Department of Internal Medicine (Cardiology), University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
Proc Natl Acad Sci U S A. 2011 Mar 8;108(10):4123-8. doi: 10.1073/pnas.1015081108. Epub 2011 Feb 18.
Histone deacetylases (HDACs) regulate cardiac plasticity; however, their molecular targets are unknown. As autophagy contributes to pathological cardiac remodeling, we hypothesized that HDAC inhibitors target autophagy. The prototypical HDAC inhibitor (HDACi), trichostatin A (TSA), attenuated both load- and agonist-induced hypertrophic growth and abolished the associated activation of autophagy. Phenylephrine (PE)-triggered hypertrophy and autophagy in cultured cardiomyocytes were each blocked by a panel of structurally distinct HDAC inhibitors. RNAi-mediated knockdown of either Atg5 or Beclin 1, two essential autophagy effectors, was similarly capable of suppressing ligand-induced autophagy and myocyte growth. RNAi experiments uncovered the class I isoforms HDAC1 and HDAC2 as required for the autophagic response. To test the functional requirement of autophagic activation, we studied mice that overexpress Beclin 1 in cardiomyocytes. In these animals with a fourfold amplified autophagic response to TAC, TSA abolished TAC-induced increases in autophagy and blunted load-induced hypertrophy. Finally, we subjected animals with preexisting hypertrophy to HDACi, finding that ventricular mass reverted to near-normal levels and ventricular function normalized completely. Together, these data implicate autophagy as an obligatory element in pathological cardiac remodeling and point to HDAC1/2 as required effectors. Also, these data reveal autophagy as a previously unknown target of HDAC inhibitor therapy.
组蛋白去乙酰化酶 (HDACs) 调节心脏的可塑性;然而,它们的分子靶点尚不清楚。由于自噬有助于病理性心脏重构,我们假设 HDAC 抑制剂靶向自噬。典型的 HDAC 抑制剂 (HDACi),曲古抑菌素 A (TSA),减轻了负荷和激动剂诱导的肥大生长,并消除了相关的自噬激活。苯肾上腺素 (PE) 触发的培养心肌细胞肥大和自噬均被一组结构不同的 HDAC 抑制剂阻断。两种必需的自噬效应物 Atg5 或 Beclin 1 的 RNAi 介导的敲低同样能够抑制配体诱导的自噬和心肌细胞生长。RNAi 实验揭示了 Class I 同工酶 HDAC1 和 HDAC2 是自噬反应所必需的。为了测试自噬激活的功能要求,我们研究了在心肌细胞中过表达 Beclin 1 的小鼠。在这些动物中,TAC 引起的自噬反应增加了四倍,TSA 消除了 TAC 诱导的自噬增加,并减弱了负荷诱导的肥大。最后,我们对已经存在肥大的动物进行了 HDACi 处理,发现心室质量恢复到接近正常水平,心室功能完全正常化。这些数据表明自噬是病理性心脏重构的必需因素,并指出 HDAC1/2 是必需的效应物。此外,这些数据揭示了自噬是 HDAC 抑制剂治疗的一个以前未知的靶点。