Article
Selective phosphorylation of threonine residues defines GPR84-arrestin interactions of biased ligands.
The Journal of biological chemistry - 1 May 2022
Marsango Sara, Ward Richard J, Jenkins Laura, Butcher Adrian J, Al Mahmud Zobaer, Dwomoh Louis, Nagel Falko, Schulz Stefan, Tikhonova Irina G, Tobin Andrew B, Milligan Graeme
Abstract excerpt
GPR84 is an immune cell-expressed, proinflammatory receptor currently being assessed as a therapeutic target in conditions including fibrosis and inflammatory bowel disease. Although it was previously shown that the orthosteric GPR84 activators 2-HTP and 6-OAU promoted its interactions with arrestin-3, a G protein-biased agonist DL-175 did not. Here, we show that replacement of all 21 serine and threonine...
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