Apicidin is a histone deacetylase inhibitor with anti-invasive and anti-angiogenic potentials
Apicidin is a histone deacetylase inhibitor with anti-invasive and anti-angiogenic potentials
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DOI：
10.1016/j.bbrc.2004.01.149
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发表时间：
2004-03-19
影响因子：
3.1
通讯作者：
Hong, S
中科院分区：
文献类型：
--
作者：
Kim, SH;Ahn, S;Hong, S
Apicidin已被鉴定为组蛋白脱乙酰酶（HDAC）抑制剂。由于HDAC抑制剂正在成为一个令人兴奋的潜在的抗癌药物的新类别，在本研究中，我们已经检查了apicidin对癌症侵袭和血管生成的抑制作用。Apicidin诱导v-ras转化的小鼠成纤维细胞NIH 3 T3细胞中组蛋白H4的二乙酰化和三乙酰化形式以及形态学改变。Apicidin能显著抑制v-ras-NIH 3 T3和人黑色素瘤A2058细胞的侵袭，其机制可能与其调节基质金属蛋白酶活性有关。有趣的是，apicidin强烈抑制绒毛尿囊膜上新血管的形成和ECV 304人血管内皮细胞的管形成。这是首次报道apicidin具有抗血管生成的潜力，它可能被开发为一种新型的抗癌药物。(C)2004爱思唯尔公司All rights reserved.
Apicidin has been identified as a histone deacetylase (HDAC) inhibitor. Since HDAC inhibitors are emerging as an exciting new class of potential anti-cancer agents, in the present study, we have examined the inhibitory effect of apicidin on cancer invasion and angiogenesis. Apicidin induced di- and tri-acetylated forms of histone H4 and the morphological alteration in v-ras-transformed mouse fibroblast NIH3T3 cells. Apicidin dramatically inhibited the invasion of v-ras-NIH3T3 and human melanoma A2058 cells and it could be associated with its ability to regulate the activities of matrix metalloproteinases. Interestingly, apicidin strongly inhibited the formation of new vessels on chorioallantoic membrane and the tube formation of ECV304 human vascular endothelial cells. This is the first report to show the anti-angiogenic potential of apicidin and it could be developed as a new type of anti-cancer drug. (C) 2004 Elsevier Inc. All rights reserved.