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Opioid receptor function is regulated by post-endocytic peptide processing.

Achla Gupta1, Ivone Gomes1, Jonathan Wardman1

  • 1From the Department of Pharmacology and Systems Therapeutics and.

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|May 22, 2014
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Summary
This summary is machine-generated.

Endothelin-converting enzyme 2 (ECE2) processes opioid peptides in endosomes. Inhibiting ECE2 impairs peptide degradation, reducing opioid receptor recycling and signaling.

Keywords:
EnkephalinG Protein-coupled Receptor (GPCR)MorphineNeprilysinOpiatesReceptor DesensitizationReceptor RecyclingReceptor RegulationResensitizationSignal Transduction

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Area of Science:

  • Neuroscience
  • Molecular Biology
  • Biochemistry

Background:

  • Neuroendocrine peptides are typically processed at basic residues by subtilisin-like endopeptidases.
  • Processing at non-classical cleavage sites, lacking basic residues, is less understood.
  • Endothelin-converting enzyme (ECE) family members are candidates for non-classical peptide processing.

Purpose of the Study:

  • To investigate the role of ECE2 in the endocytic processing of delta (δ) opioid peptides.
  • To determine ECE2's effect on delta opioid receptor function.
  • To utilize selective ECE2 inhibitors for exploring these processes.

Main Methods:

  • Employing selective ECE2 inhibitors developed via homology modeling and virtual screening.
  • Assessing intracellular co-localization of ECE2 and δ opioid receptors upon agonist treatment.
  • Evaluating the impact of ECE2 inhibition and pH modulation on receptor recycling and peptide degradation.
  • Measuring surface receptor signaling in primary neurons.

Main Results:

  • Agonist stimulation caused ECE2 to co-localize with δ opioid receptors intracellularly.
  • ECE2 inhibitors and reagents increasing endosomal pH reduced peptide degradation and impaired receptor recycling.
  • This impairment led to a significant decrease in surface receptor signaling.
  • In primary neurons, ECE2 inhibition during recycling increased receptor-ECE2 co-localization, decreasing recycling and signaling.

Conclusions:

  • ECE2 plays a role in the post-endocytic processing of peptide agonists.
  • Differential modulation of opioid receptor signaling is influenced by ECE2-mediated processing.
  • This mechanism offers a novel pathway for regulating opioid receptor activity.