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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Review Article

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

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

Volume 19, Issue 12, 2019

Page: [1041 - 1050] Pages: 10

DOI: 10.2174/1568026619666190603092407

Price: $65

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.

Graphical Abstract
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