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タイトル: | Synthesis and Biological Evaluation of the 12,12-Dimethyl Derivative of Aplog-1, an Anti-Proliferative Analog of Tumor-Promoting Aplysiatoxin |
著者: | NAKAGAWA, Yu KIKUMORI, Masayuki YANAGITA, Ryo C. MURAKAMI, Akira TOKUDA, Harukuni NAGAI, Hiroshi 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: | Aplog-1 aplysiatoxin bryostatin protein kinase C tumor promoter |
発行日: | Jun-2011 |
出版者: | Japan Society for Bioscience, Biotechnology, and Agrochemistry |
誌名: | Bioscience, Biotechnology, and Biochemistry |
巻: | 75 |
号: | 6 |
開始ページ: | 1167 |
終了ページ: | 1173 |
抄録: | Aplog-1 is a unique analog of tumor-promoting aplysiatoxin that inhibits tumor-promotion by phorbol diesters and proliferation of tumor cells. While the structural features relevant to the biological activities of Aplog-1 remain to be identified, recent studies by us have suggested that local hydrophobicity around the spiroketal moiety of Aplog-1 is a crucial determinant of its anti-proliferative activity. This hypothesis led us to design 12, 12-dimethyl-Aplog-1 (3), in which a hydrophobic geminal dimethyl group is installed proximal to the spiroketal moiety to improve biological potency. As expected, 3 was more effective than Aplog-1 in inhibiting cancer cell growth and binding to protein kinase Cδ, a putative receptor responsible for the biological response of Aplog-1. Moreover, an induction test on Epstein-Barr virus early antigen demonstrated 3 to be a better anti-tumor promoter than Aplog-1. These results indicate that 3 is a superior derivative of Aplog-1, and thus a more promising lead for anti-cancer drugs. |
著作権等: | © 2011 by Japan Society for Bioscience, Biotechnology, and Agrochemistry |
URI: | http://hdl.handle.net/2433/156509 |
DOI(出版社版): | 10.1271/bbb.110130 |
PubMed ID: | 21670518 |
関連リンク: | https://www.jstage.jst.go.jp/article/bbb/75/6/75_110130/_article |
出現コレクション: | 学術雑誌掲載論文等 |
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