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

发现并分析 Burkholderia thailandensis E264 中 thailandepsins A 至 F(强效组蛋白去乙酰化酶抑制剂)的活性

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作者:Cheng Wang, Creston J Flemming, Yi-Qiang Cheng

Abstract

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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