Histone Deacetylase Inhibitors: Recent Insights from Basic to Clinical Knowledge & Patenting of Anti-Cancer Actions

被引:29
作者
Carafa, Vincenzo [1 ]
Nebbioso, Angela [1 ]
Altucci, Lucia [1 ,2 ]
机构
[1] Univ Naples 2, Dipartimento Patol Gen, I-80138 Naples, Italy
[2] CNR IGB, I-80100 Naples, Italy
关键词
Cancer; epigenetics; human diseases; HDAC inhibitors; neurodegeneration; signal transduction; SUBEROYLANILIDE HYDROXAMIC ACID; PHASE-II TRIAL; ANTITUMOR-ACTIVITY; HDAC INHIBITOR; CELL-DEATH; IN-VITRO; ISOFORM SELECTIVITY; HODGKIN-LYMPHOMA; DNA METHYLATION; VORINOSTAT;
D O I
10.2174/157489211793980088
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
Epigenetic modifications have been causally linked to cancer development and progression, and are potentially reversible by drug treatments. The N-terminal tails of histones contain amino acid residues modifiable by posttranslational modifications such as acetylation. Given that HDAC inhibitors induce cancer cell differentiation and death, an increasing number of these compounds has been synthesized in the last ten years. Many HDAC inhibitors are in clinical trials for the treatment of cancer. Two of them, the hydroxamic acid (SAHA) and Romidepsin (FK 228), are approved in the second line treatment of refractory, persistent or relapsed Cutaneous T Cell Lymphoma (CTCL). The growing evidence of the potential benefits of an anti-cancer treatment based on the use of HDAC inhibitors have led to a large number of patent applications all over the world. The aim of this review is to give an overview of the basic current knowledge and molecular mechanisms of HDAC inhibitors and their clinical trials as well as to focus on the recent patent applications existing in the field of HDAC inhibitors and cancer treatment between 2008 and 2010 in USA.
引用
收藏
页码:131 / 145
页数:15
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