Journal of Biological Chemistry
Accelerated CommunicationsThe orphan receptor GPR139 signals via Gq/11 to oppose opioid effects
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Author contributions—H. M. S. and K. A. M. conceptualization; H. M. S. data curation; H. M. S., S. Z., and I. M. formal analysis; H. M. S., S. Z., and I. M. investigation; H. M. S. and K. A. M. writing-original draft; H. M. S., S. Z., I. M., B. G., and K. A. M. writing-review and editing; B. G. resources; B. G. and K. A. M. funding acquisition; K. A. M. supervision; K. A. M. project administration.
Funding and additional information—This work was supported by National Institutes of Health Grants DA036596 (to K. A. M.), DA048036 (to B. G. and K. A. M.), DA047771 (to H. M. S.), and DA048579 (to S. Z.). The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health.
Conflict of interest—B. G. and K. A. M. have filed a patent on the utility of GPR139 as a drug target.
Abbreviations—The abbreviations used are:
- GPCR
G protein–coupled receptor
- AC
adenylyl cyclase
- MOR
µ-opioid receptor
- GIRK
G protein inward rectifying potassium
- BRET
bioluminescence resonance energy transfer
- FSK
forskolin
- PIP2
phosphatidylinositol 4,5-bisphosphate
- mHb
medial habenula
- HA
hemagglutinin
- HASP
HA signal peptide.