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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
8
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pubmed:dateCreated |
2008-8-25
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pubmed:databankReference |
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pubmed:abstractText |
Pyrrole-imidazole polyamide (PIP) is a nuclease-resistant novel compound that inhibits gene expression through binding to the minor groove of DNA. Human aurora kinase-A (AURKA) and -B (AURKB) are important regulators in mitosis during the cell cycle. In this study, two specific PIPs (PIP-A and PIP-B) targeting AURKA and AURKB promoter regions were designed and synthesized, and their biological effects were investigated by several in vitro assays. PIP-A and PIP-B significantly inhibited the promoter activities, mRNA expression, and protein levels of AURKA and AURKB, respectively, in a concentration-dependent manner. Moreover, 1:1 combination treatment with both PIPs demonstrated prominent antiproliferative synergy (CI value [ED(50)] = 0.256) to HeLa cells as a result of inducing apoptosis-mediated severe catastrophe of cell-cycle progression. The novel synthesized PIP-A and PIP-B are potent and specific gene-silencing agents for AURKA and AURKB.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
1074-5521
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pubmed:author |
pubmed-author:AoyamaTakahikoT,
pubmed-author:AsamiYukihiroY,
pubmed-author:BandoToshikazuT,
pubmed-author:FukudaNoboruN,
pubmed-author:HaradaYuichiY,
pubmed-author:HayashiNariyukiN,
pubmed-author:IgarashiJunJ,
pubmed-author:KanouHisaoH,
pubmed-author:KitamuraEikoE,
pubmed-author:KumamotoSatoshiS,
pubmed-author:KurodaKazumichiK,
pubmed-author:MatsumotoYoshiakiY,
pubmed-author:MorohashiAikoA,
pubmed-author:NagaseHirokiH,
pubmed-author:SaitoKosukeK,
pubmed-author:ShinojimaYuiY,
pubmed-author:SugiyamaHiroshiH,
pubmed-author:SuzukiTsukasaT,
pubmed-author:TakahashiTeruyukiT,
pubmed-author:TakasuToshiakiT,
pubmed-author:WangXiaofeiX,
pubmed-author:WatanabeTakayoshiT,
pubmed-author:Yoshida-NoroChikakoC
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pubmed:issnType |
Print
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pubmed:day |
25
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pubmed:volume |
15
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
829-41
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pubmed:dateRevised |
2011-7-11
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pubmed:meshHeading |
pubmed-meshheading:18721754-Amino Acid Sequence,
pubmed-meshheading:18721754-Animals,
pubmed-meshheading:18721754-Apoptosis,
pubmed-meshheading:18721754-Cattle,
pubmed-meshheading:18721754-Cell Cycle,
pubmed-meshheading:18721754-Cell Survival,
pubmed-meshheading:18721754-DNA,
pubmed-meshheading:18721754-Drug Design,
pubmed-meshheading:18721754-Fluorescein-5-isothiocyanate,
pubmed-meshheading:18721754-Fluorescent Dyes,
pubmed-meshheading:18721754-Gene Deletion,
pubmed-meshheading:18721754-Gene Expression Regulation, Enzymologic,
pubmed-meshheading:18721754-HeLa Cells,
pubmed-meshheading:18721754-Humans,
pubmed-meshheading:18721754-Imidazoles,
pubmed-meshheading:18721754-Molecular Sequence Data,
pubmed-meshheading:18721754-Nylons,
pubmed-meshheading:18721754-Promoter Regions, Genetic,
pubmed-meshheading:18721754-Protein-Serine-Threonine Kinases,
pubmed-meshheading:18721754-Pyrroles,
pubmed-meshheading:18721754-RNA, Messenger,
pubmed-meshheading:18721754-Substrate Specificity
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pubmed:year |
2008
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pubmed:articleTitle |
Development of pyrrole-imidazole polyamide for specific regulation of human aurora kinase-A and -B gene expression.
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pubmed:affiliation |
Advanced Research Institute for the Sciences and Humanities, Nihon University, Tokyo, Japan. teruyuk@med.nihon-u.ac.jp
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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