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Histone Demethylase LSD1 Inhibitors Prevent Cell Growth by Regulating Gene Expression in Esophageal Squamous Cell

Isamu Hoshino1, Yasunori Akutsu2, Kentaro Murakami2

  • 1Department of Frontier Surgery, Graduate School of Medicine, Chiba University, Chiba, Japan. i_hosino@chiba-u.jp.

Annals of Surgical Oncology
|March 21, 2015
PubMed
Abstract

Insights

The LSD1 inhibitor NCL1 suppressed esophageal squamous cell cancer (ESCC) growth and induced apoptosis. Gene expression analysis revealed PHLDB2 as a key gene targeted by NCL1, correlating with poor prognosis in ESCC patients.

Area of Science:

  • Molecular Biology
  • Cancer Research
  • Epigenetics

Background:

  • Gene expression is regulated by histone acetylation and demethylation.
  • Imbalances in these processes are linked to cancer development.
  • The precise mechanisms of histone demethylase LSD1 inhibitors' antitumor effects remain unclear.

Purpose of the Study:

  • To investigate the antitumor effects of the LSD1 inhibitor NCL1 in esophageal squamous cell cancer (ESCC).
  • To comprehensively analyze gene expression changes induced by NCL1 in ESCC cells.
  • To elucidate the role of specific genes in the observed antitumor activity.

Main Methods:

  • Treatment of ESCC cell lines (T.Tn and TE2) with NCL1.
  • Microarray analysis to assess global gene expression changes.
  • Loss-of-function assays using siRNA to evaluate gene function.

Main Results:

  • NCL1 significantly inhibited ESCC cell proliferation and induced apoptosis.
  • NCL1 altered the expression of numerous genes, with 27 common to both cell lines studied.
  • PHLDB2, a gene downregulated by NCL1, was overexpressed in ESCC tumors and associated with poor prognosis.

Conclusions:

  • NCL1 demonstrates significant antitumor activity in ESCC.
  • Gene expression profiling provides insights into the mechanisms of LSD1 inhibitors.
  • PHLDB2 may serve as a potential biomarker for prognosis in ESCC.

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