Recent Study of Dual HDAC/PARP Inhibitor for the Treatment of Tumor

Author(s): Haiying Lu, Lan Bai, Yanping Zhou, Yongping Lu, Zhongliang Jiang*, Jianyou Shi*

Journal Name: Current Topics in Medicinal Chemistry

Volume 19 , Issue 12 , 2019

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Graphical Abstract:


The occurrence and development of tumors are closely related to epigenetic instability which modulates gene expression through DNA methylation, histone modification, chromatin remodeling, and RNA-related silencing. Histone deacetylase (HDAC) and poly (ADP-ribose) polymerase (PARP) are targets of epigenetic regulation. Over the years, a large number of studies have shown that HDAC inhibitors and PARP inhibitors have synergistic effects in the treatment of tumors, and there are reports of related dual HDAC/PARP inhibitors. This review will give a brief summary of the synergistic mechanisms of HDAC inhibitors and PARP inhibitors and introduce the design of the first dual HDAC/PARP inhibitor, which may guide the design of more dual HDAC/PARP inhibitors for the treatment of tumors.

Keywords: Epigenetics, Tumor, HDAC, PARP, Dual inhibitors, Synergy.

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Year: 2019
Published on: 29 July, 2019
Page: [1041 - 1050]
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DOI: 10.2174/1568026619666190603092407
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