A PTEN-Regulated Checkpoint Controls Surface Delivery of δ Opioid Receptors.

ABSTRACT: The δ opioid receptor (δR) is a promising alternate target for pain management because δR agonists show decreased abuse potential compared with current opioid analgesics that target the μ opioid receptor. A critical limitation in developing δR as an analgesic target, however, is that δR agonists show relatively low efficacy in vivo, requiring the use of high doses that often cause adverse effects, such as convulsions. Here we tested whether intracellular retention of δR in sensory neurons contributes to this low δR agonist efficacy in vivo by limiting surface δR expression. Using direct visualization of δR trafficking and localization, we define a phosphatase and tensin homolog (PTEN)-regulated checkpoint that retains δR in the Golgi and decreases surface delivery in rat and

SUBMITTER: Shiwarski DJ 

PROVIDER: S-EPMC5394893 | biostudies-literature | 2017 Apr

REPOSITORIES: biostudies-literature