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Next-generation of selective histone deacetylase inhibitors

期刊

RSC ADVANCES
卷 9, 期 34, 页码 19571-19583

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ROYAL SOC CHEMISTRY
DOI: 10.1039/c9ra02985k

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资金

  1. National Natural Science Foundation of China [81673304, 81703360]
  2. Open Research Project Foundation of Shanghai Key Laboratory of Regulatory Biology [2018LBR03]
  3. Natural Science Foundation of Shandong Province [ZR2016HB43]
  4. Young Taishan Scholars Program [tsqn20161037]
  5. Shandong Talents Team Cultivation Plan of University Preponderant Discipline [10027]

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Histone deacetylases (HDACs) are clinically validated epigenetic drug targets for cancer treatment. HDACs inhibitors (HDACis) have been successfully applied against a series of cancers. First-generation inhibitors are mainly pan-HDACis that target multiple isoforms which might lead to serious side effects. At present, the next-generation HDACis are mainly focused on being class- or isoform-selective which can provide improved risk-benefit profiles compared to non-selective inhibitors. Because of the rapid development in next-generation HDACis, it is necessary to have an updated and state-of-the-art overview. Here, we summarize the strategies and achievements of the selective HDACis.

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