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首页> 外文期刊>Biochemical Pharmacology >4-Hydroxybenzoic acid derivatives as HDAC6-specific inhibitors modulating microtubular structure and HSP90 alpha chaperone activity against prostate cancer
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4-Hydroxybenzoic acid derivatives as HDAC6-specific inhibitors modulating microtubular structure and HSP90 alpha chaperone activity against prostate cancer

机译：4-羟基苯甲酸衍生物作为 HDAC6 特异性抑制剂调节微管结构和 HSP90 α 伴侣活性对抗前列腺癌

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摘要

Histone deacetylase (HDAC)6 is a unique isoenzyme targeting specific substrates including a-tubulin and heat shock protein (HSP)90. HDAC6 is involved in protein trafficking and degradation, cell shape and migration. Deregulation of HDAC6 activity is associated with a variety of diseases including cancer leading to a growing interest for developing HDAC6 inhibitors. Here, we identified two new structurally related 4-hydroxybenzoic acids as selective HDAC6 inhibitors reducing proliferation, colony and spheroid formation as well as viability of prostate cancer cells. Both compounds strongly enhanced alpha-tubulin acetylation leading to remodeling of microtubular organization. Furthermore, 4-hydroxybenzoic acids decreased HSP90 alpha regulation of the human androgen receptor in prostate cancer cells by increasing HSP90 alpha acetylation levels. Collectively, our data support the potential of 4-hydroxybenzoic acid derivatives as HDAC6-specific inhibitors with anti-cancer properties. (C) 2015 Elsevier Inc. All rights reserved.
机译：组蛋白脱乙酰酶 （HDAC）6 是一种独特的同工酶，靶向特定底物，包括 α-微管蛋白和热休克蛋白 （HSP）90。HDAC6 参与蛋白质运输和降解、细胞形状和迁移。HDAC6活性的失调与包括癌症在内的多种疾病有关，导致人们对开发HDAC6抑制剂的兴趣日益浓厚。在这里，我们鉴定了两种新的结构相关的 4-羟基苯甲酸作为选择性 HDAC6 抑制剂，可减少前列腺癌细胞的增殖、集落和球状体形成以及活力。这两种化合物都强烈增强了α-微管蛋白乙酰化，导致微管组织的重塑。此外，4-羟基苯甲酸通过增加 HSP90 α 乙酰化水平来降低前列腺癌细胞中人雄激素受体的 HSP90 α 调节。总的来说，我们的数据支持4-羟基苯甲酸衍生物作为具有抗癌特性的HDAC6特异性抑制剂的潜力。（C） 2015 爱思唯尔公司保留所有权利。

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