β− Arrestins: structure, function, physiology, and pharmacological perspectives

J Wess, AB Oteng, O Rivera-Gonzalez… - Pharmacological …, 2023 - Elsevier
The two β-arrestins, β-arrestin-1 and-2 (systematic names: arrestin-2 and-3, respectively),
are multifunctional intracellular proteins that regulate the activity of a very large number of …

[HTML][HTML] New insights into GPCR coupling and dimerisation from cryo-EM structures

A Gusach, J García-Nafría, CG Tate - Current Opinion in Structural Biology, 2023 - Elsevier
Over the past three years (2020–2022) more structures of GPCRs have been determined
than in the previous twenty years (2000–2019), primarily of GPCR complexes that are large …

Tail engagement of arrestin at the glucagon receptor

K Chen, C Zhang, S Lin, X Yan, H Cai, C Yi, L Ma… - Nature, 2023 - nature.com
Arrestins have pivotal roles in regulating G protein-coupled receptor (GPCR) signalling by
desensitizing G protein activation and mediating receptor internalization,. It has been …

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 …

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 …

Snapshot of the cannabinoid receptor 1-arrestin complex unravels the biased signaling mechanism

YY Liao, H Zhang, Q Shen, C Cai, Y Ding, DD Shen… - Cell, 2023 - cell.com
Cannabis activates the cannabinoid receptor 1 (CB1), which elicits analgesic and emotion
regulation benefits, along with adverse effects, via G i and β-arrestin signaling pathways …

A key GPCR phosphorylation motif discovered in arrestin2⋅ CCR5 phosphopeptide complexes

P Isaikina, I Petrovic, RP Jakob, P Sarma, A Ranjan… - Molecular cell, 2023 - cell.com
The two non-visual arrestins, arrestin2 and arrestin3, bind hundreds of GPCRs with different
phosphorylation patterns, leading to distinct functional outcomes. Structural information on …

Molecular insights into atypical modes of β-arrestin interaction with seven transmembrane receptors

J Maharana, FK Sano, P Sarma, MK Yadav, L Duan… - Science, 2024 - science.org
β-arrestins (βarrs) are multifunctional proteins involved in signaling and regulation of seven
transmembrane receptors (7TMRs), and their interaction is driven primarily by agonist …

Structure, function and drug discovery of GPCR signaling

L Cheng, F Xia, Z Li, C Shen, Z Yang, H Hou… - Molecular …, 2023 - Springer
G protein-coupled receptors (GPCRs) are versatile and vital proteins involved in a wide
array of physiological processes and responses, such as sensory perception (eg, vision …

Pharmacologically targeting intracellular allosteric sites of GPCRs for drug discovery

M Zhang, X Lan, X Li, S Lu - Drug Discovery Today, 2023 - Elsevier
G-protein-coupled receptors (GPCRs) are a family of cell surface proteins that can sense a
variety of extracellular stimuli and mediate multiple signaling transduction pathways …