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Preclinical studies on histone deacetylase inhibitors as therapeutic reagents for endometrial and ovarian cancers.

ABSTRACT: Histone deacetylases (HDACs) remove acetyl groups from lysine residues of histones and the deacetylation allows for tighter electrostatic interactions between DNA and histones, leading to a more compact chromatin conformation with limited access for transactivators and the suppression of transcription. HDAC mRNA and protein overexpression was observed in endometrial and ovarian cancers. Numerous in vitro studies have shown that HDAC inhibitors, through their actions on histone and nonhistone proteins, are able to reactivate the tumor suppressor genes, inhibit cell cycle progression and induce cell apoptosis in endometrial and ovarian cancer cell cultures. Results from mouse xenograft models also demonstrated the potency of HDAC inhibitors as anticancer reagents when used as single agent or in combination with classical chemotherapy drugs.

SUBMITTER: Singh BN

PROVIDER: S-EPMC3273414 | biostudies-literature | 2011 Dec

REPOSITORIES: biostudies-literature

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Preclinical studies on histone deacetylase inhibitors as therapeutic reagents for endometrial and ovarian cancers.

Singh Brahma N BN Zhou Hongyuan H Li Jinping J Tipton Tracy T Wang Bin B Shao Guo G Gilbert E Nickolas EN Li Qiang Q Jiang Shi-Wen SW

Future oncology (London, England) 20111201 12

Histone deacetylases (HDACs) remove acetyl groups from lysine residues of histones and the deacetylation allows for tighter electrostatic interactions between DNA and histones, leading to a more compact chromatin conformation with limited access for transactivators and the suppression of transcription. HDAC mRNA and protein overexpression was observed in endometrial and ovarian cancers. Numerous in vitro studies have shown that HDAC inhibitors, through their actions on histone and nonhistone pro ...[more]

PMID: 22112317

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| S-EPMC3127396 | biostudies-literature

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| S-EPMC5558504 | biostudies-literature

Preclinical evaluation of dual PI3K-mTOR inhibitors and histone deacetylase inhibitors in head and neck squamous cell carcinoma.

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A high-throughput screening identifies histone deacetylase inhibitors as therapeutic agents against medulloblastoma.

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Antidepressant actions of histone deacetylase inhibitors.

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