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Issue 10, 2009
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Discovery, biological activity, synthesis and potential therapeutic utility of naturally occurring histone deacetylase inhibitors

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Abstract

Covering: up to 2009

A number of small-molecule natural products have been shown to inhibit the activity of histone deacetylases (HDACs). These enzymes catalyze the hydrolysis of N-acetyl lysine residues of the histone proteins that package chromosomal DNA and thereby play a vital role in mediating gene expression. HDAC inhibitors (HDACi) are potent cytotoxic agents with significant potential as anticancer therapeutics and it is currently thought that their selective activity on members of specific subclasses of the eighteen known human HDAC isoforms is important to this activity and to moderation of their toxicity. Herein, we discuss both linear and cyclic HDACi, as well as selected synthetically derived analogs.

Graphical abstract: Discovery, biological activity, synthesis and potential therapeutic utility of naturally occurring histone deacetylase inhibitors

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Publication details

The article was received on 04 Apr 2009 and first published on 03 Aug 2009


Article type: Review Article
DOI: 10.1039/B817886K
Nat. Prod. Rep., 2009,26, 1293-1320

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    Discovery, biological activity, synthesis and potential therapeutic utility of naturally occurring histone deacetylase inhibitors

    T. L. Newkirk, A. A. Bowers and R. M. Williams, Nat. Prod. Rep., 2009, 26, 1293
    DOI: 10.1039/B817886K

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