrestins interact with agonist-
bound GPCRs to promote receptor desensitization and downregulation. They also trigger …
bound GPCRs to promote receptor desensitization and downregulation. They also trigger …
Scaffolding mechanism of arrestin-2 in the cRaf/MEK1/ERK signaling cascade
C Qu, JY Park, MW Yun, Q He, F Yang… - Proceedings of the …, 2021 - National Acad Sciences
Arrestins were initially identified for their role in homologous desensitization and
internalization of G protein–coupled receptors. Receptor-bound arrestins also initiate …
internalization of G protein–coupled receptors. Receptor-bound arrestins also initiate …