Design and synthesis of non-hydroxamate histone deacetylase inhibitors: identification of a selective histone acetylating agent
Design and synthesis of non-hydroxamate histone deacetylase inhibitors: identification of a selective histone acetylating agent
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DOI：
10.1016/j.bmc.2005.04.002
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发表时间：
2005-07-01
影响因子：
3.5
通讯作者：
Miyata, N
中科院分区：
文献类型：
--
作者：
Suzuki, T;Matsuura, A;Miyata, N
设计、合成了一系列辛二酰苯胺异羟肟酸（SAHA）类非异羟肟酸酯，并对其抑制组蛋白去乙酰化酶（HDAC）活性进行了评价。其中，甲基亚砜15在酶测定中抑制HDAC，并引起组蛋白H4的过度乙酰化，同时不诱导HCT 116细胞中乙酰化α-微管蛋白的积累。(c)2005爱思唯尔有限公司保留所有权利。
A series of suberoylanilide hydroxamic acid (SAHA)-based non-hydroxamates was designed, synthesized, and evaluated for their histone deacetylase (HDAC) inhibitory activity. Among these, methyl sulfoxide 15 inhibited HDACs in enzyme assays and caused hyperacetylation of histone H4 while not inducing the accumulation of acetylated alpha-tubulin in HCT116 cells. (c) 2005 Elsevier Ltd. All rights reserved.