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dc.contributor.authorHanaki, Yusukeen
dc.contributor.authorYanagita, Ryo Cen
dc.contributor.authorSugahara, Takahiroen
dc.contributor.authorAida, Misakoen
dc.contributor.authorTokuda, Harukunien
dc.contributor.authorSuzuki, Nobutakaen
dc.contributor.authorIrie, Kazuhiroen
dc.contributor.alternative入江, 一浩ja
dc.date.accessioned2015-12-04T06:55:50Z-
dc.date.available2015-12-04T06:55:50Z-
dc.date.issued2015-
dc.identifier.issn0916-8451-
dc.identifier.urihttp://hdl.handle.net/2433/202083-
dc.descriptionPublished online: 23 Jan 2015en
dc.description.abstractAplog-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.en
dc.format.mimetypeapplication/pdf-
dc.language.isoeng-
dc.publisherTaylor & Francis Groupen
dc.rightsThis 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.en
dc.rightsThe 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'.en
dc.rights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。ja
dc.rightsThis is not the published version. Please cite only the published version.en
dc.subjectaplysiatoxinen
dc.subjectanti-proliferativeen
dc.subjectprotein kinase Cen
dc.subjecttumor promoteren
dc.titleSynthesis and biological activities of the amide derivative of aplog-1, a simplified analog of aplysiatoxin with anti-proliferative and cytotoxic activities.en
dc.typejournal article-
dc.type.niitypeJournal Article-
dc.identifier.ncidAA10824164-
dc.identifier.jtitleBioscience, biotechnology, and biochemistryen
dc.identifier.volume79-
dc.identifier.issue6-
dc.identifier.spage888-
dc.identifier.epage895-
dc.relation.doi10.1080/09168451.2014.1002452-
dc.textversionauthor-
dc.startdate.bitstreamsavailable2016-01-23-
dc.identifier.pmid25612633-
dcterms.accessRightsopen access-
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