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| j.tetlet.2009.10.034.pdf | 315.92 kB | Adobe PDF | 見る/開く |
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| DCフィールド | 値 | 言語 |
|---|---|---|
| dc.contributor.author | Ohtsuki, Akimichi | en |
| dc.contributor.author | Kimura, Makoto T. | en |
| dc.contributor.author | Minoshima, Masafumi | en |
| dc.contributor.author | Suzuki, Tsukasa | en |
| dc.contributor.author | Ikeda, Maki | en |
| dc.contributor.author | Bando, Toshikazu | en |
| dc.contributor.author | Nagase, Hiroki | en |
| dc.contributor.author | Shinohara Ken-ichi | en |
| dc.contributor.author | Sugiyama, Hiroshi | en |
| dc.contributor.alternative | 杉山, 弘 | ja |
| dc.date.accessioned | 2009-12-14T07:18:03Z | - |
| dc.date.available | 2009-12-14T07:18:03Z | - |
| dc.date.issued | 2009-12-30 | - |
| dc.identifier.issn | 00404039 | - |
| dc.identifier.uri | http://hdl.handle.net/2433/88220 | - |
| dc.description.abstract | 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. | en |
| dc.language.iso | eng | - |
| dc.publisher | Elsevier | en |
| dc.rights | c 2009 Elsevier Ltd. All rights reserved. | en |
| dc.rights | 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。 | ja |
| dc.rights | This is not the published version. Please cite only the published version. | en |
| dc.title | Synthesis and properties of PI polyamide-SAHA conjugate | en |
| dc.type | journal article | - |
| dc.type.niitype | Journal Article | - |
| dc.identifier.jtitle | Tetrahedron Letters | en |
| dc.identifier.volume | 50 | - |
| dc.identifier.issue | 52 | - |
| dc.identifier.spage | 7288 | - |
| dc.identifier.epage | 7292 | - |
| dc.relation.doi | 10.1016/j.tetlet.2009.10.034 | - |
| dc.textversion | author | - |
| dcterms.accessRights | open access | - |
| 出現コレクション: | 学術雑誌掲載論文等 | |
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