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The Effect of Selective Estrogen Receptor Modulators (SERMs) on the Tamoxifen Resistant Breast Cancer Cells

Bo Yoon Chang1, Sae Am Kim, Bindu Malla

  • 1Institute of Pharmaceutical Research and Development, College of Pharmacy, Wonkwang University, Iksan 570-749, Korea.

Toxicological Research
|November 27, 2013
PubMed

Insights

Toremifene and ospemifene show effectiveness against tamoxifen-resistant breast cancer cells. Toremifene is particularly promising for treating tamoxifen-resistant estrogen receptor-positive breast cancers.

Area of Science:

  • Pharmacology and Therapeutics
  • Oncology
  • Molecular Biology

Background:

  • Selective estrogen receptor modulators (SERMs) are crucial in treating estrogen receptor (ER)-positive breast cancers.
  • Tamoxifen, a widely used SERM, faces challenges due to acquired resistance and side effects.
  • Investigating alternative SERMs for tamoxifen-resistant breast cancer is critical for improving patient outcomes.

Purpose of the Study:

  • To evaluate the efficacy of conventional SERMs against tamoxifen-resistant breast cancer cells.
  • To identify SERMs that retain cytotoxic activity in the context of tamoxifen resistance.

Main Methods:

  • Comparative analysis of SERM effectiveness on MCF-7 (ER-positive) and tamoxifen-resistant breast cancer cell lines.
  • Assessment of cell proliferation inhibition and cytotoxic activity of various SERMs.

Main Results:

  • Most SERMs were less effective on tamoxifen-resistant cells compared to MCF-7 cells.
  • Toremifene demonstrated superior efficacy in tamoxifen-resistant cells over MCF-7 cells.
  • Ospemifene exhibited similar cytotoxic activity on both cell types, while other SERMs showed limited efficacy.

Conclusions:

  • Toremifene presents a potential therapeutic option for tamoxifen-resistant breast cancer.
  • The mechanism of toremifene's action in resistant cells may involve pathways beyond apoptosis and autophagy.
  • Further research is warranted to elucidate the precise molecular mechanisms underlying toremifene's effectiveness.
Keywords:
ApoptosisAutophagySelective estrogen receptor modulators (SERMs)Tamoxifen resistant breast cancerToremifene

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