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- W3023532860 endingPage "615" @default.
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- W3023532860 abstract "This chapter discusses the clinical applications of histone deacetylase inhibitors. Histone acetyl-transferases (HATs) and histone deacetylases (HDAC) play a crucial role in gene regulation. HATs catalyze the transfer of acetyl groups to lysine residues of histones, resulting in the relaxation of chromosomal DNA. In general, this promotes transcription at the affected chromosomal regions. On the other hand, HDACs function to reverse histone acetylation, causing chromosomal DNA to condense. HDAC inhibitors have shown great promise as a treatment option for a variety of cancer and non-cancer diseases. Despite the presumed global affect, pharmacological inhibition of HDACs alters the expression of only 2% of genes. Preclinical work has demonstrated that HDAC inhibitors appear to have a stronger effect on transformed cells than normal cells. Depending on the specific HDAC inhibitor, its concentration, and the cell type being treated, these drugs have demonstrated the ability to induce cell cycle arrest, increase the expression of pro-apoptotic genes, down-regulate anti-apoptotic genes, inhibit the expression of genes involved in angiogenesis, alter the expression of DNA repair genes, and down-regulate invasion and metastasis associated genes. One of the limitations of current HDAC inhibitors is their relatively narrow therapeutic window. Many HDAC inhibitor effects on biological targets are reversible upon drug removal, and sustained effects often require continuous dosing. More specific patient selection will also have a significant impact on future clinical trials of HDAC inhibitors, especially as related to cancer treatment." @default.
- W3023532860 created "2020-05-13" @default.
- W3023532860 creator A5049096078 @default.
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- W3023532860 creator A5091342791 @default.
- W3023532860 date "2011-01-01" @default.
- W3023532860 modified "2023-10-16" @default.
- W3023532860 title "Clinical Applications of Histone Deacetylase Inhibitors" @default.
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