组蛋白去乙酰化酶 2：癌症和神经退行性疾病的潜在治疗靶点。
Histone deacetylase 2: A potential therapeutic target for cancer and neurodegenerative disorders.
机构信息
Department of Pharmaceutical Chemistry, Institute of Pharmacy, Nirma University, Ahmedabad, 382481, Gujarat, India.
Department of Pharmaceutical Chemistry, Institute of Pharmacy, Nirma University, Ahmedabad, 382481, Gujarat, India; Department of Pharmaceutical Chemistry, L. M. College of Pharmacy, Navrangpura, Ahmedabad, 380009, Gujarat, India.
出版信息
Eur J Med Chem. 2021 Apr 15;216:113332. doi: 10.1016/j.ejmech.2021.113332. Epub 2021 Mar 1.
Histone deacetylases (HDACs) have been implicated in a number of diseases including cancer, cardiovascular disorders, diabetes mellitus, neurodegenerative disorders and inflammation. For the treatment of epigenetically altered diseases such as cancer, HDAC inhibitors have made a significant progress in terms of development of isoform selective inhibitiors. Isoform specific HDAC inhibitors have less adverse events and better safety profile. A HDAC isoform i.e., HDAC2 demonstrated significant role in the development of variety of diseases, mainly involved in the cancer and neurodegenerative disorders. Discovery and development of selective HDAC2 inhibitors have a great potential for the treatment of target diseases. In the present compilation, we have reviewed the role of HDAC2 in progression of cancer and neurodegenerative disorders, and information on the drug development opportunities for selective HDAC2 inhibition.
组蛋白去乙酰化酶（HDACs）与多种疾病相关，包括癌症、心血管疾病、糖尿病、神经退行性疾病和炎症。对于治疗表观遗传学改变的疾病，如癌症，HDAC 抑制剂在开发同工型选择性抑制剂方面取得了显著进展。同工型特异性 HDAC 抑制剂的不良反应较少，安全性更好。HDAC2 同工型在多种疾病的发展中发挥了重要作用，主要涉及癌症和神经退行性疾病。发现和开发选择性 HDAC2 抑制剂对于治疗目标疾病具有巨大潜力。在本综述中，我们回顾了 HDAC2 在癌症和神经退行性疾病进展中的作用，以及选择性 HDAC2 抑制的药物开发机会的信息。
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