Advances in histone deacetylase 8 selective inhibitors

NIU Jiaqi; ZHU Yong; ZHAO Shuang; TANG Xiaotian; ZHANG Zhimin; LU Tao

doi:10.11665/j.issn.1000-5048.20160301

Journal of China Pharmaceutical University > 2016 > 47(3): 251-258. > DOI: 10.11665/j.issn.1000-5048.20160301

NIU Jiaqi, ZHU Yong, ZHAO Shuang, TANG Xiaotian, ZHANG Zhimin, LU Tao. Advances in histone deacetylase 8 selective inhibitors[J]. Journal of China Pharmaceutical University, 2016, 47(3): 251-258. DOI: 10.11665/j.issn.1000-5048.20160301

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Advances in histone deacetylase 8 selective inhibitors

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Abstract

Histone deacetylase 8(HDAC8)is a zinc-dependent class I histone deacetylase, closely related to human pathophysiology. HDAC8 involves in various critical signaling networks and is implicated as a therapeutic target in various diseases, including cancer, X-linked intellectual disability and parasitic infections. More and more selective HDAC8 inhibitors have been developed based on deepening study of its well-characterized crystal structure. They are mainly divided into several categories such as phenyl hydroxamic acids, indoles, ortho-aryl-N-hydroxycinnamides, azetidinones etc. . Current challenges remain in the development of potent selective inhibitors that would specifically target HDAC8 with fewer adverse effects compared with pan-HDAC inhibitors. Herein, we reviewed the progress in the study of structure and functions of HDAC8 as well as the development of selective HDAC8 inhibitors.
- histone deacetylase 8,
- structure,
- function,
- selective inhibitor,
- target,
- antitumor activity,
- advance

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