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GPCR homo-oligomerization [PDF]
Current Opinion in Cell Biology, 2019 G protein-coupled receptors (GPCRs) are an extensive class of trans-plasma membrane proteins that function to regulate a wide range of physiological functions. Despite a general perception that GPCRs exist as monomers an extensive literature has examined whether GPCRs can also form dimers and even higher-order oligomers, and if such organization ...
Milligan, Graeme +2 more
openaire +2 more sources
Muscarinic receptor oligomerization [PDF]
, 2018 G protein-coupled receptors (GPCRs) have been classically described as monomeric entities that function by binding in a 1:1 stoichiometric ratio to both ligand and downstream signalling proteins.
Alvarez-Curto, Elisa +3 more
core +1 more source
Phylogenomic analysis reveals extensive phylogenetic mosaicism in the Human GPCR Superfamily [PDF]
, 2007 A novel high throughput phylogenomic analysis (HTP) was applied to the rhodopsin G-protein coupled receptor (GPCR) family. Instances of phylogenetic mosaicism between receptors were found to be frequent, often as instances of correlated mosaicism and ...
Allaby, Robin G., Woodwark, Mathew
core +1 more source
CHIMIA, 2021 Numerous members of the human G protein-coupled receptor (GPCR) superfamily are receptors of therapeutic interest. GPCRs are considered to be highly tractable for drug discovery, representing the targets of approximately one-third of currently licensed ...
Kalyan Bharati Akondi +2 more
doaj +1 more source
Prediction and classification for GPCR sequences based on ligand specific features [PDF]
, 2006 Functional identification of G-Protein Coupled Receptors (GPCRs) is one of the current focus areas of pharmaceutical research. Although thousands of GPCR sequences are known, many of them are orphan sequences (the activating ligand is unknown). Therefore,
F. Horn +8 more
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Arrestin-3 differentially regulates platelet GPCR subsets
Platelets, 2020 The principal demonstrated role of the nonvisual arrestins in vivo is to limit G protein-coupled receptor (GPCR) signaling. Nonetheless, a direct demonstration of this fundamental ability in platelets remains lacking, despite the prominent role played by
James L. Hutchinson +3 more
doaj +1 more source
Targeted elimination of G proteins and arrestins defines their specific contributions to both intensity and duration of G protein-coupled receptor signalling [PDF]
, 2016 G protein-coupled receptors (GPCRs) can initiate intracellular signalling cascades by coupling to an array of heterotrimeric G proteins and arrestin adaptor proteins. Understanding the contribution of each of these coupling options to GPCR signalling has
Alvarez-Curto, Elisa +6 more
core +1 more source
ALIX binds a YPX(3)L motif of the GPCR PAR1 and mediates ubiquitin-independent ESCRT-III/MVB sorting. [PDF]
, 2012 The sorting of signaling receptors to lysosomes is an essential regulatory process in mammalian cells. During degradation, receptors are modified with ubiquitin and sorted by endosomal sorting complex required for transport (ESCRT)-0, -I, -II, and -III ...
Chen, Buxin +7 more
core +3 more sources
Below the Surface: IGF-1R Therapeutic Targeting and Its Endocytic Journey
Cells, 2019 Ligand-activated plasma membrane receptors follow pathways of endocytosis through the endosomal sorting apparatus. Receptors cluster in clathrin-coated pits that bud inwards and enter the cell as clathrin-coated vesicles.
Caitrin Crudden +7 more
doaj +1 more source