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Endothelin-converting enzyme 2 regulates κ opioid receptor trafficking and function.

Achla Gupta1, Ivone Gomes1, Salvador Sierra2

  • 1Department of Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, New York, New York.

The Journal of Pharmacology and Experimental Therapeutics
|November 8, 2025
PubMed
Summary
This summary is machine-generated.

Endothelin-converting enzyme 2 (ECE2) directly interacts with and regulates κ opioid receptors (KORs). ECE2 inhibition impacts KOR recycling and signaling, suggesting ECE2 inhibitors as potential therapeutics for KOR-related disorders.

Keywords:
Endothelin-converting enzyme 2ResensitizationTraffickingκ Opioid Receptors

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Area of Science:

  • Neuroscience
  • Biochemistry
  • Pharmacology

Background:

  • Endothelin-converting enzyme 2 (ECE2) processes neuropeptides and influences μ and δ opioid receptor recycling.
  • The role of ECE2 in κ opioid receptor (KOR) regulation remains less understood.

Purpose of the Study:

  • To investigate the interaction between ECE2 and KOR.
  • To examine how ECE2 substrates modulate KOR internalization and recycling.
  • To assess the impact of ECE2 inhibition on KOR function.

Main Methods:

  • Proximity-based ligation assay to detect KOR-ECE2 interaction.
  • Treatment with ECE2 substrate and non-substrate peptides.
  • Analysis of receptor internalization and recycling kinetics.
  • Pharmacological inhibition of ECE2 in recombinant and endogenous systems.

Main Results:

  • KOR and ECE2 directly interact and cointernalize upon peptide treatment.
  • Peptide-induced internalization and recycling of ECE2 mirrors that of KOR.
  • ECE2 inhibition attenuates KOR recycling and signaling mediated by ECE2 substrates.
  • Differential ECE2 expression observed across brain regions.

Conclusions:

  • ECE2 plays a critical role in modulating KOR function, particularly with ECE2 substrate peptides.
  • ECE2 activity is essential for agonist-mediated KOR recycling and signaling.
  • ECE2 inhibitors represent a potential therapeutic strategy for KOR-related dysfunctions.