Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2021 Mar 22;11(3):223.
doi: 10.3390/jpm11030223.

Histone Deacetylase Inhibitors in the Treatment of Hepatocellular Carcinoma: Current Evidence and Future Opportunities

Nikolaos Garmpis  1   2 , Christos Damaskos  2   3 , Anna Garmpi  4 , Vasiliki E Georgakopoulou  5   6 , Panagiotis Sarantis  7 , Efstathios A Antoniou  1   2 , Michalis V Karamouzis  7 , Afroditi Nonni  8 , Dimitrios Schizas  9 , Evangelos Diamantis  10 , Evangelos Koustas  7 , Paraskevi Farmaki  11 , Athanasios Syllaios  9 , Alexandros Patsouras  12 , Konstantinos Kontzoglou  1   2 , Nikolaos Trakas  13 , Dimitrios Dimitroulis  1
Affiliations
Review

Histone Deacetylase Inhibitors in the Treatment of Hepatocellular Carcinoma: Current Evidence and Future Opportunities

Nikolaos Garmpis et al. J Pers Med. .

Abstract

Hepatocellular carcinoma (HCC) remains a major health problem worldwide with a continuous increasing prevalence. Despite the introduction of targeted therapies like the multi-kinase inhibitor sorafenib, treatment outcomes are not encouraging. The prognosis of advanced HCC is still dismal, underlying the need for novel effective treatments. Apart from the various risk factors that predispose to the development of HCC, epigenetic factors also play a functional role in tumor genesis. Histone deacetylases (HDACs) are enzymes that remove acetyl groups from histone lysine residues of proteins, such as the core nucleosome histones, in this way not permitting DNA to loosen from the histone octamer and consequently preventing its transcription. Considering that HDAC activity is reported to be up-regulated in HCC, treatment strategies with HDAC inhibitors (HDACIs) showed some promising results. This review focuses on the use of HDACIs as novel anticancer agents and explains the mechanisms of their therapeutic effects in HCC.

Keywords: HCC; HDAC; HDACI; anticancer; deacetylase; epigenetic; hepatocellular carcinoma; histone; inhibitors; targeted; therapeutics.

PubMed Disclaimer

Conflict of interest statement

All authors declare that there is no conflict of interest.

Figures

Figure 1
Figure 1
The structure of the nucleosome and the action of histone acetyltransferases and histone deacetylases.
See this image and copyright information in PMC

References

    1. Siegel R.L., Miller K.D., Jemal A. Cancer statistics, 2016. Cancer J. Clin. 2016;66:7–30. doi: 10.3322/caac.21332. - DOI - PubMed
    1. Dimitroulis D., Damaskos C., Valsami S., Davakis S., Garmpis N., Spartalis E., Athanasiou A., Moris D., Sakellariou S., Kykalos S., et al. From diagnosis to treatment of hepatocellular carcinoma: An epidemic problem for both developed and developing world. World J. Gastroenterol. 2017;23:5282–5294. doi: 10.3748/wjg.v23.i29.5282. - DOI - PMC - PubMed
    1. Ferlay J., Soerjomataram I., Dikshit R., Eser S., Mathers C., Rebelo M., Parkin D.M., Forman D., Bray F. Cancer incidence and mortality worldwide: Sources, methods and major patterns in GLOBOCAN 2012. Int. J. Cancer. 2015;136:E359–E386. doi: 10.1002/ijc.29210. - DOI - PubMed
    1. Jemal A., Bray F., Center M.M., Ferlay J., Ward E., Forman D. Global cancer statistics. Cancer J. Clin. 2011;61:69–90. doi: 10.3322/caac.20107. - DOI - PubMed
    1. Centers for Disease Control and Prevention (CDC) Hepatocellular carcinoma—United States, 2001–2006. Morb. Mortal. Wkly. Rep. 2010;59:517–520. - PubMed

LinkOut - more resources