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Targeting the kappa opioid receptor for analgesia and antitumour effects

David G Lambert1, Joshua S Mincer2

  • 1Department of Cardiovascular Sciences, Anaesthesia, Critical Care and Pain Management, University of Leicester, Hodgkin Building, Leicester, UK.

British Journal of Anaesthesia
|January 8, 2025
PubMed

Insights

Kappa opioid (KOP) receptor agonists show promise beyond pain relief. Research indicates KOP receptor activation induces glioma cell death, suggesting potential as a novel cancer therapy adjunct.

Area of Science:

  • Neuroscience and Oncology
  • Molecular Biology and Pharmacology

Background:

  • Kappa opioid (KOP) receptor agonists are known for analgesic properties but face limitations due to central side-effects.
  • Emerging research highlights non-analgesic roles of opioid receptors, prompting investigation into novel therapeutic applications.
  • High KOP receptor expression in glioma tissue has been linked to improved patient survival.

Purpose of the Study:

  • To investigate the potential of KOP receptor agonism as a therapeutic strategy for glioma.
  • To explore the mechanism by which KOP receptor activation influences glioma cell apoptosis.

Main Methods:

  • Analysis of KOP receptor expression in glioma tissues.
  • Assessment of KOP receptor agonist effects on glioma cell apoptosis.
  • Investigation of the involvement of the p38 MAPK pathway in KOP receptor-mediated effects.

Main Results:

  • A correlation was found between high KOP receptor expression in glioma and improved patient survival.
  • KOP receptor agonism was demonstrated to promote apoptosis in glioma cells.
  • The pro-apoptotic effect of KOP receptor agonism is mediated through the regulation of the p38 MAPK oncogenic pathway.

Conclusions:

  • KOP receptor ligands represent a promising therapeutic avenue for glioma treatment.
  • KOP receptor agonists may serve as effective chemotherapeutic adjuncts, enhancing glioma cell death.
  • Targeting the KOP receptor and its downstream pathways offers a novel strategy in cancer therapy.
Keywords:
analgesiakappa opioid receptoropioidtumour biology

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