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

doi:10.1007/s10637-009-9219-7

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 journal › Article › peer-review

66 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 language	English (US)
Pages (from-to)	107-114
Number of pages	8
Journal	Investigational New Drugs
Volume	28
Issue number	2
DOIs	https://doi.org/10.1007/s10637-009-9219-7
State	Published - Apr 2010
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Hepatitis B
Hepatocellular carcinoma
PXD101
Tumor suppressor genes

ASJC Scopus subject areas

Oncology
Pharmacology
Pharmacology (medical)

Access to Document

10.1007/s10637-009-9219-7

Cite this

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

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.",

keywords = "Hepatitis B, Hepatocellular carcinoma, PXD101, Tumor suppressor genes",

author = "Ma, \{Brigette B.Y.\} and Fion Sung and Qian Tao and Poon, \{Fan Fong\} and Lui, \{Vivian W.\} and Winnie Yeo and Chan, \{Stephen L.\} and Chan, \{Anthony T.C.\}",

note = "Funding Information: Acknowledgements This study was sponsored by the Cancer Therapy Evaluation Program of the National Cancer Institute (Bethesda, USA). Result of this study was presented as a poster at the 98th American Association of Cancer Research annual meeting in April 2007, Los Angeles; abstract number 2494. This study was funded by the Direct Grant of the Chinese University of Hong Kong (Reference 2005.1.018), and the Li Ka Shing Institute for Health Sciences.",

year = "2010",

month = apr,

doi = "10.1007/s10637-009-9219-7",

language = "English (US)",

volume = "28",

pages = "107--114",

journal = "Investigational New Drugs",

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T1 - The preclinical activity of the histone deacetylase inhibitor PXD101 (belinostat) in hepatocellular carcinoma cell lines

AU - Ma, Brigette B.Y.

AU - Sung, Fion

AU - Tao, Qian

AU - Poon, Fan Fong

AU - Lui, Vivian W.

AU - Yeo, Winnie

AU - Chan, Stephen L.

AU - Chan, Anthony T.C.

N1 - Funding Information: Acknowledgements This study was sponsored by the Cancer Therapy Evaluation Program of the National Cancer Institute (Bethesda, USA). Result of this study was presented as a poster at the 98th American Association of Cancer Research annual meeting in April 2007, Los Angeles; abstract number 2494. This study was funded by the Direct Grant of the Chinese University of Hong Kong (Reference 2005.1.018), and the Li Ka Shing Institute for Health Sciences.

PY - 2010/4

Y1 - 2010/4

N2 - 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.

AB - 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.

KW - Hepatitis B

KW - Hepatocellular carcinoma

KW - PXD101

KW - Tumor suppressor genes

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

Abstract

UN SDGs

Keywords

ASJC Scopus subject areas

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