A model for the signal initiation complex between Arrestin-3 and the Src family kinase Fgr.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of molecular biology"
DOI: 10.1016/j.jmb.2021.167400
Abstract: Arrestins regulate a wide range of signaling events, most notably when bound to active G protein-coupled receptors (GPCRs). Among the known effectors recruited by GPCR-bound arrestins are Src family kinases, which regulate cellular growth and… read more here.
Keywords: model signal; fgr; arrestin; src family ... See more keywords
Phosphoproteomic Analysis of Dopamine D2 Receptor Signaling Reveals Interplay of G Protein- and β-Arrestin-Mediated Effects.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of proteome research"
DOI: 10.1021/acs.jproteome.2c00707
Abstract: Leveraging biased signaling of G protein-coupled receptors has been proposed as a promising strategy for the development of drugs with higher specificity. However, the consequences of selectively targeting G protein- or β-arrestin-mediated signaling on cellular… read more here.
Keywords: dopamine receptor; protein arrestin; arrestin mediated; analysis ... See more keywords
Functionally Biased D2R Antagonists: Targeting the β-Arrestin Pathway to Improve Antipsychotic Treatment.
Sign Up to like & getrecommendations! Published in 2018 at "ACS chemical biology"
DOI: 10.1021/acschembio.8b00168
Abstract: Schizophrenia is a severe neuropsychiatric disease that lacks completely effective and safe therapies. As a polygenic disorder, genetic studies have only started to shed light on its complex etiology. To date, the positive symptoms of… read more here.
Keywords: functionally biased; treatment; biased d2r; arrestin ... See more keywords
Helix-bundle and C-terminal GPCR domains differentially influence GRK-specific functions and β-arrestin-mediated regulation
Sign Up to like & getrecommendations! Published in 2025 at "Nature Communications"
DOI: 10.1038/s41467-025-61281-4
Abstract: G protein-coupled receptors (GPCRs) orchestrate diverse physiological responses via signaling through G proteins, GPCR kinases (GRKs), and arrestins. While most G protein functions are well-established, the contributions of GRKs and arrestins remain incompletely understood. Here,… read more here.
Keywords: grk specific; gpcr domains; arrestin; gpcr ... See more keywords
Stabilized D2R G protein-coupled receptor oligomers identify multi-state β-arrestin complexes
Sign Up to like & getrecommendations! Published in 2025 at "Nature Communications"
DOI: 10.1038/s41467-025-64008-7
Abstract: The G-protein coupled receptor (GPCR) superfamily directs central roles in many physiological and pathophysiological processes via diverse and complex mechanisms. GPCRs can exhibit signal pleiotropy via formation of di/oligomers both with themselves and other GPCRs.… read more here.
Keywords: receptor; coupled receptor; protein coupled; arrestin ... See more keywords
Allosteric interactions in the parathyroid hormone GPCR–arrestin complex formation
Sign Up to like & getrecommendations! Published in 2020 at "Nature chemical biology"
DOI: 10.1038/s41589-020-0567-0
Abstract: Peptide ligands of class B G-protein-coupled receptors act via a two-step binding process, but the essential mechanisms that link their extracellular binding to intracellular receptor–arrestin interactions are not fully understood. Using NMR, crosslinking coupled to… read more here.
Keywords: pth; arrestin complex; parathyroid hormone; arrestin ... See more keywords
GRK specificity and Gβγ dependency determines the potential of a GPCR for arrestin-biased agonism
Sign Up to like & getrecommendations! Published in 2024 at "Communications Biology"
DOI: 10.1038/s42003-024-06490-1
Abstract: G protein-coupled receptors (GPCRs) are mainly regulated by GPCR kinase (GRK) phosphorylation and subsequent β-arrestin recruitment. The ubiquitously expressed GRKs are classified into cytosolic GRK2/3 and membrane-tethered GRK5/6 subfamilies. GRK2/3 interact with activated G protein… read more here.
Keywords: grk2; biased agonism; arrestin biased; grk specificity ... See more keywords
Residency time of agonists does not affect the stability of GPCR–arrestin complexes
Sign Up to like & getrecommendations! Published in 2022 at "British Journal of Pharmacology"
DOI: 10.1111/bph.15846
Abstract: The interaction of arrestins with G‐protein coupled receptors (GPCRs) desensitizes agonist‐dependent receptor responses and often leads to receptor internalization. GPCRs that internalize without arrestin have been classified as “class A” GPCRs whereas “class B” GPCRs… read more here.
Keywords: agonists affect; residency time; affect stability; arrestin ... See more keywords
Arrestin‐3 binds parkin and enhances parkin‐dependent mitophagy
Sign Up to like & getrecommendations! Published in 2024 at "Journal of Neurochemistry"
DOI: 10.1111/jnc.16043
Abstract: Arrestins were discovered for their role in homologous desensitization of G‐protein‐coupled receptors (GPCRs). Later non‐visual arrestins were shown to regulate several signaling pathways. Some of these pathways require arrestin binding to GPCRs, the regulation of… read more here.
Keywords: enhances parkin; arrestin; mitophagy; arrestin binds ... See more keywords
Noncanonical scaffolding of Gαi and β-arrestin by G protein–coupled receptors
Sign Up to like & getrecommendations! Published in 2021 at "Science"
DOI: 10.1126/science.aay1833
Abstract: Another way for GPCRs to signal G protein–coupled receptors (GPCRs) normally transmit signals by coupling to heterotrimeric guanine nucleotide–binding proteins (G proteins) or by binding β-arrestin proteins. Smith et al. provide evidence for another mechanism,… read more here.
Keywords: protein; arrestin complexes; arrestin; protein coupled ... See more keywords
Biased agonists of the chemokine receptor CXCR3 differentially signal through Gαi:β-arrestin complexes
Sign Up to like & getrecommendations! Published in 2022 at "Science Signaling"
DOI: 10.1126/scisignal.abg5203
Abstract: G protein–coupled receptors (GPCRs) are the largest family of cell surface receptors and signal through the proximal effectors, G proteins and β-arrestins, to influence nearly every biological process. The G protein and β-arrestin signaling pathways… read more here.
Keywords: arrestin complex; arrestin complexes; arrestin; protein ... See more keywords