期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 27, 期 22, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2019.115087
关键词
Histone deacetylases; Synthesis of HDACi; Anticancer activity; Neurodegenerative diseases; Immune disorders
资金
- Deutsche Forschungsgemeinschaft DFG [270650915/GRK 2158, KA 1942/1-1, KU 1577/2-1]
Epigenetic control plays an important role in gene regulation through chemical modifications of DNA and post-translational modifications of histones. An essential post-translational modification is the histone acetylation/deacetylation-process which is regulated by histone acetyltransferases (HATs) and histone deacetylases (HDACs). The mammalian zinc dependent HDAC family is subdivided into three classes: class I (HDACs 1-3, 8), class II (IIa: HDACs 4, 5, 7, 9; IIb: HDACs 6, 10) and class IV (HDAC 11). In this review, recent studies on the biological role and regulation of class IIa HDACs as well as their contribution in neurodegenerative diseases, immune disorders and cancer will be presented. Furthermore, the development, synthesis, and future perspectives of selective class IIa inhibitors will be highlighted.
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