The role of protein kinase C in the regulation of serotonin-2A receptor expression

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A Anji1, N R Sullivan Hanley, M Kumari

  • 1Department of Pharmacology, University of Texas Health Science Center, San Antonio, Texas, USA.

Journal of Neurochemistry
|April 12, 2001
PubMed

Insights

Protein kinase C (PKC) regulates serotonin (5-HT) receptor expression in C6 glioma cells. Agonist treatment decreases 5-HT(2A) receptor mRNA before binding sites, a process inhibited by PKC blockers, implicating PKC alpha and gamma.

Area of Science:

  • Neuropharmacology
  • Molecular Biology
  • Cell Signaling

Background:

  • Serotonin (5-HT) receptors are crucial in neurological function.
  • Agonist treatment can lead to receptor downregulation.
  • Protein kinase C (PKC) involvement in receptor regulation is not fully understood.

Purpose of the Study:

  • To investigate the role of PKC in regulating serotonin type 2A (5-HT(2A)) receptor expression in C6 glioma cells following agonist treatment.
  • To determine if changes in 5-HT(2A) receptor mRNA levels precede alterations in receptor binding sites.

Main Methods:

  • C6 glioma cells were treated with serotonin (5-HT).
  • Receptor number and mRNA levels were quantified over time.
  • PKC inhibitors (bisindolylmaleimide, calphostin C, Gö 6976) were used.
  • Western blot analysis identified PKC isoform expression and localization.

Main Results:

  • 5-HT treatment decreased 5-HT(2A) receptor mRNA before receptor binding sites.
  • This mRNA decrease was independent of transcript stability.
  • PKC inhibition blocked 5-HT-induced mRNA decrease and receptor downregulation.
  • PKC alpha and gamma isoforms translocated to the nucleus upon 5-HT treatment.

Conclusions:

  • PKC plays a significant role in the agonist-induced regulation of 5-HT(2A) receptor mRNA and binding sites.
  • Conventional PKC isoforms, specifically PKC alpha and/or PKC gamma, are implicated in this regulatory pathway.

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