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Largazole: from discovery to broad-spectrum therapy.

Publication ,  Journal Article
Hong, J; Luesch, H
Published in: Natural product reports
April 2012

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.

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Published In

Natural product reports

DOI

EISSN

1460-4752

ISSN

0265-0568

Publication Date

April 2012

Volume

29

Issue

4

Start / End Page

449 / 456

Related Subject Headings

  • Thiazoles
  • Structure-Activity Relationship
  • Organic Chemistry
  • Molecular Structure
  • Marine Biology
  • Humans
  • Histone Deacetylase Inhibitors
  • Depsipeptides
  • Cyanobacteria
  • Biological Products
 

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Hong, J., & Luesch, H. (2012). Largazole: from discovery to broad-spectrum therapy. Natural Product Reports, 29(4), 449–456. https://doi.org/10.1039/c2np00066k
Hong, Jiyong, and Hendrik Luesch. “Largazole: from discovery to broad-spectrum therapy.Natural Product Reports 29, no. 4 (April 2012): 449–56. https://doi.org/10.1039/c2np00066k.
Hong J, Luesch H. Largazole: from discovery to broad-spectrum therapy. Natural product reports. 2012 Apr;29(4):449–56.
Hong, Jiyong, and Hendrik Luesch. “Largazole: from discovery to broad-spectrum therapy.Natural Product Reports, vol. 29, no. 4, Apr. 2012, pp. 449–56. Epmc, doi:10.1039/c2np00066k.
Hong J, Luesch H. Largazole: from discovery to broad-spectrum therapy. Natural product reports. 2012 Apr;29(4):449–456.
Journal cover image

Published In

Natural product reports

DOI

EISSN

1460-4752

ISSN

0265-0568

Publication Date

April 2012

Volume

29

Issue

4

Start / End Page

449 / 456

Related Subject Headings

  • Thiazoles
  • Structure-Activity Relationship
  • Organic Chemistry
  • Molecular Structure
  • Marine Biology
  • Humans
  • Histone Deacetylase Inhibitors
  • Depsipeptides
  • Cyanobacteria
  • Biological Products