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dc.contributor.author | NAKAGAWA, Yu | en |
dc.contributor.author | KIKUMORI, Masayuki | en |
dc.contributor.author | YANAGITA, Ryo C. | en |
dc.contributor.author | MURAKAMI, Akira | en |
dc.contributor.author | TOKUDA, Harukuni | en |
dc.contributor.author | NAGAI, Hiroshi | en |
dc.contributor.author | IRIE, Kazuhiro | en |
dc.contributor.alternative | 入江, 一浩 | ja |
dc.date.accessioned | 2012-06-15T05:50:08Z | - |
dc.date.available | 2012-06-15T05:50:08Z | - |
dc.date.issued | 2011-06 | - |
dc.identifier.issn | 0916-8451 | - |
dc.identifier.uri | http://hdl.handle.net/2433/156509 | - |
dc.description.abstract | 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. | en |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | Japan Society for Bioscience, Biotechnology, and Agrochemistry | en |
dc.rights | © 2011 by Japan Society for Bioscience, Biotechnology, and Agrochemistry | en |
dc.subject | Aplog-1 | en |
dc.subject | aplysiatoxin | en |
dc.subject | bryostatin | en |
dc.subject | protein kinase C | en |
dc.subject | tumor promoter | en |
dc.title | Synthesis and Biological Evaluation of the 12,12-Dimethyl Derivative of Aplog-1, an Anti-Proliferative Analog of Tumor-Promoting Aplysiatoxin | en |
dc.type | journal article | - |
dc.type.niitype | Journal Article | - |
dc.identifier.ncid | AA10824164 | - |
dc.identifier.jtitle | Bioscience, Biotechnology, and Biochemistry | en |
dc.identifier.volume | 75 | - |
dc.identifier.issue | 6 | - |
dc.identifier.spage | 1167 | - |
dc.identifier.epage | 1173 | - |
dc.relation.doi | 10.1271/bbb.110130 | - |
dc.textversion | publisher | - |
dc.identifier.pmid | 21670518 | - |
dc.relation.url | https://www.jstage.jst.go.jp/article/bbb/75/6/75_110130/_article | - |
dcterms.accessRights | open access | - |
dc.identifier.eissn | 1347-6947 | - |
出現コレクション: | 学術雑誌掲載論文等 |
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