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Next-generation of selective histone deacetylase inhibitors.

ABSTRACT: 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.

SUBMITTER: Yang F

PROVIDER: S-EPMC9065321 | biostudies-literature | 2019 Jun

REPOSITORIES: biostudies-literature

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Next-generation of selective histone deacetylase inhibitors.

Yang Feifei F Zhao Na N Ge Di D Chen Yihua Y

RSC advances 20190624 34

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 ...[more]

PMID: 35519364

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