Laboratoire de Biologie Moléculaire et Cellulaire du Cancer, Hôpital Kirchberg, 9, rue Edward Steichen, L-2540 Luxembourg, Luxembourg.
Laboratoire de Biologie Moléculaire et Cellulaire du Cancer, Hôpital Kirchberg, 9, rue Edward Steichen, L-2540 Luxembourg, Luxembourg; Department of Pharmacy, College of Pharmacy, Seoul National University, 599 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea.
Cancer Lett. 2014 Feb 1;343(1):134-46. doi: 10.1016/j.canlet.2013.09.026. Epub 2013 Sep 27.
Histone acetyltransferases (HATs) and histone deacetylases (HDACs) regulate cellular processes by modifying the acetylation status of many proteins. Pathologically altered HDAC activity contributes to cancer development and thus characterization of novel acetylation modulators is important for future anti-cancer therapies. In this study, we identified three novel 4-hydroxybenzoic acid derivatives as pan-HDAC inhibitors that increased protein acetylation levels, arrested cell cycle progression and triggered apoptotic cell death, without affecting viability of normal cells. Our data support the potential of 4-hydroxybenzoic acid derivatives as pan-HDAC inhibitors with anticancer properties.
组蛋白乙酰转移酶（HATs）和组蛋白去乙酰化酶（HDACs）通过修饰许多蛋白质的乙酰化状态来调节细胞过程。病理改变的 HDAC 活性有助于癌症的发展，因此鉴定新型的乙酰化调节剂对于未来的抗癌治疗非常重要。在这项研究中，我们鉴定了三种新型的 4-羟基苯甲酸衍生物作为泛 HDAC 抑制剂，它们可以增加蛋白质乙酰化水平，阻止细胞周期进程并触发细胞凋亡，而不影响正常细胞的活力。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泛 HDAC 抑制剂的潜力。
