| 論文名 |
A cyclodextrin-capped histone deacetylase inhibitor. |
| 著者 |
Jahangir Amin
Antonino Puglisi
James Clarke
John Milton
Minghua Wang
Ronald M Paranal
James E Bradner
John Spencer
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| キーワード |
|
| 出版年月 |
1970年1月 |
| 発表先 |
Bioorg Med Chem Lett. 2013 Jun 1;23(11):3346-8. |
| WEBサイト |
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| 論文概要（和文） |
シクロデキストリンでキャップされたヒストンデアセチラーゼ阻害剤。 |
| 論文概要（英文） |
We have synthesized a β-cyclodextrin (βCD)-capped histone deacetylase (HDAC) inhibitor 3 containing an alkyl linker and a zinc-binding hydroxamic acid motif. Biological evaluation (HDAC inhibition studies) of 3 enabled us to establish the effect of replacing an aryl cap (in SAHA (vorinostat,)) 1 by a large saccharidic scaffold "cap". HDAC inhibition was observed for 3, to a lesser extent than SAHA, and rationalized by molecular docking into the active site of HDAC8. However, compound 3 displayed no cellular activity. |
