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09168451.2014.1002452.pdf | 1.93 MB | Adobe PDF | 見る/開く |
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dc.contributor.author | Hanaki, Yusuke | en |
dc.contributor.author | Yanagita, Ryo C | en |
dc.contributor.author | Sugahara, Takahiro | en |
dc.contributor.author | Aida, Misako | en |
dc.contributor.author | Tokuda, Harukuni | en |
dc.contributor.author | Suzuki, Nobutaka | en |
dc.contributor.author | Irie, Kazuhiro | en |
dc.contributor.alternative | 入江, 一浩 | ja |
dc.date.accessioned | 2015-12-04T06:55:50Z | - |
dc.date.available | 2015-12-04T06:55:50Z | - |
dc.date.issued | 2015 | - |
dc.identifier.issn | 0916-8451 | - |
dc.identifier.uri | http://hdl.handle.net/2433/202083 | - |
dc.description | Published online: 23 Jan 2015 | en |
dc.description.abstract | 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. | en |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | Taylor & Francis Group | en |
dc.rights | 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. | en |
dc.rights | 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'. | 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.rights | This is not the published version. Please cite only the published version. | en |
dc.subject | aplysiatoxin | en |
dc.subject | anti-proliferative | en |
dc.subject | protein kinase C | en |
dc.subject | tumor promoter | en |
dc.title | Synthesis and biological activities of the amide derivative of aplog-1, a simplified analog of aplysiatoxin with anti-proliferative and cytotoxic activities. | 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 | 79 | - |
dc.identifier.issue | 6 | - |
dc.identifier.spage | 888 | - |
dc.identifier.epage | 895 | - |
dc.relation.doi | 10.1080/09168451.2014.1002452 | - |
dc.textversion | author | - |
dc.startdate.bitstreamsavailable | 2016-01-23 | - |
dc.identifier.pmid | 25612633 | - |
dcterms.accessRights | open access | - |
出現コレクション: | 学術雑誌掲載論文等 |
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