2018
DOI: 10.2174/1389203718666170106101133
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Natural Product Inhibitors of Histone Deacetylases as New Anticancer Agents

Abstract: Acetylation and deactylation of histones are important determinants of gene expression. Histone deacetylases (HDACs) remove acetyl groups from histones leading to suppression and regulation of epigenetic gene expression. Current studies have demonstrated that HDAC-inhibitors (HDACIs) inducing histone hyperacetylation are promising novel agents in cancer treatment. HDACIs have been shown to have significant anticancer effects with negligible toxicity in the preclinical studies. Ongoing clinial trials are being … Show more

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Cited by 12 publications
(11 citation statements)
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“…Isolated from the fungus Streptomyces hygroscopicus in 1976 by Tsuji et al., is a classic linear hydroxamic acid derivative and one of the first natural product determined to have HDAC inhibitory activity . Because it is one of the most potent known HDAC inhibitors, with nanomolar inhibition of recombinant HDAC 1 and 6, trichostatin A (TSA) is routinely used as a positive control and as a reference to compare other HDACi ,. TSA has been reported to inhibit cell growth in, among others, lung adenocarcinoma, hepatoma, cervix carcinoma, and small cell lung cancer, through regulation P21 waf/cip1 , P27 , Bcl‐Xl , cyclin A and E, etc ,.…”
Section: Histone Deacetylase‐modulating Natural Productsmentioning
confidence: 99%
“…Isolated from the fungus Streptomyces hygroscopicus in 1976 by Tsuji et al., is a classic linear hydroxamic acid derivative and one of the first natural product determined to have HDAC inhibitory activity . Because it is one of the most potent known HDAC inhibitors, with nanomolar inhibition of recombinant HDAC 1 and 6, trichostatin A (TSA) is routinely used as a positive control and as a reference to compare other HDACi ,. TSA has been reported to inhibit cell growth in, among others, lung adenocarcinoma, hepatoma, cervix carcinoma, and small cell lung cancer, through regulation P21 waf/cip1 , P27 , Bcl‐Xl , cyclin A and E, etc ,.…”
Section: Histone Deacetylase‐modulating Natural Productsmentioning
confidence: 99%
“…Given the extensive research on the special structure, substrate, and biological function of HDAC6, it could be considered as an important potential therapeutic target for numerous diseases, including cancer ( Lee et al, 2008 ), neurodegenerative disease ( Krukowski et al, 2017 ), and inflammatory diseases ( Yan et al, 2018 ). Furthermore, HDAC6 inhibitors have been widely investigated, with some being found to act effectively with antitumor agents or other drugs ( Li et al, 2017 ; Hanikoglu et al, 2018 ). For example, colorectal and breast cancer cells are inhibited through treatment with a combination of thiol-based inhibitors and paclitaxel ( Itoh et al, 2007 ).…”
Section: Introductionmentioning
confidence: 99%
“…Valproate has the advantage that it is already approved for some clinical applications. In addition to some carboxylic acids there are a variety of structures that are histone deacetylase inhibitors and these include some naturally occurring molecules [7,8]. One objective of the present work was to compare the action of different structural classes of histone deacetylase inhibitors as inducers of enzyme activity in bladder and colon cancer cells.…”
Section: Introductionmentioning
confidence: 99%