Characterization of (-)-Matairesinol as a Potent Inhibitor of Casein Kinase I in Vitro
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概要
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The inhibitory effects of (-) -matairesinol (MTS) isolated from Thujopsis dolubrata var. hondai on the activities of four distinct Ser/Thr-protein kinases [two casein kinases (CK-I and CK-II), A-kinase and C-kinase] were determined in vitro. It was found that (I) MTS inhibits the activities of CK-I and C-kinase α (ID_50=approx. 10μM) in a dose-depedent manner, but high doses are required to inhibit A-kinase activity (ID_50=approx. 90μM); (ii) the autophosphorylation of CK-I is more sensitive to MTS (ID_50=approx. 0. 2μM); (iii) MTS inhibits CK-I activity in a manner similar to that observed with CK-I-7 (a CK-I inhibitor); and (iv) the compound inhibits CK-I activity by affecting ATP binding in a mixed type manner. These results indicate that MTS is a potent CK-I inhibitor in vitro.
- 公益社団法人日本薬学会の論文
- 2003-03-01
著者
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Okano M
Kitasato Univ. Sagamihara Jpn
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大村 三男
Fruit Tree Research Station
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Omura M
Okitsu Branch Fruit Tree Research Station Ministry Of Agriculture Forestry And Fisheries
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Omura Mitsuo
Faculty Of Pharmacy Meijo University
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Ohtsuki Kenzo
Genetical Biochem. Kitasato Univ.
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FUNAYAMA Shinji
Department of Kampo Pharmaceutical Sciences, Nihon Pharmaceutical University
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Yokoyama T
Kitasato Univ. Sagamihara Jpn
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Yokoyama T
Kyoto Pharmaceutical Univ. Kyoto Jpn
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Noshita Toshiro
Department of Clinical Pharmacy, Faculty of Pharmaceutical Sciences, Aomori University
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YOKOYAMA Takamasa
Genetical Biochemistry and Signal Biology, Graduate School of Medical Sciences, Kitasato University
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Yokoyama Takamasa
Laboratory Of Genetical Biochemistry And Signal Biology Graduate School Of Medical Sciences Kitasato
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Yokoyama Takamasa
Genetical Biochemistry And Signal Biology Graduate School Of Medical Sciences Kitasato University
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OKANO Maiko
Genetical Biochemistry, Graduate School of Medical Sciences, Kitasato University
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Ohtsuki K
Laboratory Of Genetical Biochemistry And Signal Biology Graduate School Of Medical Sciences Kitasato
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Funayama Shinji
Department Of Bioscience And Biotechnology Aomori University
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Funayama Shinji
Department Of Bioscience And Biotechnology
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Ohyama M
Cancer Prevenition Division National Cancer Center Research Instiute
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Noshita Toshiro
Department Of Bioscience And Biotechnology
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Ohtsuki Kenzo
Laboratory Of Genetical Biochemistry And Signal Biology Graduate School Of Medical Sciences Kitasato
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