Discovery and activity profiling of thailandepsins A through F, potent histone deacetylase inhibitors, from Burkholderia thailandensis E264.
Discovery and activity profiling of thailandepsins A through F, potent histone deacetylase inhibitors, from Burkholderia thailandensis E264.
复制标题
DOI：
10.1039/c2md20024d
复制
发表时间：
2012-08-01
期刊：
影响因子：
--
通讯作者：
Cheng YQ
中科院分区：
文献类型：
--
作者：
Wang C;Flemming CJ;Cheng YQ
从Burkholderia thailandensis E264的培养液中添加氨基酸前体后，发现了3个新的双环缩酚肽，分别命名为thailandepsin D（4）、E（5）和F（6），它们与已报道的thailandepsin A（1）、B（2）和C（3）有关。酶测定显示1-6是有效的组蛋白脱乙酰酶（HDAC）抑制剂，特别是针对代表I类人HDAC的HDAC 1。
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.