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dc.contributor.authorIrie, Kazuhiroen
dc.contributor.authorYanagita, Ryo Cen
dc.contributor.alternative入江, 一浩ja
dc.date.accessioned2015-09-11T06:19:42Z-
dc.date.available2015-09-11T06:19:42Z-
dc.date.issued2014-04-
dc.identifier.issn1527-8999-
dc.identifier.urihttp://hdl.handle.net/2433/199854-
dc.description.abstractProtein kinase C (PKC) isozymes play central roles in signal transduction on the cell surface and could serve as promising therapeutic targets of intractable diseases like cancer, Alzheimer's disease, and acquired immunodeficiency syndrome (AIDS). Although natural PKC ligands like phorbol esters, ingenol esters, and teleocidins have the potential to become therapeutic leads, most of them are potent tumor promoters in mouse skin. By contrast, bryostatin-1 (bryo-1) isolated from marine bryozoan is a potent PKC activator with little tumor-promoting activity. Numerous investigations have suggested bryo-1 to be a promising therapeutic candidate for the above intractable diseases. However, there is a supply problem of bryo-1 both from natural sources and by organic synthesis. Recent approaches on the synthesis of bryo-1 have focused on its simplification, without decreasing the ability to activate PKC isozymes, to develop new medicinal leads. Another approach is to use the skeleton of natural PKC ligands to develop bryo-1 surrogates. We have recently identified 10-methyl-aplog-1 (26), a simplified analog of tumor-promoting aplysiatoxin (ATX), as a possible therapeutic lead for cancer. This review summarizes recent investigations on the simplification of natural PKC ligands, bryo-1 and ATX, to develop potential medicinal leads.en
dc.format.mimetypeapplication/pdf-
dc.language.isoeng-
dc.publisherwileyen
dc.rightsThis is the peer reviewed version of the following article: Irie, K. and Yanagita, R. C. (2014), Synthesis and Biological Activities of Simplified Analogs of the Natural PKC Ligands, Bryostatin-1 and Aplysiatoxin. Chem. Rec., 14: 251–267, which has been published in final form at http://dx.doi.org/10.1002/tcr.201300036. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Self-Archiving.en
dc.rightsThis is not the published version. Please cite only the published version.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.subjectantitumor agentsen
dc.subjectantiproliferationen
dc.subjectaplysiatoxinen
dc.subjectprotein kinase Cen
dc.subjecttumor promotersen
dc.subject.meshAnimalsen
dc.subject.meshAntineoplastic Agents/chemical synthesisen
dc.subject.meshAntineoplastic Agents/pharmacologyen
dc.subject.meshAntineoplastic Agents/toxicityen
dc.subject.meshBryostatins/chemical synthesisen
dc.subject.meshBryostatins/pharmacologyen
dc.subject.meshBryostatins/toxicityen
dc.subject.meshCell Proliferation/drug effectsen
dc.subject.meshHumansen
dc.subject.meshIsoenzymes/antagonists & inhibitorsen
dc.subject.meshIsoenzymes/metabolismen
dc.subject.meshLigandsen
dc.subject.meshLyngbya Toxins/chemical synthesisen
dc.subject.meshLyngbya Toxins/pharmacologyen
dc.subject.meshLyngbya Toxins/toxicityen
dc.subject.meshProtein Kinase C/antagonists & inhibitorsen
dc.subject.meshProtein Kinase C/metabolismen
dc.subject.meshStructure-Activity Relationshipen
dc.titleSynthesis and biological activities of simplified analogs of the natural PKC ligands, bryostatin-1 and aplysiatoxin.en
dc.typejournal article-
dc.type.niitypeJournal Article-
dc.identifier.ncidAA11515019-
dc.identifier.jtitleThe Chemical Recorden
dc.identifier.volume14-
dc.identifier.issue2-
dc.identifier.spage251-
dc.identifier.epage267-
dc.relation.doi10.1002/tcr.201300036-
dc.textversionauthor-
dc.startdate.bitstreamsavailable2015-05-01-
dc.identifier.pmid24677503-
dcterms.accessRightsopen access-
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