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Transcriptional repression of RORalpha activity in human breast cancer cells by melatonin

J Dai1, P T Ram, L Yuan

  • 1Department of Structural and Cellular Biology, Tulane University School of Medicine, 1430 Tulane Avenue, New Orleans, LA 70112, USA.

Insights

Melatonin inhibits breast cancer cell growth by affecting retinoid orphan receptor alpha (RORalpha) activity. This occurs through the calcium/calmodulin signaling pathway, impacting RORalpha-regulated genes.

Area of Science:

  • Endocrinology
  • Molecular Biology
  • Cancer Research

Background:

  • Melatonin is known to inhibit MCF-7 human breast cancer cell proliferation.
  • Melatonin's mechanisms of action involve G-protein coupled membrane receptors or retinoid orphan receptors (RORalphas).

Purpose of the Study:

  • To investigate the role of RORalpha in melatonin's effect on MCF-7 cells.
  • To explore the involvement of the Ca2+/CaM signaling pathway in RORalpha regulation by melatonin.

Main Methods:

  • Demonstrated expression of RORalpha2, 3, and 4 transcripts in MCF-7 cells.
  • Assessed RORalpha transcriptional activity, DNA-binding activity, and protein levels.
  • Investigated the impact of melatonin and Ca2+/CaM signaling pathway modulators.

Main Results:

  • MCF-7 cells express RORalpha2, 3, and 4 transcripts with high basal RORalpha transcriptional activity.
  • Melatonin repressed RORalpha transactivation and DNA-binding activity in serum-stimulated MCF-7 cells without altering RORalpha protein levels.
  • RORalpha transcriptional activity was modulated by Ca2+/CaM signaling pathway modulators.

Conclusions:

  • Melatonin may inhibit breast cancer cell proliferation by modulating RORalpha transcriptional activity via the Ca2+/CaM signaling pathway.
  • This pathway influences RORalpha-regulated gene expression, offering a potential therapeutic target.

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