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Discovery of a chemical compound that suppresses expression of BEX2, a dormant cancer stem cell-related protein

Satoshi Saijoh1, Mao Nakamura-Shima2, Rie Shibuya-Takahashi2

  • 1Division of Cancer Stem Cells, Miyagi Cancer Center Research Institute, 47-1, Medeshima-Shiode, Natori, Miyagi, Japan; Department of Otolaryngology-Head and Neck Surgery, Tohoku University Graduate School of Medicine, 2-1 Seiryo-machi, Aoba-ku, Sendai, Miyagi, Japan; Head and Neck Surgery, Miyagi Cancer Center, 47-1, Medeshima-Shiode, Natori, Miyagi, Japan.

Biochemical and Biophysical Research Communications
|January 7, 2021
PubMed

Insights

Researchers identified BMPP, a novel compound that inhibits BEX2 expression in cancer stem cells (CSCs). This inhibition reduces dormant CSC phenotypes, offering potential for new cancer therapies targeting BEX2-overexpressing cancers.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Cancer stem cells (CSCs) drive metastasis and recurrence.
  • BEX2 (brain expressed X-linked gene 2) is a CSC-related gene associated with chemotherapy resistance in cholangiocarcinoma.
  • Targeting BEX2 may offer a therapeutic strategy against CSCs.

Purpose of the Study:

  • To identify small compounds that inhibit BEX2 expression.
  • To find compounds that attenuate CSC-related phenotypes.
  • To explore novel therapeutic agents for BEX2-overexpressing cancers.

Main Methods:

  • High-throughput screening of 9600 small chemical compounds.
  • Utilized cholangiocarcinoma cell line HuCCT1 expressing BEX2-NanoLuc fusion protein.
  • Evaluated compound effects on BEX2 expression, cell cycle, ATP levels, and chemosensitivity.

Main Results:

  • Identified BMPP (1, 3-Benzenediol, [4-(4-methoxyphenyl)-1H-pyrazol-3-yl]) as a BEX2 inhibitor.
  • BMPP decreased BEX2 protein expression and the G0 phase population of tumor cells.
  • BMPP increased ATP levels and chemotherapeutic sensitivity.

Conclusions:

  • BMPP effectively reduces dormant CSC phenotypes by inhibiting BEX2.
  • BMPP is a promising compound for developing novel cancer therapeutics.
  • This discovery opens avenues for treating cancers characterized by BEX2-overexpressing CSCs.
Keywords:
BEX2CholangiocarcinomaDormant cancer stem cellHepatocellular carcinoma

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