Largazole: from discovery to broad-spectrum therapy.

Journal Article (Review;Journal Article)

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.

Full Text

Duke Authors

Cited Authors

  • Hong, J; Luesch, H

Published Date

  • April 2012

Published In

Volume / Issue

  • 29 / 4

Start / End Page

  • 449 - 456

PubMed ID

  • 22334030

Pubmed Central ID

  • PMC4777309

Electronic International Standard Serial Number (EISSN)

  • 1460-4752

International Standard Serial Number (ISSN)

  • 0265-0568

Digital Object Identifier (DOI)

  • 10.1039/c2np00066k


  • eng