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Endocrine Regulations Vol.43, No.1, p.23-28, 2009 |
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Title: OPIOID ANTAGONIST-INDUCED REGULATION OF THE µ-OPIOID RECEPTOR EXPRESSION IN MCF-7 BREAST CANCER CELL LINE | ||
Author: K. Gach, M. Piestrzeniewicz, J. Fichna, J. Szemraj, A. Janecka | ||
Abstract: Objective. In our earlier study we have demonstrated that MCF-7 cell line expresses all three opioid receptor types, µ, δ and κ (MOR, DOR and KOR, respectively), but predominantly MOR. Morphine, as well as endogenous MOR-selective agonists, endomorphin-1 and endomorphin-2 were shown to decrease MOR gene expression in MCF-7 cells. Opioid antagonist – naloxone –produced the opposite effect, increasing MOR gene expression. In this study we investigated and compared the influence of several opioid antagonists of alkaloid structure (β-funaltrexamine and naloxonazine) and of peptide structure: [Dmt1, D-1-Nal4]endomorphin-2, [Dmt, D-2-Nal4]endomorphin-1, and [Dmt, D-2-Nal4]endomorphin-2 on MOR up-/down-regulation and proliferation in MCF-7 cell line. Methods. MCF-7 cells were incubated with opioids. The levels of MOR mRNA were assessed using quantitative real-time RT-PCR assay. Cell growth was measured by Mosmann tetrazolium salt assay. Results. It was shown that all tested opioid antagonists produced up-regulation of MOR gene expression, but the strongest effect was observed with naloxonazine. However, none of the antagonists at concentrations as high as 10-4 M showed any antiproliferative effects on MCF-7 cells, neither in the presence or absence of β-estradiol. Conclusion. It seems that up- or down-regulation of MOR mRNA levels has no direct effect on cell proliferation. |
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Keywords: Gene expression – Opioid receptors – Endomorphins – Morphine – Naloxone | ||
Year: 2009, Volume: 43, Issue: 1 | Page From: 23, Page To: 28 | |
doi:10.4149/endo_2009_01_23 |
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