Article
Morphine induces terminal micro-opioid receptor desensitization by sustained phosphorylation of serine-375.
The EMBO journal - 18 Aug 2004
Schulz Stefan, Mayer Dana, Pfeiffer Manuela, Stumm Ralf, Koch Thomas, Höllt Volker
Abstract excerpt
Morphine is a poor inducer of micro-opioid receptor (MOR) internalization, but a potent inducer of cellular tolerance. Here we show that, in contrast to full agonists such as [D-Ala(2)-MePhe(4)-Gly-ol]enkephalin (DAMGO), morphine stimulated a selective phosphorylation of the carboxy-terminal residue 375 (Ser(375)). Ser(375) phosphorylation was sufficient and required for morphine-induced desensitization of MOR....
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