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G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
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Heterotrimeric G proteins are guanine nucleotide-binding proteins. As the name suggests, heterotrimeric G proteins are composed of three subunits: alpha, beta, and gamma. They remain GDP-bound or GTP-bound inside the cells and switch between inactive/active states. The Gα subunit possesses the nucleotide-binding pocket that binds guanine nucleotides and switches between GDP or GTP-bound states. In contrast, the Gꞵ and Gγ subunits are always bound together with high...
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Area of Science:

  • Pharmacology
  • Cell Biology
  • Biochemistry

Background:

  • Intracellular G protein-coupled receptors (GPCRs) activation by permeant ligands influences agonist selectivity.
  • Opioid receptors (ORs) are activated by opioid drugs within the Golgi apparatus, but their intracellular function is not fully understood.
  • Differences in signaling between plasma membrane (PM) and Golgi apparatus opioid receptors remain unclear.

Purpose of the Study:

  • To investigate and compare the signaling mechanisms of mu- and delta-opioid receptors (ORs) in the plasma membrane and Golgi apparatus.
  • To determine if subcellular localization affects ORs' interaction with signal transducers like G proteins and β-arrestin.
  • To elucidate how the distinct lipid environments of the PM and Golgi influence OR signaling.

Main Methods:

  • Assessed the recruitment of signal transducers to mu- and delta-ORs in both cellular compartments.
  • Utilized molecular dynamics simulations of OR-transducer complexes in lipid bilayers mimicking PM and Golgi compositions.
  • Examined the effects of delta-ORs on transcription and protein phosphorylation in different cellular locations.

Main Results:

  • Golgi-localized ORs engage with Gαi/o probes and undergo phosphorylation.
  • Unlike PM receptors, Golgi ORs do not recruit β-arrestin or a specific Gα probe.
  • Molecular dynamics simulations revealed that lipid environments dictate location-selective OR coupling.
  • Delta-ORs in the PM and Golgi exhibit distinct downstream effects on transcription and protein phosphorylation.

Conclusions:

  • Subcellular localization is a critical determinant of opioid receptor signaling outcomes.
  • The lipid microenvironment significantly influences the specific G protein coupling of ORs.
  • Distinct signaling pathways are activated by opioid receptors depending on whether they reside in the plasma membrane or the Golgi apparatus.