The preclinical activity of the histone deacetylase inhibitor PXD101 (belinostat) in hepatocellular carcinoma cell lines

Brigette B.Y. Ma, Fion Sung, Qian Tao, Fan Fong Poon, Vivian W. Lui, Winnie Yeo, Stephen L. Chan, Anthony T.C. Chan

Research output: Contribution to journalArticlepeer-review

59 Scopus citations

Abstract

The activity of the histone deacetylase inhibitor PXD101 was investigated in three hepatocellular carcinoma (HCC) cell lines. PXD101was found to inhibit cell growth at a dose-dependent manner and induce histone acetylation in PLC/PRF/5, Hep3B and HepG2 cells. In PLC/PRF/5 and Hep3B cells which express hepatitis B-related genes (HBx, HBc and HBc), treatment with PXD101 resulted in apoptosis without a significant effect on viral gene expression. Exposure to PXD101 for up to 48 h had varying effects on the expression of 12 cellular genes with tumor suppressor functions, including p21, SOCS1, CMTM5, RASAL1, DLEC1, SFRP (-1, -2, -4 and -5), ADAMTS (-8 and -9). This study provided the basis for a phase II clinical trial of PXD101 in inoperable hepatitis-B associated HCC.

Original languageEnglish (US)
Pages (from-to)107-114
Number of pages8
JournalInvestigational New Drugs
Volume28
Issue number2
DOIs
StatePublished - Apr 2010
Externally publishedYes

Keywords

  • Hepatitis B
  • Hepatocellular carcinoma
  • PXD101
  • Tumor suppressor genes

ASJC Scopus subject areas

  • Oncology
  • Pharmacology
  • Pharmacology (medical)

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