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ファイル | 記述 | サイズ | フォーマット | |
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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 ![]() ![]() ![]() |
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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