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Issue 4, 2012
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Largazole: From discovery to broad-spectrum therapy

Jiyong Hong*a  and  Hendrik Luesch*b 
Author affiliations

* Corresponding authors

a Department of Chemistry, Duke University, Durham, USA
E-mail: jiyong.hong@duke.edu

b Department of Medicinal Chemistry, University of Florida, Gainesville, USA
E-mail: luesch@cop.ufl.edu

Abstract

Covering up to 2011

The cyclic depsipeptide largazole from a cyanobacterium of the genus Symploca is a marine natural product with a novel chemical scaffold and potently inhibits class I histone deacetylases (HDACs). Largazole possesses highly differential growth-inhibitory activity, preferentially targeting transformed over non-transformed cells. The intriguing structure and biological activity of largazole have attracted strong interest from the synthetic chemistry community to establish synthetic routes to largazole and to investigate its potential as a cancer therapeutic. This Highlight surveys recent advances in this area with a focus on the discovery, synthesis, target identification, structure–activity relationships, HDAC8–largazole thiol crystal structure, and biological studies, including in vivo anticancer and osteogenic activities.

Graphical abstract: Largazole: From discovery to broad-spectrum therapy

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Supplementary files

Publication details

The article was received on 01 Sep 2011 and first published on 14 Feb 2012


Article type: Highlight
DOI: 10.1039/C2NP00066K
Citation: Nat. Prod. Rep., 2012,29, 449-456
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    Largazole: From discovery to broad-spectrum therapy

    J. Hong and H. Luesch, Nat. Prod. Rep., 2012, 29, 449
    DOI: 10.1039/C2NP00066K

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