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Peroxiredoxin 6 mediates Gαi protein-coupled receptor inactivation by cJun kinase

Abstract:
Inactivation of opioid receptors limits the therapeutic efficacy of morphine-like analgesics and mediates the long duration of kappa opioid antidepressants by an uncharacterized, arrestin-independent mechanism. Here we use an iterative, discovery-based proteomic approach to show that following opioid administration, peroxiredoxin 6 (PRDX6) is recruited to the opioid receptor complex by c-Jun N-terminal kinase (JNK) phosphorylation. PRDX6 activation generates reactive oxygen species via NADPH oxidase, reducing the palmitoylation of receptor-associated Gαi in a JNK-dependent manner. Selective inhibition of PRDX6 blocks Gαi depalmitoylation, prevents the enhanced receptor G-protein association and blocks acute analgesic tolerance to morphine and kappa opioid receptor inactivation in vivo. Opioid stimulation of JNK also inactivates dopamine D2 receptors in a PRDX6-dependent manner. We show that the loss of this lipid modification distorts the receptor G-protein association, thereby preventing agonist-induced guanine nucleotide exchange. These findings establish JNK-dependent PRDX6 recruitment and oxidation-induced Gαi depalmitoylation as an additional mechanism of Gαi-G-protein-coupled receptor inactivation.Opioid receptors are important modulators of nociceptive pain. Here the authors show that opioid receptor activation recruits peroxiredoxin 6 (PRDX6) to the receptor-Gαi complex by c-Jun N-terminal kinase, resulting in Gαi depalmitoylation and enhanced receptor-Gαi association.
Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1038/s41467-017-00791-2

Authors

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Institution:
University of Oxford
Division:
MSD
Department:
Experimental Psychology
Role:
Author
ORCID:
0000-0001-9305-1621


Publisher:
Nature Publishing Group
Journal:
Nature Communications More from this journal
Volume:
8
Issue:
1
Pages:
743
Publication date:
2017-09-29
Acceptance date:
2017-07-27
DOI:
EISSN:
2041-1723
ISSN:
2041-1723
Pmid:
28963507

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