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09168451.2014.1002452.pdf | 1.93 MB | Adobe PDF | 見る/開く |
タイトル: | Synthesis and biological activities of the amide derivative of aplog-1, a simplified analog of aplysiatoxin with anti-proliferative and cytotoxic activities. |
著者: | Hanaki, Yusuke Yanagita, Ryo C Sugahara, Takahiro Aida, Misako Tokuda, Harukuni Suzuki, Nobutaka Irie, Kazuhiro https://orcid.org/0000-0001-7109-8568 (unconfirmed) |
著者名の別形: | 入江, 一浩 |
キーワード: | aplysiatoxin anti-proliferative protein kinase C tumor promoter |
発行日: | 2015 |
出版者: | Taylor & Francis Group |
誌名: | Bioscience, biotechnology, and biochemistry |
巻: | 79 |
号: | 6 |
開始ページ: | 888 |
終了ページ: | 895 |
抄録: | Aplog-1 is a simplified analog of the tumor-promoting aplysiatoxin with anti-proliferative and cytotoxic activities against several cancer cell lines. Our recent findings have suggested that protein kinase Cδ (PKCδ) could be one of the target proteins of aplog-1. In this study, we synthesized amide-aplog-1 (3), in which the C-1 ester group was replaced with an amide group, to improve chemical stability in vivo. Unfortunately, 3 exhibited seventy-fold weaker binding affinity to the C1B domain of PKCδ than that of aplog-1, and negligible anti-proliferative and cytotoxic activities even at 10(-4) M. A conformational analysis and density functional theory calculations indicated that the stable conformation of 3 differed from that of aplog-1. Since 27-methyl and 27-methoxy derivatives (1, 2) without the ability to bind to PKC isozymes exhibited marked anti-proliferative and cytotoxic activities at 10(-4) M, 3 may be an inactive control to identify the target proteins of aplogs. |
記述: | Published online: 23 Jan 2015 |
著作権等: | This is an Accepted Manuscript of an article published by Taylor & Francis in 'Bioscience, biotechnology, and biochemistry' available online: http://www.tandfonline.com/10.1080/09168451.2014.1002452. The full-text file will be made open to the public on 23 Jan 2016 in accordance with publisher's 'Terms and Conditions for Self-Archiving'. 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/2433/202083 |
DOI(出版社版): | 10.1080/09168451.2014.1002452 |
PubMed ID: | 25612633 |
出現コレクション: | 学術雑誌掲載論文等 |
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