AJTR Copyright © 2009-All rights reserved. Published by e-Century Publishing Corporation, Madison, WI 53711
Am J Translational Res 2011;3(2):166-179

Review Article
Histone deacetylase inhibitors: Molecular mechanisms of action and
clinical trials as anti-cancer drugs

Hyun-Jung Kim, Suk-Chul Bae

BioRunx Co., Ltd., 12 Gaesin-dong, Huengduk-gu, Cheongju, Chungbuk, 361-763, South Korea; Department of
Biochemistry, School of Medicine, Institute for Tumor Research, Chungbuk National University, 12 Gaesin-dong,
Huengduk-gu, Cheongju, Chungbuk, 361-763, South Korea

Received December 20, 2010; accepted December 25, 2010; Epub December 26, 2010; Published January 1,
2011

Abstract: Histone deacetylase (HDAC) inhibitors are a relatively new class of anti-cancer agents that play
important roles in epigenetic or non-epigenetic regulation, inducing death, apoptosis, and cell cycle arrest in
cancer cells. Recently, their use has been clinically validated in cancer patients resulting in the approval of two
HDAC inhibitors, vorinostat and depsipetide, by the FDA. Also, clinical trials of several HDAC inhibitors for use as
anti-cancer drugs (alone or in combination with other anti-cancer therapeutics) are ongoing. However, the
molecular mechanisms underlying the response to HDAC inhibitors in cancer patients are not fully understood. In
this review, we summarize our understanding of the molecular and biological events that underpin the anticancer
effects of HDAC inhibitors and the outcomes of recent clinical trials involving these drugs.(AJTR1012002).

Keywords: HDAC inhibitor, acetylation, cancer, vorinostat (SAHA), depsipeptide (FK228), MS-275

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Address all correspondence to:
Suk-Chul Bae, PhD
Department of Biochemistry, School of Medicine
Institute for Tumor Research, Chungbuk National University
Cheongju, Chungbuk, 361-763, South Korea
Tel: +82-43-261-2842
Fax: +82-43-274-8705
E-mail:
scbae@chungbuk.ac.kr