The α-arrestin ARRDC3 mediates ALIX ubiquitination and G protein-coupled receptor lysosomal sorting. [PDF]
The sorting of G protein-coupled receptors (GPCRs) to lysosomes is critical for proper signaling and cellular responses. We previously showed that the adaptor protein ALIX regulates lysosomal degradation of protease-activated receptor-1 (PAR1), a GPCR ...
Dores, Michael R +4 more
core +1 more source
Mass Spectrometry Structural Proteomics Enabled by Limited Proteolysis and Cross‐Linking
ABSTRACT The exploration of protein structure and function stands at the forefront of life science and represents an ever‐expanding focus in the development of proteomics. As mass spectrometry (MS) offers readout of protein conformational changes at both the protein and peptide levels, MS‐based structural proteomics is making significant strides in the
Haiyan Lu +4 more
wiley +1 more source
CXCR7 ameliorates myocardial infarction as a β-arrestin-biased receptor
Most seven transmembrane receptors (7TMRs) are G protein-coupled receptors; however, some 7TMRs evoke intracellular signals through β-arrestin as a biased receptor.
Masato Ishizuka +20 more
doaj +1 more source
A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice. [PDF]
It is well known that the ω-3 fatty acids (ω-3-FAs; also known as n-3 fatty acids) can exert potent anti-inflammatory effects. Commonly consumed as fish products, dietary supplements and pharmaceuticals, ω-3-FAs have a number of health benefits ascribed ...
Akiyama, Taro E +20 more
core +1 more source
Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit beta-Arrestin-2. [PDF]
Natural products found in Mitragyna speciosa, commonly known as kratom, represent diverse scaffolds (indole, indolenine, and spiro pseudoindoxyl) with opioid activity, providing opportunities to better understand opioid pharmacology.
Borics, Attila +5 more
core +1 more source
Advances in GPCRs Associated With Wnt Signaling Within the Auditory System
ABSTRACT G protein‐coupled receptors (GPCRs) that interact with the Wnt signaling pathway are pivotal for auditory system homeostasis, as they orchestrate inner ear development, hair cell (HC) regeneration, and hearing preservation. Frizzled (FZD) receptors, the core Wnt‐related GPCRs, bind Wnt ligands and co‐receptors (e.g., LRP5/6) to activate both ...
Liang Wang +3 more
wiley +1 more source
Arrestin translocation and signaling have come to the fore of the G protein-coupled receptor molecular pharmacology field. Some receptor–arrestin interactions are relatively well understood and considered responsible for specific therapeutic or adverse ...
Mikkel Søes Ibsen +9 more
doaj +1 more source
Galanin receptor 2 modifies neuropeptide Y Y1 receptor internalization and β-Arrestin recruitment [PDF]
We have recently described a Galanin receptor 2(GALR2) and Neuropeptide Y Y1 receptor(NPYY1R) interaction at behavioural, cellular and receptor levels through GALR2/NPYY1R heterodimers.
Borroto-Escuela, Dasiel +8 more
core
N‐Palmitoylglycine and other N‐acylamides activate the lipid receptor G2A/GPR132 [PDF]
The G‐protein‐coupled receptor GPR132, also known as G2A, is activated by 9‐hydroxyoctadecadienoic acid (9‐HODE) and other oxidized fatty acids. Other suggested GPR132 agonists including lysophosphatidylcholine (LPC) have not been readily reproduced ...
Brown, Andrew J. +6 more
core +1 more source
Preclinical models for evaluating psychedelics in the treatment of major depressive disorder
Psychedelic drugs have seen a resurgence in interest as a next generation of psychiatric medicines with potential as rapid‐acting antidepressants (RAADs). Despite promising early clinical trials, the mechanisms which underlie the effects of psychedelics are poorly understood.
Laith Alexander +5 more
wiley +1 more source

