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  • 标题:Characterization of (−)-Matairesinol as a Potent Inhibitor of Casein Kinase I in Vitro
  • 本地全文:下载
  • 作者:Takamasa Yokoyama ; Maiko Okano ; Toshiro Noshita
  • 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
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