4.1 Article

Discovery and activity profiling of thailandepsins A through F, potent histone deacetylase inhibitors, from Burkholderia thailandensis E264

Journal

MEDCHEMCOMM
Volume 3, Issue 8, Pages 976-981

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c2md20024d

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Funding

  1. University of Wisconsin-Milwaukee
  2. NIH/NCI [R01 CA152212]

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Three new bicyclic depsipeptides, which are related to the previously reported thailandepsins A (1), B (2) and C (3), were discovered from the culture broth of Burkholderia thailandensis E264 when supplemented with amino acid precursors, and were subsequently named as thailandepsins D (4), E (5) and F (6), respectively. Enzyme assays showed that 1-6 are potent histone deacetylase (HDAC) inhibitors, particularly toward HDAC1 which represents class I human HDACs.

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