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

Satoshi Saijoh, Mao Nakamura-Shima, Rie Shibuya-Takahashi, Ryo Ito, Akira Sugawara, Tomoko Yamazaki, Takayuki Imai, Yukinori Asada, Kazuto Matsuura, Wataru Iwai, Yuta Wakui, Makoto Abue, Sadafumi Kawamura, Yu Katayose, Haruna Fujimori, Mai Mochizuki, Jun Yasuda, Kazunori Yamaguchi, Kazuo Sugamura, Kennichi SatohYukio Katori, Keiichi Tamai

研究成果: Article査読

抄録

Cancer stem cells (CSCs) are believed to cause cancer metastasis and recurrence. BEX2 (brain expressed X-linked gene 2) is a CSC-related gene that is expressed in dormant CSCs in cholangiocarcinoma and induces resistance against chemotherapy. The aim of the present study was to identify small compounds that have activity to inhibit BEX2 expression and result in the attenuation of CSC-related phenotypes. We screened 9600 small chemical compounds in high-throughput screening using cholangiocarcinoma cell line HuCCT1 expressing BEX2 protein fused with NanoLuc, and identified a compound, BMPP (1, 3-Benzenediol, [4-(4-methoxyphenyl)-1H-pyrazol-3-yl]). BMPP was found to exert decreasing effects on BEX2 protein expression and G0 phase population of the tumor cells, and increasing effects on ATP levels and chemotherapeutic sensitivity of the cells. These findings indicate that BMPP is a valuable chemical compound for reducing dormant CSC-related phenotypes. Thus, the identification of BMPP as a potential CSC suppressor provides scope for the development of novel therapeutic modalities for the treatment of cancers with BEX2 overexpressing CSCs.

本文言語English
ページ(範囲)132-139
ページ数8
ジャーナルBiochemical and biophysical research communications
537
DOI
出版ステータスPublished - 2021 1 22

ASJC Scopus subject areas

  • 生物理学
  • 生化学
  • 分子生物学
  • 細胞生物学

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