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组蛋白去乙酰化酶:纤维化疾病的潜在治疗靶点。

Histone deacetylase: a potential therapeutic target for fibrotic disorders.

机构信息

Department of Medicine, Rhode Island Hospital, Warren Alpert Medical School of Brown University, Middle House 301, 593 Eddy Street, Providence, RI 02903, USA.

出版信息

J Pharmacol Exp Ther. 2010 Nov;335(2):266-72. doi: 10.1124/jpet.110.168385. Epub 2010 Aug 18.

Abstract

Histone deacetylases (HDACs) are enzymes that balance the acetylation activities of histone acetyltransferases on chromatin remodeling and play essential roles in regulating gene transcription. In the past several years, the role of HDACs in cancer initiation and progression, as well as the therapeutic effects of HDAC inhibitors in various types of cancer, has been well studied. Recent studies indicated that HDAC activity is also associated with the development and progression of some chronic diseases characterized by fibrosis, including chronic kidney disease, cardiac hypertrophy, and idiopathic pulmonary fibrosis. Here, we review what is known about HDACs in the progression of tissue fibrosis and the potential applications of HDAC inhibitors in the treatment of disorders associated with fibroblast activation and proliferation.

摘要

组蛋白去乙酰化酶(HDACs)是一种在染色质重塑过程中平衡组蛋白乙酰转移酶乙酰化活性的酶,在调节基因转录中发挥着重要作用。在过去的几年中,HDACs 在癌症的发生和发展中的作用,以及 HDAC 抑制剂在各种类型癌症中的治疗效果,已经得到了很好的研究。最近的研究表明,HDAC 活性也与一些以纤维化为特征的慢性疾病的发展和进展有关,包括慢性肾脏病、心脏肥大和特发性肺纤维化。在这里,我们综述了 HDACs 在组织纤维化进展中的作用,以及 HDAC 抑制剂在治疗与成纤维细胞激活和增殖相关的疾病中的潜在应用。

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