2009年12月
Synthesis and properties of PI polyamide-SAHA conjugate
TETRAHEDRON LETTERS
- ,
- ,
- ,
- ,
- ,
- ,
- ,
- ,
- 巻
- 50
- 号
- 52
- 開始ページ
- 7288
- 終了ページ
- 7292
- 記述言語
- 英語
- 掲載種別
- 研究論文(学術雑誌)
- DOI
- 10.1016/j.tetlet.2009.10.034
- 出版者・発行元
- PERGAMON-ELSEVIER SCIENCE LTD
We have designed and synthesized new types of pyrrole (P)-imidazole (1) 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. (C) 2009 Elsevier Ltd. All rights reserved.
- リンク情報
-
- DOI
- https://doi.org/10.1016/j.tetlet.2009.10.034
- J-GLOBAL
- https://jglobal.jst.go.jp/detail?JGLOBAL_ID=200902297756504821
- CiNii Articles
- http://ci.nii.ac.jp/naid/120001741230
- Web of Science
- https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=JSTA_CEL&SrcApp=J_Gate_JST&DestLinkType=FullRecord&KeyUT=WOS:000272221000016&DestApp=WOS_CPL
- ID情報
-
- DOI : 10.1016/j.tetlet.2009.10.034
- ISSN : 0040-4039
- J-Global ID : 200902297756504821
- CiNii Articles ID : 120001741230
- Web of Science ID : WOS:000272221000016