Jin Gang, Wang Kaiyue, Zhao Yaohui, Yuan Shuo, He Zhangxu, Zhang Jingyu
Pharmacy College, Henan University of Chinese Medicine, 450046 Zhengzhou, China.
Children's Hospital Affiliated to Zhengzhou University, Henan Children's Hospital, Zhengzhou Children's Hospital, Zhengzhou 450018, China.
Bioorg Chem. 2023 Sep;138:106601. doi: 10.1016/j.bioorg.2023.106601. Epub 2023 May 10.
Histone deacetylases (HDACs) are responsible for the deacetylation of lysine residues in histone or non-histone substrates, leading to the regulation of many biological functions, such as gene transcription, translation and remodeling chromatin. Targeting HDACs for drug development is a promising way for human diseases, including cancers and heart diseases. In particular, numerous HDAC inhibitors have revealed potential clinical value for the treatment of cardiac diseases in recent years. In this review, we systematically summarize the therapeutic roles of HDAC inhibitors with different chemotypes on heart diseases. Additionally, we discuss the opportunities and challenges in developing HDAC inhibitors for the treatment of cardiac diseases.
组蛋白去乙酰化酶(HDACs)负责组蛋白或非组蛋白底物中赖氨酸残基的去乙酰化,从而调控许多生物学功能,如基因转录、翻译和染色质重塑。以HDACs为靶点进行药物开发是治疗包括癌症和心脏病在内的人类疾病的一种有前景的方法。特别是,近年来众多HDAC抑制剂已显示出治疗心脏病的潜在临床价值。在本综述中,我们系统地总结了不同化学类型的HDAC抑制剂在心脏病治疗中的作用。此外,我们还讨论了开发用于治疗心脏病的HDAC抑制剂所面临的机遇和挑战。