Transcriptional activation of p21WAF1/C1P1 by apicidin, a novel histone deacetylase inhibitor
Transcriptional activation of p21WAF1/C1P1 by apicidin, a novel histone deacetylase inhibitor
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DOI：
10.1006/bbrc.2001.4434
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发表时间：
2001-03-09
影响因子：
3.1
通讯作者：
Trepel, JB
中科院分区：
文献类型：
--
作者：
Kim, JS;Lee, SM;Trepel, JB
Apicidin [cyclo（N-O-methyl-L-propanyl-L-isoleucinyl-D-pipecolinyl-L-2-amino-8-oxodecanoyl）]是一种新型的组蛋白去乙酰化酶抑制剂，具有抗原虫和抗增殖作用。在这项研究中，我们发现apicidin诱导人前列腺癌细胞中p21（WAF 1/CIP 1）（p21）的转录激活。Apicidin诱导p21蛋白和mRNA的表达以及p21启动子-荧光素酶报告构建体的活化，Apicidin引起乙酰化组蛋白H3和H4在总细胞染色质中的积累。染色质免疫沉淀显示p21启动子DNA与apicidin处理后的高乙酰化组蛋白H3和H4相关。因此，这里的数据表明apicidin激活与组蛋白H3和H4的乙酰化相关的p21转录。(C)北京：科学出版社.
Apicidin [cyclo(N-O-methyl-L-tryptophanyl-L-isoleucinyl-D-pipecolinyl-L-2-amino-8-oxodecanoyl)], a novel histone deacetylase inhibitor, has been identified as an antiprotozoal and antiproliferative agent. In this study, we show apicidin induces transcriptional activation of p21(WAF1/CIP1) (p21) in human prostate carcinoma cells. Apicidin induces expression of p21 protein and mRNA and activation of p21 promoter-luciferase reporter constructs, Apicidin causes an accumulation of acetylated histones H3 and H4 in total cellular chromatin. Chromatin immunoprecipitation shows p21 promoter DNA is associated with hyperacetylated histones H3 and H4 after treatment with apicidin. Therefore, the data here demonstrate that apicidin activates p21 transcription associated with the acetylation of histones H3 and H4. (C) 2001 Academic Press.