Article
The μ-opioid receptor variant N190K is unresponsive to peptide agonists yet can be rescued by small-molecule drugs.
Molecular pharmacology - 1 Nov 2010
Fortin Jean-Philippe, Ci Lei, Schroeder Jonathan, Goldstein Carmit, Montefusco Maria Claudia, Peter Inga, Reis Steven E, Huggins Gordon S, Beinborn Martin, Kopin Alan S
Abstract excerpt
The μ-opioid receptor (MOR) plays an important role in modulating analgesia, feeding behavior, and a range of autonomic functions. In the current study, we investigated the degree to which 13 naturally occurring missense mutations affect the pharmacological properties of the human MOR. After expression of each receptor in human embryonic kidney 293 cells, signaling (Gα(i/o)-mediated) induced by peptide agonists...
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