Department of Medicine, Division of Cardiology, University of Colorado Denver, Aurora, Colorado 80045-0508, USA.
Annu Rev Pharmacol Toxicol. 2012;52:303-19. doi: 10.1146/annurev-pharmtox-010611-134712. Epub 2011 Sep 26.
Reversible protein acetylation provides a central mechanism for controlling gene expression and cellular signaling events. Two pharmacological inhibitors of protein deacetylation are currently approved for the treatment of human cancer, and numerous follow-on compounds are in clinical development for oncology and non-oncology indications. The inhibitors target members of a family of enzymes known as histone deacetylases (HDACs). Surprisingly, HDAC inhibitors have also been shown to be efficacious in preclinical models of heart failure. This review highlights roles of HDACs in the heart and the therapeutic potential of HDAC inhibitors for the treatment of heart failure.
可逆蛋白质乙酰化提供了控制基因表达和细胞信号事件的核心机制。目前有两种蛋白质去乙酰化酶的药理学抑制剂被批准用于治疗人类癌症,还有许多后续化合物正在开发中,用于肿瘤学和非肿瘤学适应症。这些抑制剂针对一组被称为组蛋白去乙酰化酶 (HDACs) 的酶的成员。令人惊讶的是,HDAC 抑制剂在心力衰竭的临床前模型中也显示出疗效。这篇综述强调了 HDAC 在心脏中的作用以及 HDAC 抑制剂治疗心力衰竭的治疗潜力。