Acyldepsipeptide HDAC Inhibitor Production Induced in Burkholderia thailandensis

被引:88
作者
Biggins, John B. [1 ]
Gleber, Conrad D. [1 ]
Brady, Sean F. [1 ]
机构
[1] Rockefeller Univ, Lab Genetically Encoded Small Mol, Howard Hughes Med Inst, New York, NY 10065 USA
关键词
HISTONE DEACETYLASE INHIBITOR; BIOLOGICAL-ACTIVITY; SPIRUCHOSTATIN-A; DEPSIPEPTIDE; FK228; DISCOVERY; BIOSYNTHESIS; METABOLITES; FR901228; GENES;
D O I
10.1021/ol200225v
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
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.
引用
收藏
页码:1536 / 1539
页数:4
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