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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  KAKEN_id  orcid 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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