Structure and dynamics of GPCR signaling complexes

D Hilger, M Masureel, BK Kobilka - Nature structural & molecular …, 2018 - nature.com
G-protein-coupled receptors (GPCRs) relay numerous extracellular signals by triggering
intracellular signaling through coupling with G proteins and arrestins. Recent breakthroughs …

G protein-coupled receptor signaling: transducers and effectors

H Jiang, D Galtes, J Wang… - American Journal of …, 2022 - journals.physiology.org
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 …

Structure of the neurotensin receptor 1 in complex with β-arrestin 1

W Huang, M Masureel, Q Qu, J Janetzko, A Inoue… - Nature, 2020 - nature.com
Arrestin proteins bind to active, phosphorylated G-protein-coupled receptors (GPCRs),
thereby preventing G-protein coupling, triggering receptor internalization and affecting …

Molecular mechanism of GPCR-mediated arrestin activation

NR Latorraca, JK Wang, B Bauer, RJL Townshend… - Nature, 2018 - nature.com
Despite intense interest in discovering drugs that cause G-protein-coupled receptors
(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

J Maharana, P Sarma, MK Yadav, S Saha, V Singh… - Molecular cell, 2023 - cell.com
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 …

Catalytic activation of β-arrestin by GPCRs

K Eichel, D Jullié, B Barsi-Rhyne, NR Latorraca… - Nature, 2018 - nature.com
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 …

GPCR-mediated β-arrestin activation deconvoluted with single-molecule precision

WB Asher, DS Terry, GGA Gregorio, AW Kahsai… - Cell, 2022 - cell.com
Summary β-arrestins bind G protein-coupled receptors to terminate G protein signaling and
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 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 …

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 …