INHIBITION OF CDP-DG - INOSITOL TRANSFERASE BY INOSTAMYCIN

被引:23
作者
IMOTO, M [1 ]
TANIGUCHI, Y [1 ]
UMEZAWA, K [1 ]
机构
[1] KEIO UNIV,FAC SCI & TECHNOL,APPL CHEM,3-14-1 HIYOSHI,KOHOKU KU,YOKOHAMA,KANAGAWA 223,JAPAN
关键词
D O I
10.1093/oxfordjournals.jbchem.a123894
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Inostamycin, a novel microbial secondary metabolite, inhibited [H-3]inositol and P-32(i) incorporation into phosphatidylinositol (PtdIns) induced by epidermal growth factor (EGF) in cultured A431 cells, the IC50 being 0.5-mu-g/ml, without inhibiting macromolecular synthesis. The drug inhibited cellular inositol phosphate formation only when it was added at the same time as labeled inositol. It was found to inhibit in vitro CDP-DG:inositol transferase activity of the A431 cell membrane, the IC50 being about 0.02-mu-g/ml. It did not inhibit tyrosine kinase, PtdIns phospholipase C, or PtdIns kinase. Therefore, inhibition of PtdIns turnover by inostamycin must be due to the inhibition of CDP-DG: inositol transferase. Thus, inostamycin is a novel inhibitor of CDP-DG:inositol transferase.
引用
收藏
页码:299 / 302
页数:4
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