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dc.contributor.authorNAKAGAWA, Yuen
dc.contributor.authorKIKUMORI, Masayukien
dc.contributor.authorYANAGITA, Ryo C.en
dc.contributor.authorMURAKAMI, Akiraen
dc.contributor.authorTOKUDA, Harukunien
dc.contributor.authorNAGAI, Hiroshien
dc.contributor.authorIRIE, Kazuhiroen
dc.contributor.alternative入江, 一浩ja
dc.date.accessioned2012-06-15T05:50:08Z-
dc.date.available2012-06-15T05:50:08Z-
dc.date.issued2011-06-
dc.identifier.issn0916-8451-
dc.identifier.urihttp://hdl.handle.net/2433/156509-
dc.description.abstractAplog-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.mimetypeapplication/pdf-
dc.language.isoeng-
dc.publisherJapan Society for Bioscience, Biotechnology, and Agrochemistryen
dc.rights© 2011 by Japan Society for Bioscience, Biotechnology, and Agrochemistryen
dc.subjectAplog-1en
dc.subjectaplysiatoxinen
dc.subjectbryostatinen
dc.subjectprotein kinase Cen
dc.subjecttumor promoteren
dc.titleSynthesis and Biological Evaluation of the 12,12-Dimethyl Derivative of Aplog-1, an Anti-Proliferative Analog of Tumor-Promoting Aplysiatoxinen
dc.typejournal article-
dc.type.niitypeJournal Article-
dc.identifier.ncidAA10824164-
dc.identifier.jtitleBioscience, Biotechnology, and Biochemistryen
dc.identifier.volume75-
dc.identifier.issue6-
dc.identifier.spage1167-
dc.identifier.epage1173-
dc.relation.doi10.1271/bbb.110130-
dc.textversionpublisher-
dc.identifier.pmid21670518-
dc.relation.urlhttps://www.jstage.jst.go.jp/article/bbb/75/6/75_110130/_article-
dcterms.accessRightsopen access-
dc.identifier.eissn1347-6947-
Appears in Collections:Journal Articles

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