文章基本信息

标题：Characterization of (−)-Matairesinol as a Potent Inhibitor of Casein Kinase I in Vitro
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作者：Takamasa Yokoyama ; Maiko Okano ; Toshiro Noshita 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2003
卷号：26
期号：3
页码：371-374
DOI：10.1248/bpb.26.371
出版社：The Pharmaceutical Society of Japan
摘要：The inhibitory effects of (−)-matairesinol (MTS) isolated from Thujopsis dolabrata 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 (ID₅₀=approx. 10 μ M ) in a dose-depedent manner, but high doses are required to inhibit A-kinase activity (ID₅₀=approx. 90 μ M ); (ii) the autophosphorylation of CK-I is more sensitive to MTS (ID₅₀=approx. 0.2 μ M ); (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 .
关键词：casein kinase I;(−)-matairesinol;potent CK-I inhibitor;Thujopsis dolabrata var. hondai