Acyldepsipeptide HDAC inhibitor production induced in Burkholderia thailandensis

Org Lett. 2011 Mar 18;13(6):1536-9. doi: 10.1021/ol200225v. Epub 2011 Feb 24.

Abstract

Natural product gene clusters are often tightly regulated, resulting in gene cluster silencing in laboratory fermentation studies. The systematic overexpression of transcription factors (TFs) associated with biosynthetic gene clusters found in the genome of Burkholderia thailandensis E264 identified a set of TFs that, when overexpressed, alter the secondary metabolome of this bacterium. The isolation and characterization of burkholdacs A and B, two new acyldepsitripeptide histone deacetylase inhibitors produced by B. thailandensis overexpressing the TF bhcM, is reported.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Burkholderia / chemistry
  • Burkholderia / genetics
  • Burkholderia / metabolism*
  • Depsipeptides / chemistry
  • Depsipeptides / isolation & purification*
  • Depsipeptides / pharmacology*
  • Histone Deacetylase Inhibitors / chemistry
  • Histone Deacetylase Inhibitors / isolation & purification*
  • Histone Deacetylase Inhibitors / pharmacology*
  • Molecular Structure
  • Multigene Family
  • Nuclear Magnetic Resonance, Biomolecular
  • Peptides, Cyclic / chemistry
  • Transcription Factors / genetics

Substances

  • Depsipeptides
  • Histone Deacetylase Inhibitors
  • Peptides, Cyclic
  • Transcription Factors
  • burkholdac A
  • burkholdac B
  • spiruchostatin B
  • spiruchostatin A