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Signal transduction, dimerization, and therapeutic targeting of Orexin and receptor systems

Shengnan Zhang1, Peixiang Wang1, Bingyuan Ji1

  • 1Neurobiology Key Laboratory of Jining Medical University, Jining, China.

Frontiers in Pharmacology
|December 12, 2025
PubMed

Insights

Orexin receptors (OXRs) form dimers, enabling biased signaling for targeted therapies. Antagonists show promise for sleep, metabolic, and psychiatric disorders, with TM peptides offering novel strategies.

Area of Science:

  • Neuroscience
  • Pharmacology
  • Structural Biology

Background:

  • Orexin receptors (OXRs) are GPCRs activated by orexin peptides, crucial for nervous system functions.
  • OXRs form homodimers and heterodimers, leading to biased signaling pathways.

Purpose of the Study:

  • To synthesize current knowledge on orexin receptor systems.
  • To explore OXR dimerization, signaling, and therapeutic potential.
  • To evaluate OXR-targeting drugs for neurological disorders.

Main Methods:

  • Literature review of OXR structure, signaling, and dimerization.
  • Analysis of current and emerging OXR antagonist compounds.
  • Investigation of molecular pathological mechanisms in neurological disorders.

Main Results:

  • Orexin receptor dimerization generates biased signaling, a basis for precision pharmacology.
  • OXR antagonists are effective for sleep, metabolic, and psychiatric conditions.
  • Transmembrane peptides targeting dimer interfaces are a novel therapeutic approach.

Conclusions:

  • Orexin receptor systems offer valuable therapeutic targets for neurological disorders.
  • Understanding OXR dimerization is key to developing pathway-specific drugs.
  • Further research into OXR antagonists and TM peptides can advance pharmaceutical development.
Keywords:
GPCR signalingGPCRsdepressionneurologyneuropharmacology

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