Drug Discov Ther. 2014;8(5):225-228. (DOI: 10.5582/ddt.2014.01034)

HDAC1/3 dual selective inhibitors - New therapeutic agents for the potential treatment of cancer.

Li XY, Xu WF


Histone deacetylases (HDACs) have attracted a great deal of interest as anticancer drug targets, and many HDAC inhibitors (HDACIs) have displayed clinical efficacy in treating specific tumors. However, all of these agents have significant toxicity, including fatigue, nausea, vomiting, thrombocytopenia, and neutropenia. Thus, increased effort is being directed toward developing selective HDACIs that are tolerated better and cause fewer adverse reactions. This article focuses mainly on the N-hydroxycinnamamide-based HDAC 1/3 dual inhibitors, and this article outlines the anticancer potential of these inhibitors. Since selective HDAC1/3 inhibitors may cause fewer adverse reactions than selective pan-HDACIs and selective Class Ι inhibitors in clinical settings, further study of their mechanism of anticancer activity and optimization of their structure is warranted.

KEYWORDS: Epigenetic, HDACs, selective HDACIs, HDAC1/3 selective inhibitors, anti-cancer agent

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