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| ファイル | 記述 | サイズ | フォーマット | |
|---|---|---|---|---|
| j.tetlet.2009.10.034.pdf | 315.92 kB | Adobe PDF | 見る/開く |
| タイトル: | Synthesis and properties of PI polyamide-SAHA conjugate |
| 著者: | Ohtsuki, Akimichi Kimura, Makoto T. Minoshima, Masafumi Suzuki, Tsukasa Ikeda, Maki Bando, Toshikazu   Nagase, Hiroki Shinohara Ken-ichi Sugiyama, Hiroshi  https://orcid.org/0000-0001-8923-5946 (unconfirmed) |
| 著者名の別形: | 杉山, 弘 |
| 発行日: | 30-Dec-2009 |
| 出版者: | Elsevier |
| 誌名: | Tetrahedron Letters |
| 巻: | 50 |
| 号: | 52 |
| 開始ページ: | 7288 |
| 終了ページ: | 7292 |
| 抄録: | We have designed and synthesized new types of pyrrole (P)-imidazole (I) polyamide conjugates 1 and 2 possessing a suberoylanilide hydroxamic acid (SAHA) moiety that is a strong inhibitor of histone deacetylase (HDAC). SAHA conjugate 2 was designed to target the promoter region of the p16 tumor suppressor gene. The DNA binding affinity of SAHA conjugate 2 to its target sequence was examined using surface plasmon resonance. HDAC inhibition activity of conjugates 1 and 2 was evaluated using a colorimetric assay. The results demonstrated that even though it possesses the relatively large SAHA moiety, conjugate 2 has high DNA sequence-specific binding properties and moderate HDAC inhibitory activity in vitro. SAHA conjugate 2 was found to cause morphological changes in HeLa cells and to induce selective Histone H3 lysine 9 acetylation. |
| 著作権等: | c 2009 Elsevier Ltd. All rights reserved. この論文は出版社版でありません。引用の際には出版社版をご確認ご利用ください。 This is not the published version. Please cite only the published version. |
| URI: | http://hdl.handle.net/2433/88220 |
| DOI(出版社版): | 10.1016/j.tetlet.2009.10.034 |
| 出現コレクション: | 学術雑誌掲載論文等 |
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