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01.04.2010 | PRECLINICAL STUDIES

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

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

Erschienen in: Investigational New Drugs | Ausgabe 2/2010

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Summary

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.

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Titel: The preclinical activity of the histone deacetylase inhibitor PXD101 (belinostat) in hepatocellular carcinoma cell lines
verfasst von: Brigette B.Y. Ma
Fion Sung
Qian Tao
Fan Fong Poon
Vivian W. Lui
Winnie Yeo
Stephen L. Chan
Anthony T.C. Chan
Publikationsdatum: 01.04.2010
Verlag: Springer US
Erschienen in: Investigational New Drugs / Ausgabe 2/2010
Print ISSN: 0167-6997
Elektronische ISSN: 1573-0646
DOI: https://doi.org/10.1007/s10637-009-9219-7

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

Summary

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