A novel anti-cancer agent, acetyltanshinone IIA, inhibits oestrogen receptor positive breast cancer cell growth by down-regulating the oestrogen receptor

Ting Yu, Zhicai Zhou, Yuguang Mu, Gilberto De Lima Lopes, Kathy Qian Luo

Research output: Contribution to journalArticlepeer-review

Abstract

In this paper we show that acetyltanshinone IIA (ATA), a novel anti-cancer agent, preferentially inhibits cell growth of oestrogen receptor positive (ER+) breast cancer cells and that it is more potent than the commonly used anti-breast cancer agent, tamoxifen. The metabolic product of ATA, hydroquinone tanshinone IIA (HTA) binds to the ERα and causes its degradation mainly in the nucleus via an ubiquitin-mediated proteasome-dependent pathway. In addition, ATA also reduced the mRNA levels of the ERα encoding gene, ESR1, distinguishing ATA from another anti-breast cancer drug, fulvestrant. Finally, ATA reduced the transcription of an ER-responsive gene, GREB1.

Original languageEnglish (US)
Pages (from-to)94-103
Number of pages10
JournalCancer Letters
Volume346
Issue number1
DOIs
StatePublished - Apr 28 2014

Keywords

  • Acetyltanshinone IIA
  • Anti-breast cancer agent
  • Fulvestrant
  • Oestrogen receptor
  • Tamoxifen

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

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