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CC BY 4.0 · Pharmaceutical Fronts 2020; 02(02): e88-e93
DOI: 10.1055/s-0040-1713873
Review Article
Georg Thieme Verlag KG Stuttgart · New York

Dual Inhibitors Targeting DNA and Histone Deacetylases

Chen Chen
1   Department of Pharmaceutical Synthesis and Analysis, Shandong Analysis and Test Center, Qilu University of Technology (Shandong Academy of Sciences), Jinan, People's Republic of China
,
Xinying Yang
2   Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, Ministry of Education, School of Pharmaceutical Sciences, Shandong University, Jinan, People's Republic of China
,
Xuben Hou
2   Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, Ministry of Education, School of Pharmaceutical Sciences, Shandong University, Jinan, People's Republic of China
,
Hao Fang
2   Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, Ministry of Education, School of Pharmaceutical Sciences, Shandong University, Jinan, People's Republic of China
› Author Affiliations Funding This work was supported by National Natural Science Foundation of China (81874288 and 21672127), China-Australia Centre for Health Sciences Research (CACHSR No. 2019GJ07), Shandong Provincial Natural Science Foundation (No. ZR2019LZL004), the Key Research and Development Project of Shandong Province (Grant No. 2017CXGC1401), the Fundamental Research Funds of Shandong University (Grant No. 2019GN045), and the Joint Research Funds for Shandong University and Karolinska Institute (SDU-KI-2019-06).
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Publication History

Publication Date:
07 July 2020 (online)

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Abstract

Histone deacetylases (HDACs) regulate the acetylation status of histones and structural status of chromatin. The chromatin structure becomes relaxed after inhibition of HDAC, leading to DNA exposed to DNA disrupting agents, and eventually causing DNA dysfunction. Recently, more and more dual inhibitors targeting DNA and HDACs have been reported to be applied to cancer treatment. In this review, we describe the current status of dual inhibitors targeting DNA and HDACs, summarize their pharmacological characters, and predict their further trend in the field.

Keywords

DNA - HDAC - dual-targeting - antitumor agent
 

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