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Hokkaido University Collection of Scholarly and Academic Papers >
Graduate School of Science / Faculty of Science >
Peer-reviewed Journal Articles, etc >
Effects of E/Z Configuration of Fluoroalkene-containing HDAC Inhibitors on Selectivity for HDAC Isoforms
| Title: | Effects of E/Z Configuration of Fluoroalkene-containing HDAC Inhibitors on Selectivity for HDAC Isoforms |
| Authors: | Chuman, Yoshiro Browse this author | | Ueyama, Mariko Browse this author | | Sano, Satoshi Browse this author | | Wu, Fei Browse this author | | Kiyota, Yuhei Browse this author | | Higashi, Takayoshi Browse this author | | Osada, Satoshi Browse this author | | Sakaguchi, Kazuyasu Browse this author →KAKEN DB |
| Issue Date: | Aug-2013 |
| Publisher: | Chemical Society of Japan |
| Journal Title: | Chemistry Letters |
| Volume: | 42 |
| Issue: | 8 |
| Start Page: | 833 |
| End Page: | 835 |
| Publisher DOI: | 10.1246/cl.130243 |
| Abstract: | Histone deacetylase (HDAC) inhibitors belong to a new class of potential anticancer agents. It may be possible to reduce some of the toxicity by specifically targeting only the HDAC isoform. Here, stereoisomeric HDAC inhibitors containing fluoroalkene were analyzed for their specificity toward HDAC isoforms. Z-Form 1(Z) showed high affinity to HDACs whereas E-isoform 1(E) had lower affinity to HDAC1 and HDAC4. These data suggested that introduction of alkene with E/Z configuration to HDAC inhibitor can be a new strategy to develop the isoform-selective HDAC inhibitors. |
| Type: | article |
| URI: | http://hdl.handle.net/2115/63558 |
| Appears in Collections: | 理学院・理学研究院 (Graduate School of Science / Faculty of Science) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)
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Submitter: 坂口 和靖
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