Article
Multisite phosphorylation is required for sustained interaction with GRKs and arrestins during rapid μ-opioid receptor desensitization.
Science signaling - 17 Jul 2018
Miess Elke, Gondin Arisbel B, Yousuf Arsalan, Steinborn Ralph, Mösslein Nadja, Yang Yunshi, Göldner Martin, Ruland Julia G, Bünemann Moritz, Krasel Cornelius, Christie MacDonald J, Halls Michelle L, Schulz Stefan, Canals Meritxell
Abstract excerpt
G protein receptor kinases (GRKs) and β-arrestins are key regulators of μ-opioid receptor (MOR) signaling and trafficking. We have previously shown that high-efficacy opioids such as DAMGO stimulate a GRK2/3-mediated multisite phosphorylation of conserved C-terminal tail serine and threonine residues, which facilitates internalization of the receptor. In contrast, morphine-induced phosphorylation of MOR is...
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